Bis-basic-substituted polycyclic aromatic compounds. A new class of antiviral agents. 8. Bis-basic derivatives of carbazole, dibenzofuran, and dibenzothiophene
作者:William L. Albrecht、Robert W. Fleming、Stephen W. Horgan、Gerald D. Mayer
DOI:10.1021/jm00213a011
日期:1977.3
A series of bisalkamine esters, bis-basic ethers, and bis-basic ketones of carbazole, N-ethylcarbazole, dibenzofuran, and dibenzothiophene was synthesized and evaluated for antiviral activity. The series also included two bis-basic alkanes of N-ethylcarbazole and one bis-basic carboxamide of dibenzofuran. Structure-activity relationships indicated that within the carbazole and N-ethylcarbazole series
合成了咔唑,N-乙基咔唑,二苯并呋喃和二苯并噻吩的一系列双烷基胺酯,双碱性醚和双碱性酮,并评估了其抗病毒活性。该系列还包括两种N-乙基咔唑的双碱性烷烃和一种二苯并呋喃的双碱性羧酰胺。结构-活性关系表明,在咔唑和N-乙基咔唑系列中,双烷胺酯提供了最活跃的衍生物,而二苯并呋喃和二苯并噻吩的双碱性酮衍生物提供了各自系列中更有效的化合物。比较了[6,5,6]杂环核与[6,5,6]芳香核(芴和芴9-一)(包括tilorone)对脑心肌炎(EMC)病毒的抗病毒活性。