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Page 1
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D. Guo L, et al. Among authors: nargund rp. ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. doi: 10.1021/acsmedchemlett.6b00314. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994747 Free PMC article.
Orphan G-protein-coupled receptors and natural ligand discovery.
Howard AD, McAllister G, Feighner SD, Liu Q, Nargund RP, Van der Ploeg LH, Patchett AA. Howard AD, et al. Among authors: nargund rp. Trends Pharmacol Sci. 2001 Mar;22(3):132-40. doi: 10.1016/s0165-6147(00)01636-9. Trends Pharmacol Sci. 2001. PMID: 11239576 Review.
Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics.
Palucki BL, Feighner SD, Pong S, McKee KK, Hreniuk DL, Tan C, Howard AD, Van der Ploeg LH, Patchett AA, Nargund RP. Palucki BL, et al. Among authors: nargund rp. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1955-7. doi: 10.1016/s0960-894x(01)00324-9. Bioorg Med Chem Lett. 2001. PMID: 11459669
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. Among authors: nargund rp. J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h. J Med Chem. 2002. PMID: 12361385
Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.
Sebhat IK, Lai Y, Barakat K, Ye Z, Tang R, Kalyani RN, Vongs A, Macneil T, Weinberg DH, Cabello MA, Maroto M, Teran A, Fong TM, Van der Ploeg LH, Patchett AA, Nargund RP. Sebhat IK, et al. Among authors: nargund rp. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5720-3. doi: 10.1016/j.bmcl.2006.11.084. Epub 2006 Dec 3. Bioorg Med Chem Lett. 2007. PMID: 17768046
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Guo L, Ye Z, Ujjainwalla F, Sings HL, Sebhat IK, Huber J, Weinberg DH, Tang R, MacNeil T, Tamvakopoulos C, Peng Q, MacIntyre E, van der Ploeg LH, Goulet MT, Wyvratt MJ, Nargund RP. Guo L, et al. Among authors: nargund rp. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3242-7. doi: 10.1016/j.bmcl.2008.04.049. Epub 2008 Apr 25. Bioorg Med Chem Lett. 2008. PMID: 18479920
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Ruenz M, Sargent BJ, Yet L, Kelly TM, Palyha O, Kan Y, Pan J, Chen H, Marsh DJ, Shearman LP, Strack AM, Metzger JM, Feighner SD, Tan C, Howard AD, Tamvakopoulos C, Peng Q, Guan XM, Reitman ML, Patchett AA, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: nargund rp. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1913-7. doi: 10.1016/j.bmcl.2010.01.154. Epub 2010 Feb 4. Bioorg Med Chem Lett. 2010. PMID: 20167483
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: nargund rp. 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
101 results