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Page 1
Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.
He S, Lai Z, Ye Z, Dobbelaar PH, Shah SK, Truong Q, Du W, Guo L, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Reibarkh M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang B, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: bakshi rk. ACS Med Chem Lett. 2014 Apr 21;5(7):748-53. doi: 10.1021/ml500028c. eCollection 2014 Jul 10. ACS Med Chem Lett. 2014. PMID: 25050159 Free PMC article.
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: bakshi rk. ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14. ACS Med Chem Lett. 2012. PMID: 24900499 Free PMC article.
SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists.
He S, Dobbelaar PH, Guo L, Ye Z, Liu J, Jian T, Truong Q, Shah SK, Du W, Qi H, Bakshi RK, Hong Q, Dellureficio JD, Sherer E, Pasternak A, Feng Z, Reibarkh M, Lin M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK. He S, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535. doi: 10.1016/j.bmcl.2016.02.022. Epub 2016 Feb 10. Bioorg Med Chem Lett. 2016. PMID: 26898814
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
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
Hong Q, Bakshi RK, Dellureficio J, He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Tang R, Kalyani RN, Macneil T, Vongs A, Rosenblum CI, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen D, Martin WJ, Chen AS, Metzger JM, Chen HY, Strack AM, Fong TM, Maclntyre E, Van der Ploeg LH, Wyvratt MJ, Nargund RP. Hong Q, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4483-6. doi: 10.1016/j.bmcl.2010.06.038. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20598533
Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.
He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Bakshi RK, Dellureficio JP, Hong Q, Weinberg DH, Macneil T, Tang R, Strack AM, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Fong TM, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4399-405. doi: 10.1016/j.bmcl.2010.06.062. Epub 2010 Jun 15. Bioorg Med Chem Lett. 2010. PMID: 20598882
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 of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity.
He S, Ye Z, Dobbelaar PH, Bakshi RK, Hong Q, Dellureficio JP, Sebhat IK, Guo L, Liu J, Jian T, Lai Y, Franklin CL, Reibarkh M, Holmes MA, Weinberg DH, MacNeil T, Tang R, Tamvakopoulos C, Peng Q, Miller RR, Stearns RA, Chen HY, Chen AS, Strack AM, Fong TM, Wyvratt MJ Jr, Nargund RP. He S, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6524-32. doi: 10.1016/j.bmcl.2010.09.049. Epub 2010 Sep 19. Bioorg Med Chem Lett. 2010. PMID: 20933410
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Hong Q, Bakshi RK, Palucki BL, Park MK, Ye Z, He S, Pollard PG, Sebhat IK, Liu J, Guo L, 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, Nargund RP. Hong Q, et al. Among authors: bakshi rk. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2330-4. doi: 10.1016/j.bmcl.2011.02.090. Epub 2011 Mar 1. Bioorg Med Chem Lett. 2011. PMID: 21439820
Discovery of MK-4409, a Novel Oxazole FAAH Inhibitor for the Treatment of Inflammatory and Neuropathic Pain.
Chobanian HR, Guo Y, Liu P, Chioda MD, Fung S, Lanza TJ, Chang L, Bakshi RK, Dellureficio JP, Hong Q, McLaughlin M, Belyk KM, Krska SW, Makarewicz AK, Martel EJ, Leone JF, Frey L, Karanam B, Madeira M, Alvaro R, Shuman J, Salituro G, Terebetski JL, Jochnowitz N, Mistry S, McGowan E, Hajdu R, Rosenbach M, Abbadie C, Alexander JP, Shiao LL, Sullivan KM, Nargund RP, Wyvratt MJ, Lin LS, DeVita RJ. Chobanian HR, et al. Among authors: bakshi rk. ACS Med Chem Lett. 2014 Apr 10;5(6):717-21. doi: 10.1021/ml5001239. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944750 Free PMC article.
56 results