SYNTHESIS OF PYRRYL ARYL SULFONES TARGETED AT THE HIV-1 REVERSE-TRANSCRIPTASE

被引：36

作者：

ARTICO, M

SILVESTRI, R

STEFANCICH, G

MASSA, S

SCINTU, F

PAGNOZZI, E

MASU, D

PINNA, E

TINTI, E

LACOLLA, P

机构：

[1] UNIV TRIESTE,DIPARTIMENTO SCI FARMACEUT,I-34127 TRIESTE,ITALY

[2] UNIV CAGLIARI,DIPARTIMENTO BIOL SPERIMENTALE,I-09124 CAGLIARI,ITALY

来源：

ARCHIV DER PHARMAZIE | 1995年 / 328卷 / 03期

关键词：

D O I：

10.1002/ardp.19953280304

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Various aryl 1-pyrryl sulfones were synthesized and tested as inhibitors of HIV-1, 2-Nitrophenyl-2-ethoxycarbonyl-1-pyrryl sulfone, the most active among test derivatives, was selected as lead compound of the aryl pyrryl sulfone series. The in vitro anti-HIV-1 activity and cytotoxicity of 41 compounds is reported. Some structure-activity relationships are discussed also in comparison with the known NPPS (2-nitorphenyl phenyl sulfone).

引用

页码：223 / 229

页数：7

共 19 条

[1]

ADAMS J, 1993, SEARCH ANTIVIRAL DRU

[2] SYNTHESIS OF 1,2,4-BENZOTHIADIAZINES VIA READILY GENERATED IMINIUM IONS [J].