Synthesis,antimicrobial, cytotoxic and E. coli DNA gyrase inhibitory activities of coumarinyl amino alcohols
Affiliation:
1. Department of Chemistry, MMV, Banaras Hindu University, Varanasi 221005, India;2. Department of Biotechnology, Institute of Engineering and Technology, Lucknow 226021, India;3. Department of Bioinformatics, MMV, Banaras Hindu University, Varanasi 221005, India;1. Division of Molecular Biology, Bioinformatics Center, Department of Zoology, Sri Venkateswara University, Tirupati, 517 502, AP, India;2. Division of Bioorganic Natural Products, Department of Chemistry, Sri Venkateswara University, Tirupati, 517 502, AP, India;3. Structural Biology Laboratory, Department of Bioinformatics, School of Chemical and Biotechnology, SASTRA University, Thanjavur, 613 401, TN, India;4. Department of Microbiology, Sri Venkateswara University, Tirupati, 517 502, AP, India;1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Modern University for Technology and Information MTI, Cairo 11571, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt;3. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Badr University, Badr City, Cairo 11829, Egypt;4. Medicinal Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt;5. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Nahda University, Beni Suef, Egypt;1. Department of Chemistry, MMV, Banaras Hindu University, Varanasi 221005, India;2. Department of Chemistry, Howard University, 525 College Street NW, Washington DC 20059, USA;1. Department of Chemistry, University of Delhi, Delhi-110007, India;2. Department of Chemistry, Deen Dayal Upadhyaya College, University of Delhi, Delhi-110078, India;3. Department of Microbiology, VP Chest Institute, University of Delhi, Delhi-110007, India;1. Department of Chemistry, MMV, Banaras Hindu University, Varanasi 221005, India;2. Division of Parasitology, CSIR-Central Drug Research Institute, BS 10/1, Jankipuram Extension, Sitapur Road, Lucknow 226031, India;3. Department of Chemistry, Howard University, 525 College Street NW, Washington DC 20059, USA;1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City 11884, Egypt;2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Delta University for Science and Technology, Gammasa, Dakahlia, Egypt;3. Medicinal Chemistry Department, Faculty of Pharmacy (Boys), Al-Azhar University, Cairo, 11884, Egypt
Abstract:
Here we report the in vitro antimicrobial activity (minimum inhibitory concentration) of fourteen coumarinyl amino alcohols 2–16 against eight bacterial strains and two fungi. Among these compounds 4, 8, 12, 15 and 16 showed moderate to good microbial inhibition with MIC values varied from 6.25 to 25 μg/mL. The most promising compounds were also evaluated for their in vitro cytotoxic and E. coli DNA gyrase inhibitory activities along with the two 7-oxy-4-methyl coumarinyl amino alcohol derivatives 17 and 18, which were found to be the most potent in in vitro antimicrobial screening in our previous study. All the active compounds, including 17 and 18, were also docked into the E. coli DNA gyrase ATP binding site (PDB ID: 1KZN) to investigate their binding interactions. Of these compound 17 has shown maximum binding energy value of −6.13 kcal/mol.
