Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists

T R Ryder; L Y Hu; M F Rafferty; S M Lotarski; D M Rock; S J Stoehr; C P Taylor; M L Weber; G P Miljanich; E Millerman; B G Szoke

doi:10.1016/s0960-894x(99)00405-9

Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists

Bioorg Med Chem Lett. 1999 Aug 16;9(16):2453-8. doi: 10.1016/s0960-894x(99)00405-9.

Authors

T R Ryder¹, L Y Hu, M F Rafferty, S M Lotarski, D M Rock, S J Stoehr, C P Taylor, M L Weber, G P Miljanich, E Millerman, B G Szoke

Affiliation

¹ Department of Chemistry, Parke-Davis Pharmaceutical Research, Ann Arbor, MI 48105, USA.

PMID: 10476886
DOI: 10.1016/s0960-894x(99)00405-9

Abstract

Selective N-Type Voltage Sensitive Calcium Channel (VSCC) antagonists have shown utility in several models of pain and ischemia. We report the structure-activity relationship at the proximal phenyl group in a series of non-peptidyl VSCC blockers.

MeSH terms

Acoustic Stimulation
Amino Acid Sequence
Aniline Compounds / chemistry*
Aniline Compounds / pharmacology*
Aniline Compounds / therapeutic use
Animals
Calcium Channel Blockers / chemistry*
Calcium Channel Blockers / pharmacology*
Calcium Channel Blockers / therapeutic use
Leucine / analogs & derivatives*
Leucine / chemistry
Leucine / pharmacology
Leucine / therapeutic use
Mice
Mice, Inbred DBA
Molecular Sequence Data
Seizures / drug therapy
Seizures / physiopathology
Structure-Activity Relationship

Substances

Aniline Compounds
Calcium Channel Blockers
PD 181283
Leucine