Structure-activity relationship in PAF-acether. 4. Synthesis and biological activities of carboxylate isosteres

B Wichrowski, S Jouquey, C Broquet…

Index: Wichrowski, Boguslaw; Jouquey, Simone; Broquet, Colette; Heymans, Francoise; Godfroid, Jean-Jacques; et al. Journal of Medicinal Chemistry, 1988 , vol. 31, # 2 p. 410 - 415

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Citation Number: 12

Abstract

The synthesis and biological characterization of some 3-carboxylate isosteres of PAF- acether structurally modified in positions 1 (ether, carbamate), 2 (acetoyl, ethoxy), and 3 (chain length and polar head group) are reported. All derivatives present antagonist activities against PAF-acether-induced effects in vitro (platelet aggregation) and in vivo (bronchoconstriction and thrombocytopenia in guinea pig and, to a lesser extent, ...