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Indazoles as indole bioisosteres: synthesis and evaluation of the tropanyl ester and amide of indazole-3-carboxylate as antagonists at the serotonin 5HT3 receptor

P Fludzinski, DA Evrard, WE Bloomquist…

文献索引:Fludzinski; Evrard; Bloomquist; Lacefield; Pfeifer; Jones; Deeter; Cohen Journal of Medicinal Chemistry, 1987 , vol. 30, # 9 p. 1535 - 1537

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被引用次数: 74

摘要

Bioisosterism has always played an important role in medicinal chemistry. l The replacement of one moiety with a bioequivalent is an important strategy to circumvent problems of metabolism, toxicology, absorption, or other obstacles to in vivo drug activity. Thus, bioisosterism can play an important role in the development of new and novel pharmacological agents from existing ones. Since 1979, tremendous progress has been ...