Journal of Medicinal Chemistry p. 2029 - 2037 (2013)
Update date:2022-07-30
Topics:
Dang, Zhao
Ho, Phong
Zhu, Lei
Qian, Keduo
Lee, Kuo-Hsiung
Huang, Li
Chen, Chin-Ho
Bevirimat (1, BVM) is an anti-HIV agent that blocks HIV-1 replication by interfering with HIV-1 Gag-SP1 processing at a late stage of viral maturation. However, clinical trials of 1 have revealed a high baseline drug resistance that is attributed to naturally occurring polymorphisms in HIV-1 Gag. To overcome the drug resistance, 28 new derivatives of 1 were synthesized and tested against compound 1-resistant (BVM-R) HIV-1 variants. Among them, compound 6 exhibited much improved activity against several HIV-1 strains carrying BVM-R polymorphisms. Compound 6 was at least 20-fold more potent than 1 against the replication of NL4-3/V370A, which carries the most prevalent clinical BVM-R polymorphism in HIV-1 Gag-SP1. Thus, compound 6 merits further development as a potential anti-AIDS clinical trial candidate.
View MoreJiaxing Trustworthy Import And Export Co.,Ltd
Contact:+86-573-82030555
Address:Room 1202, Unit B, Charming plaza,No.1558 East Zhongshan Road , Jiaxing City, Zhejiang Province, China.
ZiBO KuoDing Trade company Ltd
website:http://www.sdzbkd.com
Contact:86-13361591822
Address:GongQingTuan road
Chengdu Pukang Biotechnology Co., Ltd
website:http://www.pu-kang.com
Contact:86-028-63976226
Address:No. 868 Xiwang Road,Xinjin county,Chengdu city, China
Contact:+86-579-85206992
Address:No 451 chouzhou north road ,room 1106 int'l business center , yiwu ,china
Contact:+86-310-7092106
Address:Quzhou Modern & New Industrial Park, Handan, Hebei 057250, China
Doi:10.1016/j.tet.2012.07.073
(2012)Doi:10.1021/ja306407x
(2012)Doi:10.1007/s11745-012-3707-9
(2012)Doi:10.1016/S0957-4166(00)82313-7
(1992)Doi:10.1039/b501875g
(2005)Doi:10.1016/j.bmcl.2020.127615
(2020)