Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
复制标题
DOI：
10.1016/j.ejmech.2008.09.013
复制
发表时间：
2009-03
影响因子：
6.7
通讯作者：
Cushman, Mark
中科院分区：
文献类型：
--
作者：
Deng, Bo-Liang;Zhao, Yujie;Hartman, Tracy L.;Watson, Karen;Buckheit, Robert W., Jr.;Pannecouque, Christophe;De Clercq, Erik;Cushman, Mark
As a continuation of efforts to replace the metabolically labile methyl esters of the lead alkenyldiarylmethanes (ADAMs) with stable bioisosteres, compounds bearing benzo[d]isoxazole and oxazolidine-2-one rings were designed and evaluated as a new series of potent HIV-1 non-nucleoside reverse transcriptase inhibitors with anti-HIV activity. All of the resulting ADAMs were found to inhibit HIV-1 RT with poly(rC)·oligo(dG) as the template primer. The most promising compound in this series was ADAM 3, with EC50 values of 40 nM (vs HIV-1RF) and 20 nM (vs HIV-1IIIB). Compound 3 also inhibited HIV-1 reverse transcriptase with an IC50 of 0.91 μM. ADAM 4 has an antiviral EC50 of 0.6 μM in CEM-SS cells and a plasma half-life of 51.4 min.
登录
查看更多内容
影响因子：
3.1
作者：
PAUWELS, R;BALZARINI, J;DECLERCQ, E
通讯作者：
DECLERCQ, E
影响因子：
7.3
作者：
Cushman, M;Golebiewski, WM;Buckheit, RW
通讯作者：
Buckheit, RW
影响因子：
7.3
作者：
Herschhorn, Alon;Lerman, Lena;Hizi, Amnon
通讯作者：
Hizi, Amnon
DOI：
10.1016/s1054-3589(08)60675-4
发表时间：
1995-01-01
期刊：
Advances in pharmacology (San Diego, Calif.)
影响因子：
--
作者：
Rice, W G;Bader, J P
通讯作者：
Bader, J P
影响因子：
2
作者：
Silvestri, MA;Miles, D;Cushman, M
通讯作者：
Cushman, M