Design,synthesis, antibacterial evaluation and molecular docking studies of some new quinoxaline derivatives targeting dihyropteroate synthase enzyme |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy & Drug Manufacturing, Pharos University in Alexandria, 21311, Egypt;3. Genetic Engineering and Biotechnology Research Institute (GEBRI), The City for Scientific Research and Technology Application, Borg El-Arab, Alexandria, Egypt;4. Department of Microbiology and Immunology, Faculty of Pharmacy & Drug Manufacturing, Pharos University in Alexandria, 21311, Egypt;1. Department of Medicinal Chemistry, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India;2. Department of Pharmacology and Toxicology, B. V. Patel Pharmaceutical Education and Research Development (PERD) Centre, S. G. Highway, Thaltej, Ahmedabad 380054, Gujarat, India;3. Institute of Pharmacy, NIRMA University, S. G. Highway, Chandlodia, Gota, Ahmedabad 82481, Gujarat, India;1. Pharmaceutical Medicinal Chemistry and Drug Design Department, Faculty of Pharmacy (Boys), Al-Azhar University, Nasr City 11884, Cairo, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Heliopolis University for Sustainable Development, Cairo, Egypt;1. Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia;2. Department of Microbiology, East West Group of Institution, No. 63, Anjananagar, Vishwaneedam Post, Bangaluru 560091, Karnataka, India;3. Department of Biosciences, Sri Sathya Sai Institute of Higher Learning, Prasanthi Nilayam, A.P. 515 134, India;1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, King Abdul-Aziz University, Jeddah, Saudi Arabia;2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Nasr City, Egypt;3. Pharmacognosy and Pharmaceutical Chemistry Department, College of Pharmacy, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia;4. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Delta University for Science and Technology, Mansoura, Egypt;5. Chemistry Department, Faculty of Science, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia;6. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Nasr City, Egypt;7. Pharmaceutical Chemistry Department, Faculty of Pharmacy, The Islamic University in Najaf, Al-Najaf Al-Ashraf 54001, Iraq;1. Department of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical Education and Research, Shirpur (Dhule), 425405, Maharashtra, India;2. Department of Biotechnology, Bioinformatics and Pharmacy, Jaypee University of Information Technology, Waknaghat, Solan, 173234, Himachal Pradesh, India;3. Department of Pharmaceutical Chemistry, Shree Dhanvantary Pharmacy College, Kim, Surat, 394110, Gujarat, India;4. School of Public Health, Postgraduate Institute of Medical Education & Research (PGIMER), Chandigarh, 160012, India |
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| Abstract: | Development of new antimicrobial agents is a good solution to overcome drug-resistance problems. From this perspective, new quinoxaline derivatives bearing various bioactive heterocyclic moieties (thiadiazoles, oxadiazoles, pyrazoles and thiazoles) were designed and synthesized. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against nine bacterial human pathogenic strains using the disc diffusion assay. In general, most of the synthesized compounds exhibited good antibacterial activities. The thiazolyl 11c displayed significant antibacterial activities against P. aeruginosa (MIC, 12.5 µg/mL vs levofloxacin 12.5 µg/mL). Molecular docking studies indicated that the synthesized compounds could occupy both p-amino benzoic acid (PABA) and pterin binding pockets of the dihydropteroate synthase (DHPS), suggesting that the target compounds could act by the inhibition of bacterial DHPS enzyme. The results provide important information for the future design of more potent antibacterial agents. |
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| Keywords: | Synthesis Quinoxalines Dihyropteroate synthase Antibacterial activity Docking |
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