New Quinoline Linked Chalcone and Pyrazoline Conjugates: Molecular Properties Prediction, Antimicrobial and Antitubercular Activities

被引:24
作者
Rao, N. Sankara [1 ]
Shaik, Anver Basha [1 ]
Routhu, Sunitha Rani [1 ]
Hussaini, S. M. Ali [1 ]
Sunkari, Satish [1 ]
Rao, A. V. Subba [1 ]
Reddy, A. Malla [1 ]
Alarifi, Abdullah [2 ]
Kamal, Ahmed [1 ,2 ]
机构
[1] CSIR Indian Inst Chem Technolog, Med Chem & Pharmacol, Hyderabad 500007, Andhra Pradesh, India
[2] King Saud Univ, Coll Sci, Chem Dept, Riyadh 11451, Saudi Arabia
关键词
antimicrobial; antitubercular; molecular docking; quinoline; chalcone; pyrazoline; MYCOBACTERIUM-TUBERCULOSIS; IN-VITRO; BIOLOGICAL EVALUATION; ORAL BIOAVAILABILITY; MIC DETERMINATION; DRUG DISCOVERY; EFFLUX PUMP; RESISTANCE; ANTICANCER; FLUOROQUINOLONES;
D O I
10.1002/slct.201602022
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Two novel series comprising of forty two compounds have been synthesized by conjugating quinoline scaffold with chalcone as well as pyrazoline motifs. All the synthesized conjugates were tested for their antibacterial, antifungal and anti-tubercular activities. Several of these novel compounds exhibited good to appreciable antibacterial activity against the tested bacterial strains. Compounds 4j and 7b were found to be the promising candidates exhibiting MIC 4 mu g/mL against B. subtilisMTCC 121 and M. luteus MTCC 2470. Moreover, several conjugates significantly inhibited growth of certain fungal organisms. Furthermore, some of the conjugates displayed moderate anti-tubercular activity against both H37RV as well as Rif(R) strains. The binding modes and effect of the C4 quinoline substitution on the activity have been studied using computational techniques. Methyl group enhances the antimicrobial activity upon replacement by aromatic phenyl group and this is supported by the experimental data.
引用
收藏
页码:2989 / 2996
页数:8
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