1562664-75-8

Upstream product

• 88-74-4 2-nitro-aniline 
• 2905-27-3 3,5-dimethyl-benzenesulfonyl chloride 
• 1562666-42-5 N-(2-nitrophenyl)-3,5-dimethylbenzenesulfonamide 
• 1306685-55-1 N-(2-aminophenyl)-3,5-dimethylbenzenesulfonamide 
• 6160-65-2 1,1'-Thiocarbonyldiimidazole 

Downstream Products

• 1562664-85-0 2-({1-[(3,5-dimethylphenyl)sulfonyl]-1H-benzimidazol-2-yl}sulfanyl)-N-2-chlorophenylacetamide 
• 1562664-98-5 2-({1-[(3,5-dimethylphenyl)sulfonyl]-1H-benzimidazol-2-yl}sulfanyl)-N-2-bromophenylacetamide 
• 1562665-16-0 2-({1-[(3,5-dimethylphenyl)sulfonyl]-1H-benzimidazol-2-yl}sulfanyl)-N-2-nitrophenylacetamide 
• 1562665-39-7 C₂₄H₂₂ClN₃O₃S₂ 
• 1562665-54-6 methyl-3-chloro-4-{[({1-[(3,5-dimethylphenyl)sulfonyl]-1H-benzimidazol-2-yl}sulfanyl)acetyl]amino}benzoate 
• 1562665-78-4 2-({1-[(3,5-dimethylphenyl)sulfonyl]-1H-benzimidazol-2-yl}sulfanyl)-N-[2-chloro-4-(methylsulfonyl)phenyl]acetamide 
• 1562665-99-9 C₂₃H₂₁ClN₄O₅S₃ 

Relevant academic research and scientific papers

Discovery of benzimidazole-based Leishmania mexicana cysteine protease CPB2.8ΔCTE inhibitors as potential therapeutics for leishmaniasis

Chemotherapy is currently the only effective approach to treat all forms of leishmaniasis. However, its effectiveness is severely limited due to high toxicity, long treatment length, drug resistance, or inadequate mode of administration. As a consequence,

Structural optimization of N1-aryl-benzimidazoles for the discovery of new non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are recommended components of preferred combination antiretroviral therapies used for the treatment of human immunodeficiency virus (HIV) infection. These regimens are extremely effective in suppressing virus replication. Recently, our research group identified some N1-aryl-2-arylthioacetamido-benzimidazoles as a novel class of NNRTIs. In this research work we report the design, the synthesis and the structure–activity relationship studies of new compounds (20–34) in which some structural modifications have been introduced in order to investigate their effects on reverse transcriptase (RT) inhibition and to better define the features needed to increase the antiviral activity. Most of the new compounds proved to be highly effective in inhibiting both RT enzyme at nanomolar concentrations and HIV-1 replication in MT4 cells with minimal cytotoxicity. Among them, the most promising N1-aryl-2-arylthioacetamido-benzimidazoles and N1-aryl-2-aryloxyacetamido-benzimidazoles were also tested toward a panel of single- and double-mutants strain responsible for resistance to NNRTIs, showing in vitro antiviral activity toward single mutants L100I, K103N, Y181C, Y188L and E138K. The best results were observed for derivatives 29 and 33 active also against the double mutants F227L and V106A. Computational approaches were applied in order to rationalize the potency of the new synthesized inhibitors.

Design and synthesis of N1-aryl-benzimidazoles 2-substituted as novel HIV-1 non-nucleoside reverse transcriptase inhibitors

A series of novel N1-aryl-2-arylthioacetamido-benzimidazoles were synthesized and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Some of them proved to be effective in inhibiting HIV-1 replication at submicromolar and nanomolar concentration acting as HIV-1 non-nucleoside RT inhibitors (NNRTIs), with low cytotoxicity. The preliminary structure-activity relationship (SAR) of these new derivatives was discussed and rationalized by docking studies.