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.
Botta, M., Artico, M., Massa, S., Gambacorta, A., Marongiu, M.e., Pani, A., et al. (1992). SYNTHESIS, ANTIMICROBIAL AND ANTIVIRAL ACTIVITIES OF ISOTRIMETHOPRIM AND SOME RELATED DERIVATIVES. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 27(3), 251-257 [10.1016/0223-5234(92)90009-P].
SYNTHESIS, ANTIMICROBIAL AND ANTIVIRAL ACTIVITIES OF ISOTRIMETHOPRIM AND SOME RELATED DERIVATIVES
GAMBACORTA, Augusto;
1992-01-01
Abstract
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
