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Page 1
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
Liu P, Hu Z, DuBois BG, Moyes CR, Hunter DN, Zhu C, Kar NF, Zhu Y, Garfunkle J, Kang L, Chicchi G, Ehrhardt A, Woods A, Seo T, Woods M, van Heek M, Dingley KH, Pang J, Salituro GM, Powell J, Terebetski JL, Hornak V, Campeau LC, Lamberson J, Ujjainwalla F, Miller M, Stamford A, Wood HB, Kowalski T, Nargund RP, Edmondson SD. Liu P, et al. Among authors: nargund rp. ACS Med Chem Lett. 2015 Jul 10;6(8):936-41. doi: 10.1021/acsmedchemlett.5b00207. eCollection 2015 Aug 13. ACS Med Chem Lett. 2015. PMID: 26288697 Free PMC article.
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
Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.
Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: nargund rp. Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5. doi: 10.1016/j.bmcl.2004.10.020. Bioorg Med Chem Lett. 2005. PMID: 15582434
2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.
Palucki BL, Park MK, Nargund RP, Tang R, MacNeil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, Van der Ploeg LH, Patchett AA. Palucki BL, et al. Among authors: nargund rp. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1993-6. doi: 10.1016/j.bmcl.2005.02.068. Bioorg Med Chem Lett. 2005. PMID: 15808454
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. Among authors: nargund rp. 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
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
101 results