6-Benzylamino 4-oxo-1, 4-dihydro-1, 8-naphthyridines and 4-oxo-1, 4-dihydroquinolines as HIV integrase inhibitors

…, HW Kim, J Blazel, S Ouk, B Groschel, V Borges…

文献索引：Nagasawa, Johnny Y.; Song, Jenny; Chen, Huanming; Kim, Hong-Woo; Blazel, Julie; Ouk, Samedy; Groschel, Bettina; Borges, Virginia; Ong, Voon; Yeh, Li-Tain; Girardet, Jean-Luc; Vernier, Jean-Michel; Raney, Anneke K.; Pinkerton, Anthony B. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 2 p. 760 - 763

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被引用次数: 16

摘要

... Compds, X, Y, Z, EC 50 a (nM) (0/40% HS), Microsomal stability b (% remaining). 2, CH, C(OCH 3 ), CH, 0.7/36, 38. 12, CH, C(OCH 3 ), N, 11/136, 100. 13, CH, N, CH, 54/425, 100. 14, CH, CH, N, 65/1937, 99. 15, N, CH, CH, >2500, ND. 16, CH, N, C(OCH 3 ), 291/1772, ND. a Values are means of two or more experiments, coefficient of variation (CV) is <25%. HS = human serum. b Human liver microsomes, 30 min incubation; ND = not determined. ...