Abstract
A series of phthalimido-(substituted-alkyl-2-thioureido)alkyl carboxylic acid derivatives 5–13 and methyl 2-(4-(phthalimido-2-yl)butanamido)alkyl carboxylates 14–23 were synthesized with the aim to develop newly non-nucleoside reverse transcriptase inhibitors (NNRTIs). The new synthesized compounds were assayed against human immunodeficiency virus-1 and human immunodeficiency virus-2 in MT-4 cells. The results showed that 22 and 23 were the only compounds in the series inhibiting human immunodeficiency virus-1 (IIIB strain) replication in cell culture with an EC50 value of >2.07 and >4.23 μM (SI = 7 and 5), respectively. In addition, the new analogs were screened against hepatitis virus C genotype 1b in the Huh-5-2 replicon system. Compounds 9 and 12 were the most active analogs of the series and exhibited activity with EC50 = 26.7 and 22.0 μM (SI > 1.87 and >2.28, respectively). The molecular docking of 22 with some amino acids of human immunodeficiency virus reverse transcriptase has been studied.
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