Synthesis and HIV-1 integrase inhibitory activities of 4-hydroxy-5-azacoumarin 3-carboxamides
- Authors
- Lee, Seung Uk; Park, Jang Hyun; Kwon, Tae Hoon; Yoo, Yeong Jae; Lee, Jae Yeol; Shin, Cha-Gyun; Yoo, Kyung Ho; Lee, Yong Sup
- Issue Date
- Sep-2007
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- HIV-1 integrase inhibitor; strand transfer; 4-hydroxy-5-azacoumarin
- Citation
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.28, no.9, pp 1510 - 1514
- Pages
- 5
- Journal Title
- BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- Volume
- 28
- Number
- 9
- Start Page
- 1510
- End Page
- 1514
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/23984
- DOI
- 10.5012/bkcs.2007.28.9.1510
- ISSN
- 0253-2964
1229-5949
- Abstract
- 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.
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Collections - College of Biotechnology & Natural Resource > Department of Systems Biotechnology > 1. Journal Articles
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