Bioorganic & Medicinal Chemistry 2010-07-01

Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.

Yong-Hong Liang, Qiu-Qin He, Zhao-Sen Zeng, Zhi-Qian Liu, Xiao-Qing Feng, Fen-Er Chen, Jan Balzarini, Christophe Pannecouque, Erik De Clercq

文献索引：Bioorg. Med. Chem. 18(13) , 4601-5, (2010)

全文：HTML全文

摘要

Nine newly 6-cyano-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. The antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC₅₀ of 0.16 and 0.15 μM, and were more activity than that of efavirenz.Copyright © 2010 Elsevier Ltd. All rights reserved.

相关化合物

  • 6-氰基-2-萘酚

相关文献：

Synthesis and structure-activity study of protease inhibitors. V. Chemical modification of 6-amidino-2-naphthyl 4-guanidinobenzoate.

1993-01-01

[Chem. Pharm. Bull. 41(1) , 117-25, (1993)]

Exploration of the active site of β4GalT7: modifications of the aglycon of aromatic xylosides.

2015-03-21

[Org. Biomol. Chem. 13(11) , 3351-62, (2015)]

Minor groove binding compounds that jump a gc base pair and bind to adjacent AT base pair sites.

2009-02-24

[Biochemistry 48(7) , 1573-83, (2009)]

Preparation and pharmacological evaluation of novel glycoprotein (Gp) IIb/IIIa antagonists. 1. The selection of naphthalene derivatives.

1999-12-01

[Chem. Pharm. Bull. 47(12) , 1685-93, (1999)]

Doping of Polyaniline with 6-Cyano-2-naphthol. Das D, et al.

[J. Phys. Chem. B 118(45) , 12993-13001, (2014)]

更多文献...