Abstract
A series of substituted 1-(5-bromopyridin-2-yl)-3-[2-(isoindolo[2,1-a]quinoxalin-6ylamino)ethyl]thiourea and 1-(5-bromopyridin-2-yl)-3-[2-(6-iminoisoindolo[2,1-a]quinoxalin5(6H)-yl)ethyl]thiourea derivatives were prepared in good yields (63-85%) by reaction between the corresponding amino compounds with 5-bromo-2-isothiocyanatopyridine. All thiourea derivatives, tested for inhibition of HIV-1 RT, showed no significant antiviral activity.
Highlights
Human immunodeficiency virus (HIV) is a retrovirus responsible for transmission and development of the acquired immune deficiency syndrome (AIDS). It is characterized by the presence of a viral reverse transcriptase (RT) that is able to synthesize DNA from the viral RNA genoma
Due to its important role in the viral life cycle, this enzyme is considered an excellent target in the chemotherapy against AIDS
In the current treatment strategy, called highly active antiretroviral therapy (HAART), HIV-1 RT inhibitors are used in combination with HIV-1 protease inhibitors.[1,2,3]
Summary
Synthesis of substituted isoindolo[2,1-a]quinoxalin-6-yl–amino and 6-imino-5-yl thiourea derivatives.
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