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Dibasic benzo[b]thiophene derivatives as a novel class of active site-directed thrombin inhibitors. 1. Determination of the serine protease selectivity, structure-activity relationships, and binding orientation.
Sall DJ, Bastian JA, Briggs SL, Buben JA, Chirgadze NY, Clawson DK, Denney ML, Giera DD, Gifford-Moore DS, Harper RW, Hauser KL, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Palkowitz AD, Smith GF, Takeuchi K, Thrasher KJ, Tinsley JM, Utterback BG, Yan SC, Zhang M. Sall DJ, et al. Among authors: chirgadze ny. J Med Chem. 1997 Oct 24;40(22):3489-93. doi: 10.1021/jm9704107. J Med Chem. 1997. PMID: 9357512 No abstract available.
D-phenylglycinol-derived non-covalent factor Xa inhibitors: effect of non-peptidic S4 linkage elements on affinity and anticoagulant activity.
Klimkowski VJ, Watson BM, Wiley MR, Liebeschuetz J, Franciskovich JB, Marimuthu J, Bastian JA, Sall DJ, Smallwood JK, Chirgadze NY, Smith GF, Foster RS, Craft T, Sipes P, Chastain M, Sheehan SM. Klimkowski VJ, et al. Among authors: chirgadze ny. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5801-5. doi: 10.1016/j.bmcl.2007.08.051. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17881231
The crystal structure of human alpha-thrombin complexed with LY178550, a nonpeptidyl, active site-directed inhibitor.
Chirgadze NY, Sall DJ, Klimkowski VJ, Clawson DK, Briggs SL, Hermann R, Smith GF, Gifford-Moore DS, Wery JP. Chirgadze NY, et al. Protein Sci. 1997 Jul;6(7):1412-7. doi: 10.1002/pro.5560060705. Protein Sci. 1997. PMID: 9232642 Free PMC article.
The inhibitor binds to the active site in an L-shaped manner, mimicking the bound conformation of the tripeptide arginal series of thrombin inhibitors (Chirgadze NY et al., 1992, American Crystallographic Association Meeting 20: 116 [Abstr. ...
The inhibitor binds to the active site in an L-shaped manner, mimicking the bound conformation of the tripeptide arginal series of thrombin …
Dibasic benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 2. Sidechain optimization and demonstration of in vivo efficacy.
Zhang M, Bailey DL, Bastian JA, Briggs SL, Chirgadze NY, Clawson DK, Denney ML, Gifford-Moore DS, Harper RW, Johnson LM, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Richett ME, Sall DJ, Smith AJ, Smith GF, Snyder DW, Takeuchi K, Utterback BG, Yan SC. Zhang M, et al. Among authors: chirgadze ny. Bioorg Med Chem Lett. 1999 Mar 8;9(5):775-80. doi: 10.1016/s0960-894x(99)00074-8. Bioorg Med Chem Lett. 1999. PMID: 10201846
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Potency, efficacy, and pharmacokinetic properties of modified C-3 side chain derivatives.
Sall DJ, Bailey DL, Bastian JA, Buben JA, Chirgadze NY, Clemens-Smith AC, Denney ML, Fisher MJ, Giera DD, Gifford-Moore DS, Harper RW, Johnson LM, Klimkowski VJ, Kohn TJ, Lin HS, McCowan JR, Palkowitz AD, Richett ME, Smith GF, Snyder DW, Takeuchi K, Toth JE, Zhang M. Sall DJ, et al. Among authors: chirgadze ny. J Med Chem. 2000 Feb 24;43(4):649-63. doi: 10.1021/jm9903388. J Med Chem. 2000. PMID: 10691691
Structure-based design of potent, amidine-derived inhibitors of factor Xa: evaluation of selectivity, anticoagulant activity, and antithrombotic activity.
Wiley MR, Weir LC, Briggs S, Bryan NA, Buben J, Campbell C, Chirgadze NY, Conrad RC, Craft TJ, Ficorilli JV, Franciskovich JB, Froelich LL, Gifford-Moore DS, Goodson T Jr, Herron DK, Klimkowski VJ, Kurz KD, Kyle JA, Masters JJ, Ratz AM, Milot G, Shuman RT, Smith T, Smith GF, Tebbe AL, Tinsley JM. Wiley MR, et al. Among authors: chirgadze ny. J Med Chem. 2000 Mar 9;43(5):883-99. doi: 10.1021/jm9903287. J Med Chem. 2000. PMID: 10715155
43 results