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Part VI. Nonpeptide angiotensin II receptor antagonists: N-[(benzyloxy) benzyl] imidazoles and related compounds as potent antihypertensives

DJ Carini, JV Duncia, AL Johnson…

文献索引:Carini, David J.; Duncia, John V.; Johnson, Alexander L.; Chiu, Andrew T.; Price, William A.; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1330 - 1336

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被引用次数: 82

摘要

14 3e displace [3H]-AII (2 nM) fromits specific binding sites in rat adrenal cortical microsomes; the data are reported in Table I. Direct comparison of the ICso values for 2a, 3a, 4, 5, 6a, 7, and 8 demonstrates that activity in this series is optimal when the linking group, X, is 0-1 atoms in length. The biphenyl 2a, benzophenone 3a, diaryl ether 4, and diaryl sulfide 5 (IC5,-,'s= 0.16-0.49 pM) are essentially equipotent with the N-( ...