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1Medi 201-Synthesis Of 1,3,4-Thiadiazole And 1,3,4-Oxadiazole Containing Butanoic Acids As Potent And Selective Alpha V Beta 3 Integrin Receptor Antagonists

John A. Wendt,Heather G. Stenmark,Mark L. Boys, Lori Schretzman,Thomas D. Penning,Mark A. Russell,V. Wayne Engleman,Sandra K. Freeman,Melanie L. Hanneke,Marissa Westlin,Tiffany Duffin,Mary Beth Finn,

2006ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY（2006）

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2Synthesis of 2,5-Thiazole Butanoic Acids As Potent and Selective Αvβ3 Integrin Receptor Antagonists with Improved Oral Pharmacokinetic Properties

JA Wendt,HW Wu,HG Stenmark,ML Boys,VL Downs,TD Penning,BB Chen, YP Wang,T Duffin,MB Finn,JL Keene,VW Engleman,

We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin alpha(V)beta(3) and show selectivity relative to the other integrins, such as alpha(IIB)beta(3) and alpha(V)beta(6). These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs. (c) 2005 Elsevier Ltd. All rights reserved.

2005Bioorganic & Medicinal Chemistry Letters（2005）引用：11

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3Convergent, Parallel Synthesis of a Series of Beta-Substituted 1,2,4-Oxadiazole Butanoic Acids As Potent and Selective Alpha(v)beta3 Receptor Antagonists.

Mark L Boys,Lori A Schretzman,Nizal S Chandrakumar,Michael B Tollefson,Scott B Mohler,Victoria L Downs,Thomas D Penning,Mark A Russell,John A Wendt,Barbara B Chen,Heather G Stenmark,Hongwei Wu,

We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin alpha(v)beta3 and, in addition, show selectivity relative to the other beta3 integrin alpha(IIb)beta3. In whole cells, the majority of these analogs also demonstrated modest selectivity against other alpha(v) integrins such as alpha(v)beta1 and alpha(v)beta6.

2005Bioorganic & medicinal chemistry letters（2005）引用：55

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