Inhibitors of proteases and amide hydrolases that employ an alpha-ketoheterocycle as a key enabling functionality.
Maryanoff BE, Costanzo MJ.
Bioorg Med Chem · review; journal article · DOI 10.1016/j.bmc.2007.11.015 PUBLIKATIONSREGISTRET
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Publikationer i urvalet
12 träffarIn-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.
Costanzo MJ, Almond HR, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Corcoran TW, Giardino EC, Kauffman JA, Lewis JM, de Garavilla L, Haertlein BJ, Maryanoff BE.
J Med Chem · journal article · DOI 10.1021/jm0303857Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.
Maryanoff BE.
J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm030493tRetro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.
Iwanowicz EJ, Kimball SD, Lin J, Lau W, Han WC, Wang TC, Roberts DG, Schumacher WA, Ogletree ML, Seiler SM.
Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(02)00651-0Thrombin active site inhibitors: chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues.
Das J, Kimball SD, Reid JA, Wang TC, Lau WF, Roberts DG, Seiler SM, Schumacher WA, Ogletree ML.
Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(01)00664-3Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664.
Das J, Kimball SD, Hall SE, Han WC, Iwanowicz E, Lin J, Moquin RV, Reid JA, Sack JS, Malley MF, Chang CY, Chong S, Wang-Iverson DB, Roberts DG, Seiler SM, Schumacher WA, Ogletree ML.
Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(01)00667-9The design of potent, selective, non-covalent, peptide thrombin inhibitors utilizing imidazole as a S1 binding element.
Wiley MR, Weir LC, Briggs SL, Chirgadze NY, Clawson D, Gifford-Moore DS, Schacht AL, Smith GF, Vasudevan V, Zornes LL, Klimkowski VJ.
Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(99)00459-xDibasic 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.
Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(99)00074-81,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors.
Harmat NJ, Di Bugno C, Criscuoli M, Giorgi R, Lippi A, Martinelli A, Monti S, Subissi A.
Bioorg Med Chem Lett · journal article · DOI 10.1016/s0960-894x(98)00200-5Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.
Costanzo MJ, Maryanoff BE, Hecker LR, Schott MR, Yabut SC, Zhang HC, Andrade-Gordon P, Kauffman JA, Lewis JM, Krishnan R, Tulinsky A.
J Med Chem · research support, u.s. gov't, p.h.s.; journal article · DOI 10.1021/jm9603274Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.
Shuman RT, Rothenberger RB, Campbell CS, Smith GF, Gifford-Moore DS, Paschal JW, Gesellchen PD.
J Med Chem · journal article · DOI 10.1021/jm00022a009Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.
Iwanowicz EJ, Lau WF, Lin J, Roberts DG, Seiler SM.
J Med Chem · journal article · DOI 10.1021/jm00040a001