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

被引:2
|
作者
Gurgu, Horea [1 ]
Stefanescu, Emil [2 ]
Nuta, Diana Camelia [1 ]
Caproiu, Miron Teodor [4 ]
Dumitrascu, Florea [4 ]
Chifiriuc, Mariana Carmen [5 ,6 ]
Bleotu, Coralia [7 ]
Nitulescu, George Mihai [1 ]
Radulescu, Flavian Stefan [3 ]
Limban, Carmen [1 ]
机构
[1] Carol Davila Univ Med & Pharm, Fac Pharm, Pharmaceut Chem Dept, 6 Traian Vuia St, Bucharest 020956, Romania
[2] Carol Davila Univ Med & Pharm, Fac Pharm, Pharmacol & Clin Pharm Dept, 6 Traian Vuia St, Bucharest 020956, Romania
[3] Carol Davila Univ Med & Pharm, Fac Pharm, Drug Ind & Pharmaceut Biotechnol Dept, 6 Traian Vuia St, Bucharest 020956, Romania
[4] Romanian Acad, Costin D Nenitescu Organ Chem Ctr, 202B Splaiul Independentei, Bucharest 060023, Romania
[5] Univ Bucharest, Fac Biol, Dept Microbiol, 1-3 Portocalelor Alley, Bucharest 060101, Romania
[6] Univ Bucharest, Res Inst, Univ Bucharest ICUB, 91-95 Splaiul Independentei, Bucharest 050095, Romania
[7] Prof St Nicolau Inst Virol, 36 Mihai Bravu Rd, Bucharest 021326, Romania
关键词
benzamides; adamantane; microbiological assay; cytotoxicity; ANTI-BIOFILM ACTIVITY; THIOUREA DERIVATIVES; ANTIMICROBIAL ACTIVITY; BENZAMIDES; INHIBITORS;
D O I
10.31925/FARMACIA.2018.6.6
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
This paper presents the synthesis of five novel benzamide derivatives containing adamantane moiety. The compounds structure was proven through elemental analysis, FT-IR, H-1-NMR and C-13-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.
引用
收藏
页码:963 / 971
页数:9
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