SYNTHESIS, ANTIMICROBIAL AND ANTIVIRAL ACTIVITIES OF ISOTRIMETHOPRIM AND SOME RELATED DERIVATIVES

被引：67

作者：

BOTTA, M

ARTICO, M

MASSA, S

GAMBACORTA, A

MARONGIU, ME

PANI, A

LACOLLA, P

机构：

[1] UNIV ROME LA SAPIENZA,DIPARTIMENTO STUDI FARMACEUT,I-00185 ROME,ITALY

[2] UNIV ROME LA SAPIENZA,DIPARTIMENTO CHIM,I-00185 ROME,ITALY

[3] UNIV CAGLIARI,DIPARTIMENTO BIOL SPERIMENTALE,SEZ MICROBIOL,I-09124 CAGLIARI,ITALY

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1992年 / 27卷 / 03期

关键词：

TRIMETHOPRIM ANALOGS; ANTIMICROBIAL AGENTS; ANTIVIRAL AGENTS; DIAMINOPYRIMIDINES;

D O I：

10.1016/0223-5234(92)90009-P

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and the antimicrobial activities of 2,4-diamino-6-(3,4.5-trimethoxvbenzyl)pyrimidine (isotrimethoprim) and some related derivatives are reported. The new derivatives have been found scarcely active against bacteria and fungi, with the only exception of 4-chloro-2-methoxypyrimidinyl-3,4,5-trimethoxyphenyldichloromethane, which showed good antibacterial activity against Staphylococcus aureus. Cytotoxicity and antiviral assays, HIV included, have also been determined in comparison with TMP and AZT. Little but selective activity was shown by some derivatives against HIV retrovirus.

引用

页码：251 / 257

页数：7

共 9 条

[1] 6-ALKYL-2-METHOXY-4(3H)-PYRIMIDINONES AND 5,6-DIALKYL-2-METHOXY-4(3H)-PYRIMIDINONES IN THE TRANSFORMATIONS OF PYRIMIDINES - CONVERSION INTO 2-SUBSTITUTED "AMINO-CHLORO-PYRIMIDINE-DERIVATIVES AND 4-CHLORO-PYRIMIDINE-DERIVATIVES [J].