Interphenylene 7-oxabicyclo [2.2. 1] heptane oxazoles. Highly potent, selective, and long-acting thromboxane A2 receptor antagonists

RN Misra, BR Brown, PM Sher, MM Patel…

Index: Misra, Raj N.; Brown, Baerbel R.; Sher, Philip M.; Patel, Manorama M.; Hall, Steven E.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 10 p. 1401 - 1417

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Citation Number: 26

Abstract

1s-(la, 2a, 3a, 4a)]-2-[[3-14-[(n-pentylamino) carbonyll-2-oxazolyll-7-oxabicyclo [2.2. 11 hept- 2-yl] methyl] benzenepropanoic acid) was found to be a potent, selective, and orally-active TxA2 antagonist with a long duration of action and has been selected as a candidate for clinical development. In human platelet-rich plasma, 42 inhibited arachidonic acid (800 pM) and U-46,-619 (10 pM) induced aggregation with150 values of 7 and 21 nM, respectively. ...