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.