doi: 10.1016/s0960-894x(99)00284-x.
Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers
Affiliations
- PMID: 10406647
- DOI: 10.1016/s0960-894x(99)00284-x
Item in Clipboard
Multiple parallel synthesis of N,N-dialkyldipeptidylamines as N-type calcium channel blockers
Bioorg Med Chem Lett.
.
Abstract
Selective N-type Voltage Sensitive Calcium Channel (VSCC) blockers have shown utility in several models of stroke and pain. A series of N,N-dialkyldipeptidylamines with potent functional activity at N-type VSCC's has been identified. Multiple parallel synthesis of a focused array of thirty compounds using polymer-supported quenching reagents and preliminary pharmacology are presented. Eighteen compounds were identified with an IC50 below 1 microM in an in vitro functional assay.
Similar articles
-
N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.Bioorg Med Chem Lett. 1999 Mar 22;9(6):907-12. doi: 10.1016/s0960-894x(99)00100-6. Bioorg Med Chem Lett. 1999. PMID: 10206559
-
Structure-activity relationship at the leucine side chain in a series of N,N-dialkyldipeptidyl-amines as N-type calcium channel blockers.Drug Des Discov. 2000;16(4):317-22. Drug Des Discov. 2000. PMID: 10807036
-
Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.Bioorg Med Chem Lett. 1999 Apr 19;9(8):1121-6. doi: 10.1016/s0960-894x(99)00160-2. Bioorg Med Chem Lett. 1999. PMID: 10328297
-
Structure-activity relationship of N-methyl-N-aralkyl-peptidylamines as novel N-type calcium channel blockers.Bioorg Med Chem Lett. 1999 Aug 2;9(15):2151-6. doi: 10.1016/s0960-894x(99)00359-5. Bioorg Med Chem Lett. 1999. PMID: 10465535
-
Synthesis and structure-activity relationship of substituted 1,2,3,4-tetrahydroisoquinolines as N-type calcium channel blockers.Bioorg Med Chem Lett. 1998 Sep 22;8(18):2415-8. doi: 10.1016/s0960-894x(98)00440-5. Bioorg Med Chem Lett. 1998. PMID: 9873552
Cited by
-
Molecular modelling and QSAR analysis of some structurally diverse N-type calcium channel blockers.J Mol Model. 2010 Apr;16(4):629-44. doi: 10.1007/s00894-009-0591-1. Epub 2009 Oct 4. J Mol Model. 2010. PMID: 19802636
-
Targeting voltage-gated calcium channels in neurological and psychiatric diseases.Nat Rev Drug Discov. 2016 Jan;15(1):19-34. doi: 10.1038/nrd.2015.5. Epub 2015 Nov 6. Nat Rev Drug Discov. 2016. PMID: 26542451 Review.
-
Acute visceral pain relief mediated by A3AR agonists in rats: involvement of N-type voltage-gated calcium channels.Pain. 2020 Sep 1;161(9):2179-2190. doi: 10.1097/j.pain.0000000000001905. Pain. 2020. PMID: 32379223 Free PMC article.
-
Calcium channel blockers and pain therapy.Curr Rev Pain. 2000;4(6):488-98. doi: 10.1007/s11916-000-0073-8. Curr Rev Pain. 2000. PMID: 11060595 Review.
-
The Physiology, Pathology, and Pharmacology of Voltage-Gated Calcium Channels and Their Future Therapeutic Potential.Pharmacol Rev. 2015 Oct;67(4):821-70. doi: 10.1124/pr.114.009654. Pharmacol Rev. 2015. PMID: 26362469 Free PMC article. Review.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Chemical Information
