1,3,4,5-四氢-2H-1,4-苯并二氮杂卓-2-酮（TBO）衍生物的合成及抗HIV活性。截短的4,5,6,7-四氢-5-甲基咪唑并[4,5,1-jk][1,4]苯并二氮杂卓-2(1H)-酮（TIBO）类似物。

Synthesis and anti-HIV activity of 1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-one (TBO) derivatives. Truncated 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2( 1H)-on es (TIBO) analogues.

作者信息

Breslin H J, Kukla M J, Kromis T, Cullis H, De Knaep F, Pauwels R, Andries K, De Clercq E, Janssen M A, Janssen P A

机构信息

Janssen Research Foundation, Spring House, PA 19477, USA.

出版信息

Bioorg Med Chem. 1999 Nov;7(11):2427-36. doi: 10.1016/s0968-0896(99)00198-4.

DOI:10.1016/s0968-0896(99)00198-4

PMID:10632052

Abstract

4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1 H)-ones (TIBO), 1, have been shown to significantly inhibit HIV-1 replication, as reported in detail in our prior publications. Since our earlier reports, we have modified the TIBO structures 1 by removing the 5-membered ring of 1, generating 1,3,4,5-tetrahydro-2H-1,4-benzodiazepin-2-ones (TBO), 4, a bicyclic series of compounds. Although compounds 4 possess modest activity when compared to TIBO analogues 1, they clearly demonstrated significant anti-HIV-1 activity.

摘要

4,5,6,7-四氢-5-甲基咪唑并[4,5,1-jk][1,4]苯并二氮杂䓬-2(1H)-酮（TIBO），即化合物1，已被证明能显著抑制HIV-1复制，详情见我们之前的出版物。自我们早期的报告以来，我们通过去除化合物1的五元环对TIBO结构进行了修饰，生成了1,3,4,5-四氢-2H-1,4-苯并二氮杂䓬-2-酮（TBO），即化合物4，这是一类双环化合物。尽管与TIBO类似物1相比，化合物4的活性适中，但它们显然具有显著的抗HIV-1活性。