Romanian Society of Pharmaceutical Sciences
 

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N-(1-ADAMANTYLCARBAMOTHIOYL)BENZAMIDES: SYNTHESIS, BIOLOGICAL EVALUATION AND ADME PREDICTIONS

HOREA GURGU 1#, EMIL ȘTEFĂNESCU 2#, DIANA CAMELIA NUȚĂ 1*, MIRON TEODOR CĂPROIU 4, FLOREA DUMITRAŞCU 4, MARIANA CARMEN CHIFIRIUC 5,6, CORALIA BLEOTU 7, GEORGE MIHAI NIȚULESCU 1, FLAVIAN ŞTEFAN RĂDULESCU 3, CARMEN LIMBAN 1

1.“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Pharmaceutical Chemistry Department, 6 Traian Vuia Street, 020956, Bucharest, Romania
2 .“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Pharmacology and Clinical Pharmacy Department, 6 Traian Vuia Street, 020956, Bucharest, Romania
3 .“Carol Davila” University of Medicine and Pharmacy, Faculty of Pharmacy, Drug Industry and Pharmaceutical Biotechnologies Department, 6 Traian Vuia Street, 020956, Bucharest, Romania
4 .“Costin D. Nenițescu” The Organic Chemistry Centre of Romanian Academy, 202B Splaiul Independenței, 060023, Bucharest, Romania
5 .University of Bucharest, Faculty of Biology, Department of Microbiology, 1-3 Portocalelor Alley, 060101, Bucharest, Romania
6 .University of Bucharest, Research Institute of the University of Bucharest - ICUB, 91-95 Splaiul Independenței, 050095, Bucharest, Romania
7 .“Prof. Șt. Nicolau” Institute of Virology, 36 Mihai Bravu Road, 021326, Bucharest, Romania

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This paper presents the synthesis of five novel benzamide derivatives containing adamantane moiety. The compounds structure was proven through elemental analysis, FT-IR, 1H-NMR and 13C-NMR spectroscopy. Their therapeutic potential was evaluated by the in vitro testing of the antimicrobial activity. Two different parameters of the antimicrobial activity were determined: minimum inhibitory concentration (MIC) and minimal biofilm eradication concentration (MBEC). Also, an in vitro cytotoxicity study was carried out on Hep-2 cell line. An in silico study of the compounds determined their ADME profile. The study reports the preliminary biological screening of five novel benzamides with adamantane scaffold, that evidenced a good toxicological and ADME profile, thus representing favourable candidates for further studies.