Abstract
The development of new HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating structures of increased potency. On this basis, new derivatives of the angiotensin-converting enzyme ‘Captopril’ bearing benzimidazoles, benzothiazole, purine and pyridine residues were synthesized with the aim of developing new NNRTIs. Alternatively, the thioether analogs bearing carboxymethylthio, 2-amino-2-oxo-ethylthio, 2-(phthalimido-2-yl)-2ethylthio, 1-benzyl-2-ethyl-4-nitro-imidazol-5-yl)-piperazin-1-yl)-2-oxo-ethylthio, and the carboxamide analogs were prepared from condensation of Captopril with various halide derivatives. The new compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. The compound having a 4-chlorobenzimidazole group was the most active in inhibiting HIV-1, with EC50 = 0.24 µg/ml, with therapeutic indexes (SI) of 21, is a leading candidate for further development.
Highlights
The global spread and fatal prognosis of human immunodeficiency virus (HIV) infection emphasize the urgent need for effective antiretroviral therapies
The introduction of highly active antiretroviral therapy (HAART) based on a combination of HIV-1 reverse transcriptase (RT) and protease inhibitors to treat AIDS has had a dramatic impact on the morbidity and mortality of individuals infected by the HIV.[1,2,3,4,5]
Some benzimidazoles have been reported as new HIV-1 reverse transcriptase inhibitors, and/or potent DNA gyrase inhibitors.[9]
Summary
The global spread and fatal prognosis of human immunodeficiency virus (HIV) infection emphasize the urgent need for effective antiretroviral therapies. The spectrum demonstrated a higher field signal at δ 177.1 that was assigned to C=O, since the resonance at δ 152.5 was attributed to C-6 and C-7a of the benzimidazole ring.
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