lithospermic-acid and bevirimat

lithospermic-acid has been researched along with bevirimat* in 1 studies

Other Studies

1 other study(ies) available for lithospermic-acid and bevirimat

Article	Year
Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1. Journal of medicinal chemistry, 2016, 10-13, Volume: 59, Issue:19 Two "privileged fragments", caffeic acid and piperazine, were integrated into bevirimat producing new derivatives with improved activity against HIV-1/NL4-3 and NL4-3/V370A carrying the most prevalent bevirimat-resistant polymorphism. The activity of one of these, 18c, was increased by 3-fold against NL4-3 and 51-fold against NL4-3/V370A. Moreover, 18c is a maturation inhibitor with improved metabolic stability. Our study suggested that integration of privileged motifs into promising natural product skeletons is an effective strategy for discovering potent derivatives. Topics: Animals; Anti-HIV Agents; Caffeic Acids; Cell Line; Chlorocebus aethiops; COS Cells; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Piperazine; Piperazines; Succinates; Triterpenes; Virus Replication	2016

Article

Year

Incorporation of Privileged Structures into Bevirimat Can Improve Activity against Wild-Type and Bevirimat-Resistant HIV-1.

Journal of medicinal chemistry, 2016, 10-13, Volume: 59, Issue:19

Two "privileged fragments", caffeic acid and piperazine, were integrated into bevirimat producing new derivatives with improved activity against HIV-1/NL4-3 and NL4-3/V370A carrying the most prevalent bevirimat-resistant polymorphism. The activity of one of these, 18c, was increased by 3-fold against NL4-3 and 51-fold against NL4-3/V370A. Moreover, 18c is a maturation inhibitor with improved metabolic stability. Our study suggested that integration of privileged motifs into promising natural product skeletons is an effective strategy for discovering potent derivatives.

Topics: Animals; Anti-HIV Agents; Caffeic Acids; Cell Line; Chlorocebus aethiops; COS Cells; Drug Resistance, Viral; HIV Infections; HIV-1; Humans; Piperazine; Piperazines; Succinates; Triterpenes; Virus Replication

2016