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Substituted thiophene-anthranilamides as potent inhibitors of human factor Xa

Publikováno v: Bioorganic & Medicinal Chemistry. 15:2127-2146

A series of thiophene-containing non-amidine factor Xa inhibitors is described. Simple methyl-substituted thiophene analogs were relatively weak inhibitors. However, introduction of hydrophilic substituents at C-4 or C-5 of the thiophene afforded inh

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79b4b05420f1f0b4641803f66b53494f
https://doi.org/10.1016/j.bmc.2006.12.019

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Synthesis and biological evaluation of menthol-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)

Autor: Kenneth J. Shaw, Bauer Shawn M, Amy Liang, Brad O. Buckman, Wheeseong Lee, Brian D. Griedel, Ghannam Ameen F, Qingyu Wu, Zuchun Zhao, Khim Seock-Kyu, Karna Lyn Sacchi, Bin Ye

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:3361-3365

Compound 2 was identified by high throughput screening as a novel PAI-1 inhibitor. Systematic optimization of the A, B, and C segments of 2 resulted in the identification of a more potent compound 39 with good oral bioavailability. The synthesis and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::701deb338599f8ed8ca158f60220935d
https://doi.org/10.1016/s0960-894x(03)00686-3

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Identification and Characterization of a Potent, Selective, and Orally Active Antagonist of the CC Chemokine Receptor-1

Publikováno v: Journal of Biological Chemistry. 275:19000-19008

The CC chemokine receptor-1 (CCR1) is a prime therapeutic target for treating autoimmune diseases. Through high capacity screening followed by chemical optimization, we identified a novel non-peptide CCR1 antagonist, R-N-[5-chloro-2-[2-[4-[(4-fluorop

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::96836a4797891eb0ce582451db65d51a
https://doi.org/10.1074/jbc.m001222200

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Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors

Autor: Marc Whitlow, Morrissey Michael M, Amy Liang, Brian D. Griedel, Jerry L. Dallas, Arnaiz Damian O, Joseph Post, Zuchun Zhao, Kenneth J. Shaw, Lan Trinh, Sakata Steven T

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:963-966

Inhibitors based on the benzimidazole scaffold showed subnanomolar potency against Factor Xa with 500–1000-fold selectivity against thrombin and 50–100-fold selectivity against trypsin. The 2-substituent on the benzimidazole ring had a strong imp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eeb26d2396da2df3e284c79ad0b0fba
https://doi.org/10.1016/s0960-894x(00)00139-6

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Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors

Autor: Lan Trinh, Sunil K. Koovakkat, Amy Liang, Arnaiz Damian O, Zuchun Zhao, Marc Whitlow, Kenneth J. Shaw

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 10:957-961

A series of indole and carbazole based inhibitors of factor Xa (FXa) has been investigated. The most potent compound inhibits FXa with a Ki of 0.2 nM and has 900- and 750-fold selectivity over thrombin and trypsin, respectively.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c2e0f2a9ad346c1e040a3ab9f700c4f
https://doi.org/10.1016/s0960-894x(00)00138-4

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Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin

Autor: Sunil K. Koovakkat, William J. Guilford, Wei Xu, Brad O. Buckman, Marian Seto, Brain Griedel, David R. Light, Morrissey Michael M, David D. Davey, Kenneth J. Shaw, Damain O. Arnaiz, Amy Liang, Gary Phillips, Zuchun Zhao, Raju Mohan, Marc Whitlow

Publikováno v: Acta Crystallographica Section D Biological Crystallography. 55:1395-1404

Factor Xa is a serine protease which activates thrombin (factor IIa) and plays a key regulatory role in the blood-coagulation cascade. Factor Xa is, therefore, an important target for the design of anti-thrombotics. Both factor Xa and thrombin share

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::014adafa43785dad6d1450599562bf33
https://doi.org/10.1107/s0907444999007350

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Dehydroamino acid derivatives from D-arabinose and L-serine: synthesis of models for the azinomycin antitumor antibiotics

Autor: Zuchun Zhao, John E. Tellew, Edmund J. Moran, Robert W. Armstrong

Publikováno v: The Journal of Organic Chemistry. 58:7848-7859

Synthesis of aldehydes 17 from D-arabinose and 31 from L-serine provided key precursors for the generation of highly functionalized dehydroamino acid derivatives upon condensation with glycyl phosphonates. Subsequent bromination and intramolecular ad

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e34c203bffe1b85a1072433f812e243a
https://doi.org/10.1021/jo00079a033

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