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

来源：

FARMACIA | 2018年 / 66卷 / 06期

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

页码：963 / 971

页数：9

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