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Concepção, síntese e atividade anti-HIV de análogos da curcumina

Concepção, síntese e atividade anti-HIV de análogos da curcumina

Mohamed Jawed Ahsan / Sachin Kumar Sharma

58,88 €
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Editorial:
KS OmniScriptum Publishing
Año de edición:
2025
Materia
Farmacología
ISBN:
9786209363573
58,88 €
IVA incluido
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Uma série de 11 análogos da curcumina foi submetida a previsão de propriedades moleculares e semelhança com medicamentos pelos softwares Molinspiration e MolSoft, parâmetros de lipofilia e solubilidade usando o programa ALOGPS 2.1. Os compostos seguiram a Regra dos cinco de Lipinski e foram sintetizados para triagem anti-HIV como fármacos/chumbo biodisponíveis por via oral. Além disso, a estrutura dos compostos sintetizados foi confirmada por análises espectrais (IR, NMR e massa) e os compostos (3a-k) foram avaliados quanto à atividade anti-HIV de acordo com o protocolo padrão. A pontuação máxima do modelo de semelhança com fármacos (1.1.0) foi encontrada para 3,5-bis(4-hidroxi-3-metilestiril)-N-(4-clorofenil)-1H-pirazol-1-carboxamida (3b). Verificou-se que o composto 3b tinha atividade anti-HIV com IC50 >3,71 µM e CC50 3,71 µM, no entanto, a atividade foi considerada inferior à do medicamento padrão zidovudina.

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