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Page 1
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: chintala m. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
Discovery of a vorapaxar analog with increased aqueous solubility.
Xia Y, Chackalamannil S, Greenlee WJ, Wang Y, Hu Z, Root Y, Wong J, Kong J, Ahn HS, Boykow G, Hsieh Y, Kurowski S, Chintala M. Xia Y, et al. Among authors: chintala m. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6676-9. doi: 10.1016/j.bmcl.2010.09.009. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20888225
Himbacine-derived thrombin receptor antagonists: c7-spirocyclic analogues of vorapaxar.
Chelliah MV, Eagen K, Guo Z, Chackalamannil S, Xia Y, Tsai H, Greenlee WJ, Ahn HS, Kurowski S, Boykow G, Hsieh Y, Chintala M. Chelliah MV, et al. Among authors: chintala m. ACS Med Chem Lett. 2014 Mar 11;5(5):561-5. doi: 10.1021/ml500008w. eCollection 2014 May 8. ACS Med Chem Lett. 2014. PMID: 24900880 Free PMC article.
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.
Clasby MC, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee WJ, Lin Y, Tsai H, Xia Y, Ahn HS, Agans-Fantuzzi J, Boykow G, Chintala M, Foster C, Bryant M, Lau J. Clasby MC, et al. Among authors: chintala m. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1544-8. doi: 10.1016/j.bmcl.2005.12.042. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16380251
Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring.
Xia Y, Chackalamannil S, Clasby M, Doller D, Eagen K, Greenlee WJ, Tsai H, Agans-Fantuzzi J, Ahn HS, Boykow GC, Hsieh Y, Lunn CA, Chintala M. Xia Y, et al. Among authors: chintala m. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4509-13. doi: 10.1016/j.bmcl.2007.06.002. Epub 2007 Jun 15. Bioorg Med Chem Lett. 2007. PMID: 17574850
Discovery of nor-seco himbacine analogs as thrombin receptor antagonists.
Chelliah MV, Chackalamannil S, Xia Y, Eagen K, Greenlee WJ, Ahn HS, Agans-Fantuzzi J, Boykow G, Hsieh Y, Bryant M, Chan TM, Chintala M. Chelliah MV, et al. Among authors: chintala m. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2544-9. doi: 10.1016/j.bmcl.2012.01.138. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22405832
Heterotricyclic himbacine analogs as potent, orally active thrombin receptor (protease activated receptor-1) antagonists.
Chelliah MV, Chackalamannil S, Xia Y, Eagen K, Clasby MC, Gao X, Greenlee W, Ahn HS, Agans-Fantuzzi J, Boykow G, Hsieh Y, Bryant M, Palamanda J, Chan TM, Hesk D, Chintala M. Chelliah MV, et al. Among authors: chintala m. J Med Chem. 2007 Oct 18;50(21):5147-60. doi: 10.1021/jm070704k. Epub 2007 Sep 14. J Med Chem. 2007. PMID: 17854166
67 results