Design and synthesis of novel dihydroquinoline-3-carboxylic acids as HIV-1 integrase inhibitors

…, TW Sanchez, L Taheri, R Dayam, N Neamati

Index: Sechi, Mario; Rizzi, Giuseppe; Bacchi, Alessia; Carcelli, Mauro; Rogolino, Dominga; Pala, Nicolino; Sanchez, Tino W.; Taheri, Laleh; Dayam, Raveendra; Neamati, Nouri Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 7 p. 2925 - 2935

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Citation Number: 47

Abstract

Previously, we discovered linomide analogues as novel HIV-1 integrase (IN) inhibitors. Here, to make possible structure–activity relationships, we report on the design and synthesis of a series of substituted dihydroquinoline-3-carboxylic acids. The crystal structure of the representative compound 2c has also been solved. Among the eight new analogues, 2e showed a potency in inhibiting IN strand transfer catalytic activity similar to the ...