New potent antibacterials against Gram-positive multiresistant pathogens: Effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles |
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| Institution: | 1. Dipartimento di Scienze Chimiche, Università degli Studi di Catania, Viale Andrea Doria 6, I-95125 Catania, Italy;2. Dipartimento di Chimica e Chimica Industriale, Università di Pisa, Via Risorgimento, 35, I-56126 Pisa, Italy;3. Laboratori de Medicina Computacional, Unitat de Bioestadística, Facultat de Medicina, Universitat Autònoma de Barcelona, 08193 Bellaterra, Spain;4. Laboratory for Chemometrics and Cheminformatics, Chemistry Department, University of Perugia, Via Elce di Sotto 10, I-06123 Perugia, Italy;5. Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Sez. Chimica, Università degli Studi di Palermo, Viale delle Scienze Ed. 17—Parco D’Orleans II, I-90128 Palermo, Italy;6. Istituto EuroMediterraneo di Scienza e Tecnologia (IEMEST), Via Emerico Amari 123, I-90139 Palermo, Italy;7. Dipartimento di Scienze della Salute, Università di Milano-Bicocca, Via Cadore 48, I-20900 Monza (MB), Italy;8. Dipartimento di Chirurgia e Medicina Traslazionale, Università di Milano-Bicocca, Via Cadore 48, I-20900 Monza (MB), Italy;1. Department of Studies in Chemistry, Mangalore University, Mangalagangothri, Karnataka 574 199, India;2. SeQuent Scientific Limited, No. 120 A&B, Industrial Area, Baikampady, New Mangalore, Karnataka 575 011, India;3. Department of Bio-Chemistry, Jnanasahyadri, Kuvempu University, Shankaraghatta, Karnataka 577 451, India;4. Department of P.G. Studies and Research in Biotechnology and Bioinformatics, Jnanasahyadri, Kuvempu University, Shankaraghatta, Karnataka 577 451, India;1. School of Chemistry, Madurai Kamaraj University, Madurai 625021, India;2. Centre for Green Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai 625021, India;1. Pharmacy and Applied Science, La Trobe Institute for Molecular Science, La Trobe University, P.O. Box 199 Bendigo, VIC 3552, Australia;2. Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia;3. Australian Centre for Blood Diseases and Department of Clinical Haematology, Monash University, 99 Commercial Road, Melbourne, Victoria 3004, Australia;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kuwait University, P.O. Box 24923, Safat 13110, Kuwait;2. Department of Microbiology, Faculty of Medicine, Kuwait University, P.O. Box 24923, Safat 13110, Kuwait |
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| Abstract: | The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compounds, enantiomers separation and absolute configuration assignment. Experimental determination of the antibacterial activity of the designed (S)-1-((3-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea and (S)-1-((3-(3-fluoro-4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea against multidrug resistant linezolid bacterial strains was higher than that of linezolid. |
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| Keywords: | Drug design Linezolid Antibiotics Multidrug-resistant bacteria Enantiomers |
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