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(S)-4-Methyl-2-(methylamino)pentanoic acid [4, 4-bis(4-fluorophenyl)butyl]amide hydrochloride, a novel calcium channel antagonist, is efficacious in several animal models of pain.
Song Y, Bowersox SS, Connor DT, Dooley DJ, Lotarski SM, Malone T, Miljanich G, Millerman E, Rafferty MF, Rock D, Roth BD, Schmidt J, Stoehr S, Szoke BG, Taylor C, Vartanian M, Wang YX. Song Y, et al. Among authors: taylor c. J Med Chem. 2000 Sep 21;43(19):3474-7. doi: 10.1021/jm000134n. J Med Chem. 2000. PMID: 11000000 No abstract available.
N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers.
Hu LY, Ryder TR, Rafferty MF, Cody WL, Lotarski SM, Miljanich GP, Millerman E, Rock DM, Song Y, Stoehr SJ, Taylor CP, Weber ML, Szoke BG, Vartanian MG. Hu LY, et al. Among authors: taylor cp. 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
The discovery of [1-(4-dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phen yl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia.
Hu LY, Ryder TR, Rafferty MF, Taylor CP, Feng MR, Kuo BS, Lotarski SM, Miljanich GP, Millerman E, Siebers KM, Szoke BG. Hu LY, et al. Among authors: taylor cp. Bioorg Med Chem. 2000 Jun;8(6):1203-12. doi: 10.1016/s0968-0896(00)00077-8. Bioorg Med Chem. 2000. PMID: 10896101
Carboxylate bioisosteres of gabapentin.
Burgos-Lepley CE, Thompson LR, Kneen CO, Osborne SA, Bryans JS, Capiris T, Suman-Chauhan N, Dooley DJ, Donovan CM, Field MJ, Vartanian MG, Kinsora JJ, Lotarski SM, El-Kattan A, Walters K, Cherukury M, Taylor CP, Wustrow DJ, Schwarz JB. Burgos-Lepley CE, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2333-6. doi: 10.1016/j.bmcl.2005.05.016. Epub 2005 Jun 8. Bioorg Med Chem Lett. 2006. PMID: 15946842
Carboxylate bioisosteres of pregabalin.
Schwarz JB, Colbry NL, Zhu Z, Nichelson B, Barta NS, Lin K, Hudack RA, Gibbons SE, Galatsis P, DeOrazio RJ, Manning DD, Vartanian MG, Kinsora JJ, Lotarski SM, Li Z, Dickerson MR, El-Kattan A, Thorpe AJ, Donevan SD, Taylor CP, Wustrow DJ. Schwarz JB, et al. Bioorg Med Chem Lett. 2006 Jul 1;16(13):3559-63. doi: 10.1016/j.bmcl.2006.03.083. Epub 2006 Apr 18. Bioorg Med Chem Lett. 2006. PMID: 16621528
7,932 results