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Curr Microbiol ; 62(5): 1349-54, 2011 May.
Artigo em Inglês | MEDLINE | ID: mdl-21225264

RESUMO

Herpes simplex virus is an important human pathogen responsible for a range of diseases from mild uncomplicated mucocutaneous infections to life-threatening ones. Currently, the emergence of Herpes simplex virus resistant strains increased the need for more effective and less cytotoxic drugs for Herpes treatment. In this work, we synthesized a series of oxoquinoline derivatives and experimentally evaluated the antiviral activity against acyclovir resistant HSV-1 strain as well as their cytotoxity profile. The most active compound (3b), named here as Fluoroxaq-3b, showed a promising profile with a better cytotoxicity profile than acyclovir. The theoretical analysis of the structure-activity relationship of these compounds revealed some stereoelectronic properties such as lower LUMO energy and lipophilicity, besides a higher polar surface area and number of hydrogen bond acceptor groups as important parameters for the antiviral activity. Fluoroxaq-3b showed a good oral theoretical bioavailability, according to Lipinski rule of five, with a promising profile for further in vivo analysis.


Assuntos
Antivirais/química , Antivirais/farmacologia , Herpes Simples/virologia , Herpesvirus Humano 1/efeitos dos fármacos , Quinolonas/química , Quinolonas/farmacologia , Animais , Antivirais/síntese química , Linhagem Celular , Chlorocebus aethiops , Herpes Simples/tratamento farmacológico , Humanos , Quinolonas/síntese química , Relação Estrutura-Atividade , Células Vero
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