Synthesis and biological evaluation of newer 1,3,4-oxadiazoles incorporated with benzothiazepine and benzodiazepine moieties

被引:13
|
作者
Navin, Patel [1 ]
Sarvil, Patel [1 ]
Amit, Purohit [1 ]
Divyesh, Patel [2 ]
Dhansukh, Rajani [3 ]
Moo-Puc, Rosa [4 ]
Rivera, Gildardo [5 ]
机构
[1] Veer Narmad South Gujarat Univ, Dept Chem, Organ Res Lab, Udhana Magdalla Rd, Surat 395007, Gujarat, India
[2] Maharaja Sayajirao Univ Baroda, Fac Sci, Dept Chem, Vadodara 390002, Gujarat, India
[3] Microcare Lab & TB Diag & Res Ctr, Surat, India
[4] Inst Mexicano Seguro Social, Unidad Med Alta Especialidad, Merida 97150, Mexico
[5] Inst Politecn Nacl, Ctr Biotecnol Genom, Reynosa 88710, Mexico
来源
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES | 2017年 / 72卷 / 3-4期
关键词
antimicrobial activity; antituberculosis activity; benzodiazepines; benzothiazepines; 1,3,4-Oxadiazole; MOLECULAR DOCKING; DERIVATIVES; AGENTS; THIOPHENE; DESIGN;
D O I
10.1515/znc-2016-0129
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of thiazepines and diazepines having 1,3,4-oxadiazole moiety were synthesized, and they were analyzed for their in vitro antimicrobial activity against several bacteria (Staphylococcus aureus, Staphylococcus pyogenes, Escherichia coli, and Pseudomonas aeruginosa) and fungi (Candida albicans, Aspergillus niger, and Aspergillus Clavatus) and protozoa (Entamoeba histolytica, Giardia lamblia, Trypanosoma cruzi and Leishmania mexicana). Few of the selected compounds were tested for their antitubercular activity. However, it was noticed that the potency of final analogs against each strain placed reliance on the type of substituent present on aryl ring of oxadiazole as well as presence of thiophene, pyridine, and furan at benzothiazepines and benzodiazepines. The biological screening identified that some of the compounds were found to possess good antimicrobial and antitubercular (62.5-100 mu g/mL of MIC) activity.
引用
收藏
页码:133 / 146
页数:14
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