کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1394808 1501185 2010 8 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents
چکیده انگلیسی

By modifying the chemical structure of anti-orthopoxvirus compound ST-246, we designed and synthesized a series of tricyclononene carboxamide derivatives and tested their anti-HIV-1 activity and cytotoxicity. We found that benzoimidazol-containing compound 7g was highly effective in inhibiting HIV-1 R5 infection with an IC50 value of 0.41 μM and a selectivity index of 292, but it exhibited no significant inhibitory activity on HIV-1 reverse transcriptase, integrase and protease. CoMFA was used to analyze structure–activity relationships with good predictive power (r2 = 0.921; q2 = 0.582). Moreover, the CoMFA model showed that the length of the molecule, the amide, and the amine moieties all played crucial roles in anti-HIV activity. These results suggest that 7g may serve as a lead for the development of novel anti-HIV-1 therapies.

A series of tricyclononene carboxamide derivatives based on anti-orthopoxvirus compound ST-246 were synthesized and characterized as novel anti-HIV-1 agents.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Medicinal Chemistry - Volume 45, Issue 9, September 2010, Pages 4096–4103
نویسندگان
, , , , , , ,