Synthesis of novel benzimidazole functionalized chiral thioureas and evaluation of their antibacterial and anticancer activities |
| |
| Affiliation: | 1. Fluoroorganics Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500 007, India;2. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Hyderabad 500 007, India;1. Department of Chemistry, Georgia State University, Atlanta, GA, 30303, United States;2. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt;3. Department of Chemistry, Faculty of Science, Mansoura University, Mansoura 35516, Egypt;4. Swiss Tropical and Public Health Institute, 4002 Basel, Switzerland;5. University of Basel, 4003 Basel, Switzerland;1. College of Natural Sciences, Can Tho University, Viet Nam;2. Korea Bioactive Natural Material Bank, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Sillim-dong, Gwanak-gu, Seoul 151-742, Republic of Korea;3. Department of Chemistry, Umeå University, SE90187 Umeå, Sweden;4. Umeå Centre for Microbial Research (UCMR), SE90187 Umeå, Sweden;5. College of Basic Science, Tra Vinh University, Viet Nam;1. Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Seville, E-41071 Seville, Spain;2. Clinical Unit of Infectious Diseases, Microbiology, and Preventive Medicine, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain;3. Institute of Biomedicine of Seville, University Hospital Virgen del Rocío, CSIC, University of Seville, Seville, Spain;4. Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy;5. Department of Medicine, University of Seville, Seville, Spain;1. Chair and Department of Biochemistry, Medical University, 02-097 Warszawa, Poland;2. Department of Pharmaceutical Microbiology, Medical University, 02-007 Warszawa, Poland;3. Department of Microbiology, National Tuberculosis and Lung Diseases Research Institute, 01-138 Warszawa, Poland;4. Department of Biomedical Science, University of Cagliari, 09042 Monserrato, CA, Italy;5. Department of Pharmacogenomics, Faculty of Pharmacy, Medical University, 02-097 Warszawa, Poland;1. Department of Chemistry, Faculty of Exact Sciences and Informatics ZIANE Achour University, Djelfa, Algeria;2. Department of Chemistry, Faculty of Exact Sciences Echahid Hamma Lakhdar University of El-Oued, Algeria;3. Laboratory of Organic Chemistry and Natural Substance Faculty of Exact Sciences and Informatics, ZIANE Achour University, Djelfa, Algeria;4. Centre de Recherche Scientifique et Technique en Analyses Physico-Chimiques CRAPC, BP384, Bou-Ismail, 42004, Tipaza, Algeria;5. QOPNA and LAQV-REQUIMTE, Department of Chemistry University of Aveiro, 3810-193, Aveiro, Portugal;6. Institute of Biomedicine (iBiMED), Department of Medical Sciences University of Aveiro, 3810-193, Aveiro, Portugal;7. CICECO-Aveiro Institute of Material University of Aveiro, 3810-193, Aveiro, Portugal |
| |
| Abstract: | A small library of benzimidazole functionalized chiral thioureas was prepared starting from natural amino acids (S)-alanine, (S)-phenylalanine, (S)-valine and (S)-leucine and also their (R)-isomers and studied their antimicrobial activity against a various Gram-positive and Gram-negative bacterial strains. In this study, compounds 5g and 5j were found to exhibit good antibacterial activity against both Gram-positive and Gram-negative bacterial strains such as Staphylococcus aureus, Bacillus subtilis, Micrococcus luteus, Klebsiella planticola, Escherichia coli and Pseudomonas aeruginosa. In the cytotoxicity study, thioureas derived from non-natural amino acids 5a–l showed good activity against human cancer cell lines A549, MCF7, DU145, HeLa, and no cytotoxicity was observed with their antipodes 6a–l. |
| |
| Keywords: | Amino acids Chiral thioureas Antibacterial activity Anticancer activity |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
