Synthesis and biological evaluation of some 6-substituted purines

Fernanda Gambogi Braga; Elaine Soares Coimbra; Magnum de Oliveira Matos; Arturene Maria Lino Carmo; Marisa Damato Cancio; Adilson David da Silva

doi:10.1016/j.ejmech.2006.10.014

Synthesis and biological evaluation of some 6-substituted purines

Eur J Med Chem. 2007 Apr;42(4):530-7. doi: 10.1016/j.ejmech.2006.10.014. Epub 2006 Dec 6.

Authors

Fernanda Gambogi Braga¹, Elaine Soares Coimbra, Magnum de Oliveira Matos, Arturene Maria Lino Carmo, Marisa Damato Cancio, Adilson David da Silva

Affiliation

¹ Departamento de Parasitologia, Microbiologia e Imunologia, Instituto de Ciências Biológicas, Universidade Federal de Juiz de Fora, Campus Universitario, Bairro Martelos, Juiz de Fora, Minas Gerais 36036-900, Brazil.

PMID: 17156894
DOI: 10.1016/j.ejmech.2006.10.014

Abstract

We report herein the synthesis and the in vitro antileishmanial evaluation of a series of 6-substituted purines. The most active compounds against Leishmania amazonensis promastigotes were 6-(3'-chloropropylthio)purine 2 [11,12] [corrected] 6-(3'-(thioethylamine)propylthio)purine 5, 6-(alpha-aceticacidthio)purine 7 and 6-(6'-deoxy-1'-O-methyl-beta-D-ribofuranose)purine 14 with an IC(50)=50, 50, 39 and 29 microM, respectively.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Ethylamines / chemical synthesis*
Ethylamines / chemistry
Ethylamines / pharmacology*
Inhibitory Concentration 50
Leishmania / drug effects*
Macrophages / drug effects
Mice
Molecular Structure
Parasitic Sensitivity Tests
Purines / chemical synthesis*
Purines / chemistry
Purines / pharmacology*

Substances

6-(3'-(thioethylamine)propylthio)purine
6-(3'-chloropropylthio)purine
6-(6'-deoxy-1'-O-methyl-beta-D-ribofuranose)purine
Ethylamines
Purines