The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27185330 |
60 |
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. |
Vanderbilt University Medical Center |
26988801 |
55 |
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents. |
Jagiellonian University Medical College |
26471092 |
23 |
Molecular hybridization yields triazole bronchodilators for the treatment of COPD. |
Pfizer |
26299349 |
66 |
Design and synthesis of N-[6-(Substituted Aminoethylideneamino)-2-Hydroxyindan-1-yl]arylamides as selective and potent muscarinic M1 agonists. |
Eli Lilly |
25893046 |
77 |
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5. |
Bristol-Myers Squibb |
25800115 |
62 |
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists. |
RhôNe-Poulenc Rorer |
24980056 |
44 |
Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites. |
Universit£ |
24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
25275964 |
171 |
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1). |
Universit£ |
25241924 |
47 |
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor. |
Novartis Institutes For Biomedical Research |
25147929 |
105 |
Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). |
Vanderbilt University Medical Center |
24844758 |
6 |
Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities. |
Keio University |
24805037 |
380 |
Novel arylsulfonamide derivatives with 5-HT6/5-HT7 receptor antagonism targeting behavioral and psychological symptoms of dementia. |
Adamed |
24690494 |
92 |
Antagonists of the kappa opioid receptor. |
The Scripps Research Institute |
18077164 |
40 |
Rapid novel divergent synthesis and muscarinic agonist profile of all four optical isomers of N,N,N-trimethyl(6-methyl-1,4-dioxan-2-yl)methanaminium iodide. |
Universit£ |
23953189 |
53 |
Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor. |
Pfizer |
23379472 |
187 |
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists. |
University Of Arkansas For Medical Sciences |
23200253 |
67 |
Further exploration of M1 allosteric agonists: subtle structural changes abolish M1 allosteric agonism and result in pan-mAChR orthosteric antagonism. |
Vanderbilt University Medical Center |
23177787 |
59 |
Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. |
Vanderbilt University Medical Center |
13678406 |
7 |
Synthesis and biological characterization of 1-methyl-1,2,5,6-tetrahydropyridyl-1,2,5-thiadiazole derivatives as muscarinic agonists for the treatment of neurological disorders. |
The University Of Toledo |
22047691 |
76 |
The discovery of AZD9164, a novel muscarinic M3 antagonist. |
Astrazeneca |
21036043 |
78 |
The discovery of new spirocyclic muscarinic M3 antagonists. |
Astrazeneca |
20709550 |
80 |
The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists. |
Glaxosmithkline |
20483611 |
89 |
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR. |
Glaxosmithkline |
20483599 |
81 |
2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling. |
Glaxosmithkline |
19896386 |
85 |
Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation. |
Universit£ |
19928767 |
88 |
Synthesis, affinity profile and functional activity of potent chiral muscarinic antagonists with a pyrrolidinylfuran structure. |
Universita Di Firenze |
19243945 |
73 |
M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines. |
Glaxosmithkline |
18818072 |
162 |
Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas. |
Glaxosmithkline |
18798607 |
27 |
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists. |
Glaxosmithkline |
18543900 |
105 |
Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonists. |
Universit£ |
18680280 |
34 |
Discovery of novel and long acting muscarinic acetylcholine receptor antagonists. |
Glaxosmithkline |
18595721 |
32 |
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics. |
Alma Mater Studiorum-University Of Bologna |
18455407 |
125 |
Muscarinic antagonists with multiple stereocenters: Synthesis, affinity profile and functional activity of isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine sulfoxide derivatives. |
Universit£ |
9548813 |
53 |
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo. |
Smithkline Beecham Pharmaceuticals |
12182854 |
45 |
A new series of M3 muscarinic antagonists based on the 4-amino-piperidine scaffold. |
Universit£ |
| 20 |
Design, synthesis and biological activity of some 4-DAMP- related compounds |
TBA |
23099092 |
74 |
Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups. |
Glaxosmithkline |
22959245 |
175 |
As(1) receptor pharmacophore derived from a series of N-substituted 4-azahexacyclo[5.4.1.0(2,6).0(3,10).0(5,9).0(8,11)]dodecan-3-ols (AHDs). |
The University Of Sydney |
23116186 |
68 |
Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687). |
Astrazeneca |
22931505 |
69 |
Chemokine receptor antagonists. |
National Heart And Lung Institute |
23062550 |
59 |
Synthesis and biological characterization of a series of novel diaryl amide M1 antagonists. |
Vanderbilt University Medical Center |
22335555 |
43 |
1,2,3,4-tetrahydroquinoline-based selective human neuronal nitric oxide synthase (nNOS) inhibitors: lead optimization studies resulting in the identification of N-(1-(2-(methylamino)ethyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophene-2-carboximidamide as a preclinical development candidate. |
Neuraxon |
21062081 |
47 |
Histamine H3 receptor as a drug discovery target. |
TBA |
24900202 |
38 |
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists. |
TBA |
22677319 |
64 |
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential. |
H. Lundbeck |
22749871 |
92 |
Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012. |
Vanderbilt University Medical Center |
22243489 |
75 |
1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists. |
Universit£ |
22607684 |
50 |
7-Azabicyclo[2.2.1]heptane as a scaffold for the development of selective sigma-2 (s2) receptor ligands. |
The University Of Sydney |
22542010 |
31 |
Discovery of a novel melanin concentrating hormone receptor 1 (MCHR1) antagonist with reduced hERG inhibition. |
Amgen |
22313227 |
78 |
Radiosynthesis and evaluation of an (18)F-labeled positron emission tomography (PET) radioligand for brain histamine subtype-3 receptors based on a nonimidazole 2-aminoethylbenzofuran chemotype. |
National Institute Of Mental Health |
22507963 |
73 |
Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. |
Vanderbilt University Medical Center |
22460029 |
21 |
Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists. |
Glaxosmithkline |
22230199 |
12 |
Unbiased binding assays for discovering small-molecule probes and drugs. |
Broad Institute Of Harvard And Mit |
21634396 |
55 |
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. |
Cephalon |
19630384 |
32 |
Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists. |
Glaxosmithkline |
21207959 |
69 |
Syntheses of 2-amino and 2-halothiazole derivatives as high-affinity metabotropic glutamate receptor subtype 5 ligands and potential radioligands for in vivo imaging. |
National Institute Of Mental Health |
20875743 |
90 |
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela |
Pfizer |
20931963 |
112 |
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome. |
Aska Pharmaceutical |
20684563 |
176 |
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. |
H. Lundbeck |
19963380 |
38 |
Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. |
Hunter College And The Graduate Center Of The City University Of New York |
19653626 |
111 |
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo |
RhôNe-Poulenc Rorer |
18468904 |
48 |
High specific activity tritium-labeled N-(2-methoxybenzyl)-2,5-dimethoxy-4-iodophenethylamine (INBMeO): a high-affinity 5-HT2A receptor-selective agonist radioligand. |
Purdue University |
18042383 |
20 |
Design and synthesis of a fluorescent muscarinic antagonist. |
Pfizer |
17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
17889543 |
90 |
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes. |
Universit£ |
16275087 |
78 |
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives. |
Ucb Pharma |
16198561 |
99 |
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis. |
Novartis Institutes For Biomedical Research |
14998318 |
112 |
Selective optimization of side activities: another way for drug discovery. |
Prestwick Chemical |
11831911 |
15 |
Cyclohexylmethylpiperidinyltriphenylpropioamide: a selective muscarinic M(3) antagonist discriminating against the other receptor subtypes. |
Banyu Tsukuba Research Institute |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities Of Lille |
9986705 |
290 |
Identification and characterization of m1 selective muscarinic receptor antagonists1. |
Warner-Lambert |
10354408 |
58 |
1-(1,2,5-Thiadiazol-4-yl)-4-azatricyclo[2.2.1.0(2,6)]heptanes as new potent muscarinic M1 agonists: structure-activity relationship for 3-aryl-2-propyn-1-yloxy and 3-aryl-2-propyn-1-ylthio derivatives. |
Novo Nordisk |
9622546 |
109 |
6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors. |
National Institute Of Diabetes And Digestive And Kidney Diseases |
7562938 |
17 |
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists. |
Wyeth-Ayerst Research |
8057277 |
54 |
Novel 1-phenylcycloalkanecarboxylic acid derivatives are potent and selective sigma 1 ligands. |
National Institute On Drug Abuse-Intramural Research Program |
2016720 |
4 |
Crystal, solution, and molecular modeling structural properties and muscarinic antagonist activity of azaprophen. |
Research Triangle Institute |
2738887 |
22 |
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates. |
Institute Of Research |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
10450949 |
24 |
Discovery of a highly potent, functionally-selective muscarinic M1 agonist, WAY-132983 using rational drug design and receptor modelling. |
Wyeth-Ayerst Research |
9873644 |
74 |
Identification of side chains on 1,2,5-thiadiazole-azacycles optimal for muscarinic m1 receptor activation. |
Novo Nordisk |
9873472 |
102 |
Identification and characterization of m4 selective muscarinic antagonists. |
Parke-Davis Pharmaceutical Research |
| 8 |
The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptor |
TBA |
22226656 |
75 |
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT6 receptor antagonist showing activity in rat social recognition test. |
Cephalon |
22197136 |
29 |
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists. |
Cephalon |
22197142 |
42 |
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012. |
Vanderbilt University Medical Center |
21930376 |
92 |
Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071. |
Vanderbilt University Medical Center |
21870878 |
61 |
Inhalation by design: novel tertiary amine muscarinic M3 receptor antagonists with slow off-rate binding kinetics for inhaled once-daily treatment of chronic obstructive pulmonary disease. |
Pfizer |
21788137 |
33 |
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma (s) receptor ligands. |
The University Of Sydney |
21865048 |
29 |
2-({6-[(3R)-3-amino-3-methylpiperidine-1-yl]-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydro-5H-pyrrolo[3,2-d]pyrimidine-5-yl}methyl)-4-fluorobenzonitrile (DSR-12727): a potent, orally active dipeptidyl peptidase IV inhibitor without mechanism-based inactivation of CYP3A. |
Dainippon Sumitomo Pharma |
21524581 |
105 |
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists. |
RhôNe-Poulenc Rorer |
21194936 |
39 |
Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe. |
Vanderbilt Institute Of Chemical Biology/Chemical Synthesis Core |
21146989 |
46 |
Trishomocubane as a scaffold for the development of selective dopamine transporter (DAT) ligands. |
The University Of Sydney |
20812727 |
157 |
Synthesis, structure-affinity relationships, and radiolabeling of selective high-affinity 5-HT4 receptor ligands as prospective imaging probes for positron emission tomography. |
National Institute Of Mental Health |
20801651 |
25 |
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. |
Vanderbilt University Medical Center |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical And Public Health Institute |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
20202841 |
47 |
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists. |
Vanderbilt University Medical Center |
19646882 |
72 |
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways. |
University Of Medicine And Dentistry Of New Jersey-Robert Wood Johnson Medical School And The Informatics Institute Of Umdnj |
19616944 |
27 |
Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD. |
Glaxosmithkline |
19199480 |
6 |
Discovery of imidazo[1,2-b]thiazole derivatives as novel SIRT1 activators. |
Sirtris Pharmaceuticals |
18922694 |
84 |
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists. |
Johnson & Johnson Prd |
7673927 |
6 |
Isolation and Structure of Two Novel Muscarinic Receptor Antagonists |
TBA |
8496700 |
16 |
The Role of Receptor Binding in Drug Discovery |
TBA |
| 14 |
Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligands |
TBA |
| 31 |
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists |
TBA |
| 88 |
A rationale for the design and synthesis of m1 selective muscarinic agonists. |
TBA |
| 8 |
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine. |
TBA |
19317446 |
51 |
Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists. |
Glaxosmithkline |
19208472 |
52 |
Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists. |
Novartis Institutes For Biomedical Research |
18829311 |
74 |
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen. |
Vanderbilt University Medical Center |
18817368 |
57 |
Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. |
Merck Research Laboratories |
18805692 |
99 |
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. |
Vanderbilt University Medical Center |
18507369 |
85 |
Designing selective, high affinity ligands of 5-HT1D receptor by covalent dimerization of 5-HT1F ligands derived from 4-fluoro-N-[3-(1-methyl-4-piperidinyl)-1H-indol-5-yl]benzamide. |
Theravance |
16038549 |
20 |
Nocardimicins A, B, C, D, E, and F, siderophores with muscarinic M3 receptor inhibiting activity from Nocardia sp. TP-A0674. |
Mitsubishi Pharma |
15844951 |
5 |
Cremastrine, a pyrrolizidine alkaloid from Cremastra appendiculata. |
Mitsubishi Pharma |
18032038 |
38 |
Development of CXCR3 antagonists. Part 3: Tropenyl and homotropenyl-piperidine urea derivatives. |
Ucb Pharma |
17911022 |
108 |
Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists. |
Glaxosmithkline |
17571866 |
49 |
Synthesis and simple 18F-labeling of 3-fluoro-5-(2-(2-(fluoromethyl)thiazol-4-yl)ethynyl)benzonitrile as a high affinity radioligand for imaging monkey brain metabotropic glutamate subtype-5 receptors with positron emission tomography. |
National Institute Of Mental Health |
17352463 |
59 |
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 2). |
Via Zambeletti 25 |
17352462 |
90 |
Discovery of diaryl imidazolidin-2-one derivatives, a novel class of muscarinic M3 selective antagonists (Part 1). |
Via Zambeletti 25 |
17188867 |
66 |
1,5-Benzodioxepin derivatives as a novel class of muscarinic M3 receptor antagonists. |
Mitsubishi Pharma |
16970392 |
91 |
Identification of a novel 4-aminomethylpiperidine class of M3 muscarinic receptor antagonists and structural insight into their M3 selectivity. |
Tsukuba Research Institute |
16722631 |
87 |
An integrated in silico 3D model-driven discovery of a novel, potent, and selective amidosulfonamide 5-HT1A agonist (PRX-00023) for the treatment of anxiety and depression. |
Predix Pharmaceuticals |
16458504 |
37 |
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand. |
Columbia University College Of Physicians And Surgeons |
16392798 |
46 |
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand. |
Columbia University College Of Physicians And Surgeons |
16143528 |
213 |
Synthesis of potent and selective serotonin 5-HT1B receptor ligands. |
Columbia University College Of Physicians And Surgeons |
16134937 |
154 |
6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode. |
7Tm Pharma |
15225708 |
32 |
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations. |
Schering-Plough Research Institute |
15115380 |
24 |
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a potent, highly selective, and orally bioavailable CCR5 antagoni |
Schering-Plough Research Institute |
15026073 |
28 |
Isopropyl amide derivatives of potent and selective muscarinic M2 receptor antagonists. |
Schering-Plough Research Institute |
12798328 |
87 |
Muscarinic M(3) receptor antagonists with (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxyphenylacetamide Structures. Part 2. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
12747793 |
32 |
C(8) substituted 1-azabicyclo[3.3.1]non-3-enes and C(8) substituted 1-azabicyclo[3.3.1]nonan-4-ones: novel muscarinic receptor antagonists. |
University Of North Carolina At Chapel Hill |
12565973 |
33 |
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides. |
Schering-Plough Research Institute |
12459007 |
13 |
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists. |
Schering-Plough Research Institute |
12086500 |
59 |
Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity. |
Schering-Plough Research Institute |
11909724 |
35 |
Sulfide analogues as potent and selective M(2) muscarinic receptor antagonists. |
Schering-Plough Research Institute |
11859005 |
24 |
Synthesis and structure-activity relationships of M(2)-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family. |
Schering-Plough Research Institute |
11859004 |
18 |
Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands. |
Schering-Plough Research Institute |
11708906 |
15 |
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators. |
University Of Bologna |
11585438 |
21 |
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoromethyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-oxide (Sch-350634), an orally bioavailable, potent CCR5 antagonist. |
Schering-Plough Research Institute |
11527721 |
12 |
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution. |
Schering-Plough Research Institute |
11514156 |
28 |
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element. |
Schering-Plough Research Institute |
11378358 |
254 |
Synthesis of potent and selective dopamine D(4) antagonists as candidate radioligands. |
Columbia University College Of Physicians And Surgeons |
11294385 |
21 |
Design and synthesis of ether analogues as potent and selective M2 muscarinic receptor antagonists. |
Schering-Plough Research Institute |
11150173 |
120 |
A potent, long-acting, orally active (2R)-2-[(1R)-3, 3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: novel muscarinic M(3) receptor antagonist with high selectivity for M(3) over M(2) receptors. |
Banyu Tsukuba Research Institute In Collaboration With Merck Research Laboratories |
11133078 |
20 |
Benzylidene ketal derivatives as M2 muscarinic receptor antagonists. |
Schering-Plough Research Institute |
11055332 |
42 |
Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor. |
Schering-Plough Research Institute |
11055330 |
30 |
Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists. |
Schering-Plough Research Institute |
11012031 |
57 |
Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency. |
Schering-Plough Research Institute |
10891110 |
87 |
6beta-Acyloxy(nor)tropanes: affinities for antagonist/agonist binding sites on transfected and native muscarinic receptors. |
National Institute Of Diabetes And Digestive And Kidney Diseases |
10612600 |
14 |
First fatty acylated dipeptides to affect muscarinic receptor ligand binding. |
University Of Toledo |
10498210 |
27 |
A new class of selective and potent inhibitors of neuronal nitric oxide synthase. |
Pfizer |
10206558 |
50 |
Design, synthesis, and structure-activity relationship studies of himbacine derived muscarinic receptor antagonists. |
Schering-Plough Research Institute |
9651157 |
52 |
Design and synthesis of m1-selective muscarinic agonists: (R)-(-)-(Z)-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-(3'-methoxyphenyl)-2-propynyl)oxime maleate (CI-1017), a functionally m1-selective muscarinic agonist. |
Warner-Lambert |
9438027 |
30 |
Conformationally constrained analogues of the muscarinic agonist 3-(4-(methylthio)-1,2,5-thiadiazol-3-yl)-1,2,5,6-tetrahydro-1-methylpyr idine. Synthesis, receptor affinity, and antinociceptive activity. |
Novo Nordisk |
9435896 |
36 |
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere. |
Smithkline Beecham Pharmaceuticals |
7990109 |
62 |
Bioisosteres of arecoline: 1,2,3,6-tetrahydro-5-pyridyl-substituted and 3-piperidyl-substituted derivatives of tetrazoles and 1,2,3-triazoles. Synthesis and muscarinic activity. |
H. Lundbeck |
7853341 |
115 |
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships. |
Uppsala University |
7783150 |
33 |
Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. |
Royal Danish School Of Pharmacy |
1578479 |
24 |
Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology. |
Uppsala University |
1560441 |
35 |
Muscarinic receptor subtype specificity of (N,N-dialkylamino)alkyl 2-cyclohexyl-2-phenylpropionates: cylexphenes (cyclohexyl-substituted aprophen analogues). |
Institute Of Research |
1548680 |
12 |
Synthesis and in vitro biological profile of all four isomers of the potent muscarinic agonist 3-(3-methyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane. |
Merck Sharp And Dohme Research Laboratories |
1507203 |
96 |
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine. |
University Of South Carolina |
26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
23548908 |
1 |
Inhibition of isoleucyl-tRNA synthetase as a potential treatment for human African Trypanosomiasis. |
University Of Washington |
26518975 |
9 |
Synthesis, Antifolate and Anticancer Activities of N(5) -Substituted 8,10-Dideazatetrahydrofolate Analogues. |
Peking University |
26077890 |
33 |
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids. |
Tehran University Of Medical Sciences |
26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University Of Leipzig |
26390252 |
12 |
Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer. |
Dana-Farber Cancer Institute |
26174207 |
21 |
Hydroxybenzaldoximes Are D-GAP-Competitive Inhibitors of E. coli 1-Deoxy-D-Xylulose-5-Phosphate Synthase. |
The Johns Hopkins University School Of Medicine |
25462626 |
6 |
Organocatalyzed solvent free an efficient novel synthesis of 2,4,5-trisubstituted imidazoles for a-glucosidase inhibition to treat diabetes. |
Comsats Institute Of Information Technology |
23547776 |
25 |
Development of an ALK2-Biased BMP Type I Receptor Kinase Inhibitor. |
Massachusetts Institute Of Technology |
12773052 |
14 |
Novel indolyl aryl sulfones active against HIV-1 carrying NNRTI resistance mutations: synthesis and SAR studies. |
Sapienza University Of Rome |