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31 results

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Page 1
Identification of a novel, orally bioavailable histamine H(3) receptor antagonist based on the 4-benzyl-(1H-imidazol-4-yl) template.
Aslanian R, Mutahi MW, Shih NY, McCormick KD, Piwinski JJ, Ting PC, Albanese MM, Berlin MY, Zhu X, Wong SC, Rosenblum SB, Jiang Y, West R, She S, Williams SM, Bryant M, Hey JA. Aslanian R, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2002 Mar 25;12(6):937-41. doi: 10.1016/s0960-894x(02)00055-0. Bioorg Med Chem Lett. 2002. PMID: 11958998
III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.
Kim SH, Anilkumar GN, Zawacki LG, Zeng Q, Yang DY, Shao Y, Dong G, Xu X, Yu W, Jiang Y, Jenh CH, Hall JW 3rd, Carroll CD, Hobbs DW, Baldwin JJ, McGuinness BF, Rosenblum SB, Kozlowski JA, Shankar BB, Shih NY. Kim SH, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2011 Dec 1;21(23):6982-6. doi: 10.1016/j.bmcl.2011.09.120. Epub 2011 Oct 5. Bioorg Med Chem Lett. 2011. PMID: 22018463
Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA. Yu W, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27282742
Optimization of potency and pharmacokinetics of tricyclic indole derived inhibitors of HCV NS5B polymerase. Identification of ester prodrugs with improved oral pharmacokinetics.
Venkatraman S, Velazquez F, Gavalas S, Wu W, Chen KX, Nair AG, Bennett F, Huang Y, Pinto P, Jiang Y, Selyutin O, Vibulbhan B, Zeng Q, Lesburg C, Duca J, Heimark L, Huang HC, Agrawal S, Jiang CK, Ferrari E, Li C, Kozlowski J, Rosenblum S, Shih NY, Njoroge FG. Venkatraman S, et al. Bioorg Med Chem. 2014 Jan 1;22(1):447-58. doi: 10.1016/j.bmc.2013.11.007. Epub 2013 Nov 13. Bioorg Med Chem. 2014. PMID: 24275348
I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.
Anilkumar GN, Lesburg CA, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Vaccaro H, Wang L, Bennett F, Chen KX, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Butkiewicz N, Feld B, Ferrari E, He Z, Jiang CK, Palermo RE, McMonagle P, Huang HC, Shih NY, Njoroge G, Kozlowski JA. Anilkumar GN, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5336-41. doi: 10.1016/j.bmcl.2011.07.021. Epub 2011 Jul 19. Bioorg Med Chem Lett. 2011. PMID: 21840715
Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.
Chen KX, Vibulbhan B, Yang W, Sannigrahi M, Velazquez F, Chan TY, Venkatraman S, Anilkumar GN, Zeng Q, Bennet F, Jiang Y, Lesburg CA, Duca J, Pinto P, Gavalas S, Huang Y, Wu W, Selyutin O, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG. Chen KX, et al. Among authors: rosenblum sb. J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148957
A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors.
Chen KX, Lesburg CA, Vibulbhan B, Yang W, Chan TY, Venkatraman S, Velazquez F, Zeng Q, Bennett F, Anilkumar GN, Duca J, Jiang Y, Pinto P, Wang L, Huang Y, Selyutin O, Gavalas S, Pu H, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG. Chen KX, et al. Among authors: rosenblum sb. J Med Chem. 2012 Mar 8;55(5):2089-101. doi: 10.1021/jm201322r. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22247956
Discovery of an irreversible HCV NS5B polymerase inhibitor.
Zeng Q, Nair AG, Rosenblum SB, Huang HC, Lesburg CA, Jiang Y, Selyutin O, Chan TY, Bennett F, Chen KX, Venkatraman S, Sannigrahi M, Velazquez F, Duca JS, Gavalas S, Huang Y, Pu H, Wang L, Pinto P, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Li C, Hesk D, Gesell J, Sorota S, Shih NY, Njoroge FG, Kozlowski JA. Zeng Q, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6585-7. doi: 10.1016/j.bmcl.2013.10.060. Epub 2013 Nov 6. Bioorg Med Chem Lett. 2013. PMID: 24252545
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
Nair AG, Wong MK, Shu Y, Jiang Y, Jenh CH, Kim SH, Yang DY, Zeng Q, Shao Y, Zawacki LG, Duo J, McGuinness BF, Carroll CD, Hobbs DW, Shih NY, Rosenblum SB, Kozlowski JA. Nair AG, et al. Among authors: rosenblum sb. Bioorg Med Chem Lett. 2014 Feb 15;24(4):1085-8. doi: 10.1016/j.bmcl.2014.01.009. Epub 2014 Jan 11. Bioorg Med Chem Lett. 2014. PMID: 24486132
31 results