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
5University of Bucharest, Faculty of Biology, Department of Microbiology, 1-3 Portocalelor Alley, 060101, Bucharest,
Romania
6University 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
*corresponding author: diananuta@yahoo.com
#Authors with equal contribution.
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Abstract:
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.






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