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Page 1
4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency.
Bakshi RK, Rasmusson GH, Patel GF, Mosley RT, Chang B, Ellsworth K, Harris GS, Tolman RL. Bakshi RK, et al. J Med Chem. 1995 Aug 18;38(17):3189-92. doi: 10.1021/jm00017a001. J Med Chem. 1995. PMID: 7650670 No abstract available.
MK386: a potent, selective inhibitor of the human type 1 5alpha-reductase.
Ellsworth K, Azzolina B, Baginsky W, Bull H, Chang B, Cimis G, Mitra S, Toney J, Bakshi RK, Rasmusson GR, Tolman RL, Harris GS. Ellsworth K, et al. Among authors: bakshi rk. J Steroid Biochem Mol Biol. 1996 Jul;58(4):377-84. doi: 10.1016/0960-0760(96)00050-7. J Steroid Biochem Mol Biol. 1996. PMID: 8903421
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Sebhat IK, et al. J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h. J Med Chem. 2002. PMID: 12361385
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Bakshi RK, et al. Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3. doi: 10.1016/j.bmcl.2005.05.012. Bioorg Med Chem Lett. 2005. PMID: 15951175
Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.
Guo L, Ye Z, Liu J, He S, Bakshi RK, Sebhat IK, Dobbelaar PH, Hong Q, Jian T, Dellureficio JP, Tsou NN, Ball RG, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Chen HY, Chen AS, Martin WJ, MacIntyre DE, Strack AM, Fong TM, Wyvratt MJ, Nargund RP. Guo L, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4895-900. doi: 10.1016/j.bmcl.2010.06.068. Epub 2010 Jun 17. Bioorg Med Chem Lett. 2010. PMID: 20621473
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP. Ye Z, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. doi: 10.1016/j.bmcl.2005.05.109. Bioorg Med Chem Lett. 2005. PMID: 15982875
Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist.
He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Tsou NN, Ball RG, Cashen DE, Martin WJ, Weinberg DH, Macneil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Macintyre DE, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2106-10. doi: 10.1016/j.bmcl.2010.02.058. Epub 2010 Feb 19. Bioorg Med Chem Lett. 2010. PMID: 20207541
56 results