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IN SILICO AND EXPERIMENTAL STUDIES FOR THE DEVELOPMENT OF NOVEL OXAZOL-5(4H)-ONES WITH PHARMACOLOGICAL POTENTIAL

ELENA VALENTINA ROȘCA ¹, THEODORA VENERA APOSTOL ¹, MARIANA CARMEN CHIFIRIUC ², GRAȚIELA GRĂDIȘTEANU PÎRCĂLĂBIORU ², CONSTANTIN DRĂGHICI ³, LAURA ILEANA SOCEA ¹, OCTAVIAN TUDOREL OLARU ⁴, GEORGE MIHAI NIȚULESCU ⁵, ELENA MIHAELA PAHONȚU ⁶, MĂDĂLINA HRUBARU ³, ȘTEFANIA FELICIA BĂRBUCEANU ^1*

1.Organic Chemistry Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956, Bucharest, Romania
2.University of Bucharest, Research Institute of the University of Bucharest (ICUB) and Faculty of Biology, Microbiology Department, 1-3 Portocalelor Alley, 060101, Bucharest, Romania
3.“Costin D. Nenițescu” Organic Chemistry Centre of Romanian Academy, 202B Splaiul Independenței Street, 060023, Bucharest, Romania
4.Pharmaceutical Botany and Cell Biology Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956, Bucharest, Romania
5.Pharmaceutical Chemistry Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956, Bucharest, Romania
6.General and Inorganic Chemistry Department, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia Street, 020956, Bucharest, Romania

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New 2-(4-(4-X-phenylsulfonyl)phenyl)-4-(3-bromo/3-bromo-4-methoxy-benzylidene)oxazol-5(4H)-ones have been synthesized by reaction of some 2-(4-(4-X-phenylsulfonyl)benzamido)acetic acids derivatives with 3-bromobenzaldehyde or 3-bromo-4-methoxybenzaldehyde. The structures of the newly obtained heterocycles were elucidated by IR, 1H-NMR, 13C-NMR, mass spectra and elemental analysis. The cytotoxicity of the new oxazolones was evaluated using Artemia salina and Daphnia magna organisms and the in vitro antimicrobial activity was assessed on Gram-positive and Gram-negative bacterial and fungal strains.