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Page 1
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ. Powell NA, et al. Among authors: zhang e. Bioorg Med Chem. 2007 Sep 1;15(17):5912-49. doi: 10.1016/j.bmc.2007.05.069. Epub 2007 Jun 2. Bioorg Med Chem. 2007. PMID: 17574423
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Sarver RW, Peevers J, Cody WL, Ciske FL, Dyer J, Emerson SD, Hagadorn JC, Holsworth DD, Jalaie M, Kaufman M, Mastronardi M, McConnell P, Powell NA, Quin J 3rd, Van Huis CA, Zhang E, Mochalkin I. Sarver RW, et al. Among authors: zhang e. Anal Biochem. 2007 Jan 1;360(1):30-40. doi: 10.1016/j.ab.2006.10.017. Epub 2006 Oct 30. Anal Biochem. 2007. PMID: 17113558
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Holsworth DD, Jalaie M, Belliotti T, Cai C, Collard W, Ferreira S, Powell NA, Stier M, Zhang E, McConnell P, Mochalkin I, Ryan MJ, Bryant J, Li T, Kasani A, Subedi R, Maiti SN, Edmunds JJ. Holsworth DD, et al. Among authors: zhang e. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3575-80. doi: 10.1016/j.bmcl.2007.04.052. Epub 2007 Apr 25. Bioorg Med Chem Lett. 2007. PMID: 17482464
The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Rapundalo ST, Saiya-Cork K, Leadley RJ, Narasimhan L, Zhang E, Whitlow M, Adler M, McLean K, Chou YL, McKnight C, Arnaiz DO, Shaw KJ, Light DR, Edmunds JJ. Kohrt JT, et al. Among authors: zhang e. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4752-6. doi: 10.1016/j.bmcl.2005.07.059. Bioorg Med Chem Lett. 2005. PMID: 16125385
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Narasimhan LS, Zhang E, Rapundalo ST, Saiya-Cork K, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: zhang e. Bioorg Med Chem Lett. 2006 Feb 15;16(4):1060-4. doi: 10.1016/j.bmcl.2005.10.076. Epub 2005 Nov 11. Bioorg Med Chem Lett. 2006. PMID: 16289811
Ketopiperazine-based renin inhibitors: optimization of the "C" ring.
Holsworth DD, Cai C, Cheng XM, Cody WL, Downing DM, Erasga N, Lee C, Powell NA, Edmunds JJ, Stier M, Jalaie M, Zhang E, McConnell P, Ryan MJ, Bryant J, Li T, Kasani A, Hall E, Subedi R, Rahim M, Maiti S. Holsworth DD, et al. Among authors: zhang e. Bioorg Med Chem Lett. 2006 May 1;16(9):2500-4. doi: 10.1016/j.bmcl.2006.01.084. Epub 2006 Feb 15. Bioorg Med Chem Lett. 2006. PMID: 16480874
The discovery of glycine and related amino acid-based factor Xa inhibitors.
Kohrt JT, Filipski KJ, Cody WL, Bigge CF, La F, Welch K, Dahring T, Bryant JW, Leonard D, Bolton G, Narasimhan L, Zhang E, Peterson JT, Haarer S, Sahasrabudhe V, Janiczek N, Desiraju S, Hena M, Fiakpui C, Saraswat N, Sharma R, Sun S, Maiti SN, Leadley R, Edmunds JJ. Kohrt JT, et al. Among authors: zhang e. Bioorg Med Chem. 2006 Jul 1;14(13):4379-92. doi: 10.1016/j.bmc.2006.02.040. Epub 2006 Mar 10. Bioorg Med Chem. 2006. PMID: 16529937
The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an orally efficacious factor Xa inhibitor.
Kohrt JT, Bigge CF, Bryant JW, Casimiro-Garcia A, Chi L, Cody WL, Dahring T, Dudley DA, Filipski KJ, Haarer S, Heemstra R, Janiczek N, Narasimhan L, McClanahan T, Peterson JT, Sahasrabudhe V, Schaum R, Van Huis CA, Welch KM, Zhang E, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: zhang e. Chem Biol Drug Des. 2007 Aug;70(2):100-12. doi: 10.1111/j.1747-0285.2007.00539.x. Chem Biol Drug Des. 2007. PMID: 17683371
2,805 results