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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 28, Number 9
BKCSDE 28(9)
September 20, 2007 

Synthesis and HIV-1 Integrase Inhibitory Activities of 4-Hydroxy-5-azacoumarin 3-Carboxamides
Seung Uk Lee, Jang Hyun Park, Tae Hoon Kwon, Yeong Jae Yoo, Jae Yeol Lee, Cha-Gyun Shin, Kyung Ho Yoo, Yong Sup Lee*
HIV-1 integrase inhibitor, Strand transfer, 4-Hydroxy-5-azacoumarin
Recently, it has been reported that the inhibition of the strand transfer function of HIV-1 integrase is necessary to obtain significant antiviral activity. Accordingly, several compounds typified by aryl 1,3-diketo acids that can inhibit strand transfer reaction of HIV-1 IN have been identified. In this work, we synthesized new 4- hydroxy-5-azacoumarin-3-carbox(thio)amides (1a-h) and evaluated for the inhibition of HIV-1 IN strand transfer reaction with a brief SAR. Among synthesized, compound 1e was the most potent HIV-1 IN inhibitor with equipotent activity to that of L-708,906. Therefore, the 4-hydroxy-5-azacoumarin ring can be considered as a new scaffold in designing more potent of HIV-1 IN inhibitors for treatment of AIDS.
1510 - 1514
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