Anichina K.Mavrova A.2024-07-162024-07-162024-07-162024-07-162022-01-011314-79781314-7471SCOPUS_ID:85123897817https://rlib.uctm.edu/handle/123456789/1354The benzimidazole heterocycle system is a very important structure in the medicinal chemistry due to its use as a building block of a wide range of bioactive compounds. This review highlights the progress of the synthesis and the optimization of benzimidazole compounds as Non-nucleoside Reverse Transcriptase Inhibitors (NNRTIs) against Human Immunodeficiency Virus Type 1 (HIV-1). Since the discovery of NSC 625487 (1-(2’,6’-difluorophenyl)-lH,3H-thiazolo[3,4-a]benzimidazole) as potential anti-retroviral drug candidate, three structural subclasses of benzimidazole HIV-1 NNRTIs in the groups of 1H,3H-thiazolo[3,4-a]benzimidazoles, 2-aryl-1-benzylbenzimidazoles and 1,3-dihydro-benzimidazol-2-ones/2-thione were synthesized and studied up to now. In the current review we report their structural modifications in chronological order and discuss the structure-activity relationship (SAR) to demonstrate the sequential progress in this area. Thus, this study may contribute to the further development and synthesis of novel representatives of the benzimidazole family as anti-HIV-1 agents in the future.enArticle