| Literature DB >> 23845222 |
Tsukasa Mizuhara1, Takayuki Kato, Atsushi Hirai, Hideki Kurihara, Yasuhiro Shimada, Masahiko Taniguchi, Hideki Maeta, Hiroaki Togami, Kazuya Shimura, Masao Matsuoka, Shiho Okazaki, Tomoki Takeuchi, Hiroaki Ohno, Shinya Oishi, Nobutaka Fujii.
Abstract
The structure-activity relationship of phenylpyrazole derivative 1 was investigated for the development of novel anti-HIV agents. Initial efforts revealed that the diazenyl group can be replaced by an aminomethylene group. In addition, we synthesized various derivatives by the reductive amination of benzaldehydes with 5-aminopyrazoles and carried out parallel structural optimization on the benzyl group and the pyrazole ring. This optimization led to a six-fold more potent derivative 32j than the lead compound 1, and this derivative has a 3',4'-dichloro-(1,1'-biphenyl)-3-yl group.Entities:
Keywords: Anti-HIV agent; HIV; NNRTI; NRTI; PI; Phenylpyrazole; human immunodeficiency virus; non-nucleoside reverse transcriptase inhibitor; nucleoside reverse transcriptase inhibitor; protease inhibitor
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Year: 2013 PMID： 23845222 DOI： 10.1016/j.bmcl.2013.06.026
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823