The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27190600 |
48 |
Discovery of Novel Tricyclic Heterocycles as Potent and Selective DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. |
Merck Research Laboratories |
25164763 |
95 |
Design, synthesis and biological evaluation of 4-fluoropyrrolidine-2-carbonitrile and octahydrocyclopenta[b]pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors. |
Shanghai Institute Of Materia Medica |
25782055 |
9 |
Discovery of a Cyclic Boronic Acidß-Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases. |
Rempex Pharmaceuticals |
25457126 |
55 |
(R)-3-amino-1-((3aS,7aS)-octahydro-1H-indol-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one derivatives as potent inhibitors of dipeptidyl peptidase-4: design, synthesis, biological evaluation, and molecular modeling. |
Chinese Academy Of Sciences |
24617858 |
239 |
Extended structure-activity relationship and pharmacokinetic investigation of (4-quinolinoyl)glycyl-2-cyanopyrrolidine inhibitors of fibroblast activation protein (FAP). |
University Of Antwerp |
24660890 |
12 |
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. |
Merck |
23072865 |
59 |
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors. |
Toray Industries |
23121075 |
119 |
P2-substituted N-acylprolylpyrrolidine inhibitors of prolyl oligopeptidase: biochemical evaluation, binding mode determination, and assessment in a cellular model of synucleinopathy. |
University Of Antwerp |
22938786 |
86 |
Discovery of 3H-imidazo[4,5-c]quinolin-4(5H)-ones as potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. |
Dainippon Sumitomo Pharma |
22525314 |
159 |
Acylated Gly-(2-cyano)pyrrolidines as inhibitors of fibroblast activation protein (FAP) and the issue of FAP/prolyl oligopeptidase (PREP)-selectivity. |
University Of Antwerp (Ua) |
20718420 |
167 |
Substituted 4-carboxymethylpyroglutamic acid diamides as potent and selective inhibitors of fibroblast activation protein. |
National Health Research Institutes |
19375196 |
22 |
Synthesis and evaluation of structurally constrained imidazolidin derivatives as potent dipeptidyl peptidase IV inhibitors. |
Sichuan University |
19217790 |
68 |
Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes. |
Matrix Laboratories |
18331795 |
44 |
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors. |
Merck |
18201067 |
276 |
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines. |
Merck Research Laboratories |
17869513 |
112 |
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes. |
Merck Research Laboratories |
17331715 |
19 |
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors. |
Korea Research Institute Of Chemical Technology |
17822893 |
61 |
(3R,4S)-4-(2,4,5-Trifluorophenyl)-pyrrolidin-3-ylamine inhibitors of dipeptidyl peptidase IV: synthesis, in vitro, in vivo, and X-ray crystallographic characterization. |
Pfizer |
14584950 |
132 |
Design, synthesis, and SAR of potent and selective dipeptide-derived inhibitors for dipeptidyl peptidases. |
University Of Antwerp (Uia) |
8642568 |
28 |
Structure-activity relationships of boronic acid inhibitors of dipeptidyl peptidase IV. 1. Variation of the P2 position of Xaa-boroPro dipeptides. |
Boehringer Ingelheim Pharmaceuticals |
12270155 |
56 |
Development of potent and selective dipeptidyl peptidase II inhibitors. |
University Of Antwerp (Uia) |
22019046 |
35 |
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor. |
Sanwa Kagaku Kenkyusho |
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 |
21711053 |
106 |
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal? |
University Of Antwerp (Ua) |
21324688 |
36 |
1-((3S,4S)-4-amino-1-(4-substituted-1,3,5-triazin-2-yl) pyrrolidin-3-yl)-5,5-difluoropiperidin-2-one inhibitors of DPP-4 for the treatment of type 2 diabetes. |
Pfizer |
21320777 |
375 |
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors. |
Merck Research Laboratories |
20483603 |
106 |
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile: a potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV. |
National Health Research Institutes |
19643608 |
58 |
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor. |
Torrent Pharmaceuticals |
19833514 |
104 |
The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements. |
Santhera Pharmaceuticals (Switzerland) |
19576767 |
142 |
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV. |
Santhera Pharmaceuticals (Switzerland) |
19539471 |
130 |
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors. |
Merck |
19515557 |
47 |
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV. |
Santhera Pharmaceuticals (Switzerland) |
19285862 |
30 |
Piperidinyl-2-phenethylamino inhibitors of DPP-IV for the treatment of type 2 diabetes. |
Pfizer |
19275964 |
64 |
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor. |
Pfizer |
19269819 |
102 |
Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors. |
National Health Research Institutes |
19261480 |
113 |
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors. |
National Health Research Institutes |
18996694 |
30 |
Synthesis and biological evaluation of homopiperazine derivatives with beta-aminoacyl group as dipeptidyl peptidase IV inhibitors. |
Korea Research Institute Of Chemical Technology |
18602260 |
177 |
Discovery of conformationally rigid 3-azabicyclo[3.1.0]hexane-derived dipeptidyl peptidase-IV inhibitors. |
Ranbaxy Research Laboratories |
18556199 |
234 |
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads. |
University Of Antwerp |
18556198 |
125 |
Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 2: isoindoline containing inhibitors. |
University Of Antwerp |
17958345 |
75 |
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates. |
University Of Antwerp |
17827003 |
68 |
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. |
Merck Research Laboratories |
17562364 |
150 |
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
17544668 |
55 |
Synthesis, SAR, and X-ray structure of novel potent DPPIV inhibitors: oxadiazolyl ketones. |
Lg Life Sciences |
17502141 |
25 |
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors. |
Merck Research Laboratories |
17433672 |
16 |
Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin. |
Merck Research Laboratories |
17194587 |
106 |
3-[2-((2S)-2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-3-methyl-butyramide analogues as selective DPP-IV inhibitors for the treatment of type-II diabetes. |
National Health Research Institutes |
17055271 |
18 |
Synthesis and activity of a potent, specific azabicyclo[3.3.0]-octane-based DPP II inhibitor. |
Tufts University School Of Medicine |
16844373 |
25 |
Synthesis and dipeptidyl peptidase inhibition of N-(4-substituted-2,4-diaminobutanoyl)piperidines. |
Laboratory Of Medicinal Chemistry University Of Antwerp |
16722626 |
94 |
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization. |
Pfizer |
16168640 |
82 |
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV. |
Glaxosmithkline |
16085416 |
45 |
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7. |
Activx Biosciences |
16084722 |
55 |
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors. |
Activx Biosciences |
15927466 |
52 |
Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors. |
National Health Research Institutes |
15380217 |
87 |
Potent and selective proline derived dipeptidyl peptidase IV inhibitors. |
Merck |
15324904 |
52 |
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors. |
Merck |
15324903 |
49 |
Discovery of potent and selective beta-homophenylalanine based dipeptidyl peptidase IV inhibitors. |
Merck |
15293982 |
12 |
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes. |
Merck Research Laboratories |
15139769 |
87 |
Gamma-amino-substituted analogues of 1-[(S)-2,4-diaminobutanoyl]piperidine as highly potent and selective dipeptidyl peptidase II inhibitors. |
University Of Antwerp |
15012982 |
129 |
Diastereoselective synthesis and configuration-dependent activity of (3-substituted-cycloalkyl)glycine pyrrolidides and thiazolidides as dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
14980678 |
88 |
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors. |
Merck Research Laboratories |
14684294 |
79 |
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors. |
Merck |
12801240 |
105 |
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. |
Novartis Institute For Biomedical Research |
28442252 |
62 |
Approaches towards the development of chimeric DPP4/ACE inhibitors for treating metabolic syndrome. |
Ranbaxy Laboratories |
24003220 |
1 |
Evaluation of cancer dependence and druggability of PRP4 kinase using cellular, biochemical, and structural approaches. |
Sanofi Oncology |
20017516 |
11 |
Development of near-infrared fluorophore (NIRF)-labeled activity-based probes for in vivo imaging of legumain. |
Stanford University |
15582469 |
16 |
Identification and characterization of nonsubstrate based inhibitors of the essential dengue and West Nile virus proteases. |
University Of Alabama At Birmingham |
18760609 |
66 |
Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors. |
Philipps University Marburg |
19630403 |
19 |
Discovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the Treatment of Schizophrenia (dagger) dagger Coordinates of the PDE10A crystal structures have been depo |
Pfizer |
19422229 |
125 |
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13. |
Novartis |
19348415 |
52 |
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IkappaB kinase-beta (IKK-beta). |
Gsk |
19143533 |
44 |
Discovery and Structure-Activity Relationships of Trisubstituted Pyrimidines/Pyridines as Novel Calcium-Sensing Receptor Antagonists. |
Bristol-Myers Squibb |
19256504 |
18 |
Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-1 inhibitor. |
Astrazeneca |
19193011 |
49 |
Pyrido[2,3-d]pyrimidin-5-ones: A Novel Class of Antiinflammatory Macrophage Colony-Stimulating Factor-1 Receptor Inhibitors (dagger). |
Johnson & Johnson Pharmaceutical |
19056263 |
34 |
Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase. |
Gsk |