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Page 1
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Winneroski LL, Schiffler MA, Erickson JA, May PC, Monk SA, Timm DE, Audia JE, Beck JP, Boggs LN, Borders AR, Boyer RD, Brier RA, Hudziak KJ, Klimkowski VJ, Garcia Losada P, Mathes BM, Stout SL, Watson BM, Mergott DJ. Winneroski LL, et al. Among authors: klimkowski vj. Bioorg Med Chem. 2015 Jul 1;23(13):3260-8. doi: 10.1016/j.bmc.2015.04.062. Epub 2015 May 6. Bioorg Med Chem. 2015. PMID: 26001341
Discovery of non-covalent dipeptidyl peptidase IV inhibitors which induce a conformational change in the active site.
Sheehan SM, Mest HJ, Watson BM, Klimkowski VJ, Timm DE, Cauvin A, Parsons SH, Shi Q, Canada EJ, Wiley MR, Ruehter G, Evers B, Petersen S, Blaszczak LC, Pulley SR, Margolis BJ, Wishart GN, Renson B, Hankotius D, Mohr M, Zechel JC, Michael Kalbfleisch J, Dingess-Hammond EA, Boelke A, Weichert AG. Sheehan SM, et al. Among authors: klimkowski vj. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1765-8. doi: 10.1016/j.bmcl.2006.12.074. Epub 2006 Dec 24. Bioorg Med Chem Lett. 2007. PMID: 17239592
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
Durham TB, Klimkowski VJ, Rito CJ, Marimuthu J, Toth JL, Liu C, Durbin JD, Stout SL, Adams L, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR. Durham TB, et al. Among authors: klimkowski vj. J Med Chem. 2014 Dec 26;57(24):10476-85. doi: 10.1021/jm501522n. Epub 2014 Dec 5. J Med Chem. 2014. PMID: 25415648
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. 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
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: klimkowski vj. J Med Chem. 2000 Mar 9;43(5):883-99. doi: 10.1021/jm9903287. J Med Chem. 2000. PMID: 10715155
Investigation of the terminal P4 domain in a series of D-phenylglycinamide-based factor Xa inhibitors.
Franciskovich JB, Masters JJ, Weber WW, Klimkowski VJ, Chouinard M, Sipes PR, Johnson LM, Snyder DW, Chastain MK, Craft TJ, Towner RD, Gifford-Moore DS, Froelich LL, Smallwood JK, Foster RS, Smith GF, Liebeschuetz JW, Murray CW, Young SC. Franciskovich JB, et al. Among authors: klimkowski vj. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6910-3. doi: 10.1016/j.bmcl.2007.09.105. Epub 2007 Oct 24. Bioorg Med Chem Lett. 2007. PMID: 17976987
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: klimkowski vj. 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
1,2-Dibenzamidobenzene inhibitors of human factor Xa.
Herron DK, Goodson T Jr, Wiley MR, Weir LC, Kyle JA, Yee YK, Tebbe AL, Tinsley JM, Mendel D, Masters JJ, Franciskovich JB, Sawyer JS, Beight DW, Ratz AM, Milot G, Hall SE, Klimkowski VJ, Wikel JH, Eastwood BJ, Towner RD, Gifford-Moore DS, Craft TJ, Smith GF. Herron DK, et al. Among authors: klimkowski vj. J Med Chem. 2000 Mar 9;43(5):859-72. doi: 10.1021/jm990326m. J Med Chem. 2000. PMID: 10715153
30 results