Tetrazoloquinoline-1,2,3-Triazole Derivatives as Antimicrobial Agents: Synthesis, Biological Evaluation and Molecular Docking Study

被引：4

作者：

Shaikh, Mubarak H. ^{[1
,2
]}

Subhedar, Dnyaneshwar D. ^{[1
]}

Akolkar, Satish V. ^{[1
]}

Nagargoje, Amol A. ^{[1
,3
]}

Khedkar, Vijay M. ^{[4
]}

Sarkar, Dhiman ^{[5
]}

Shingate, Bapurao B. ^{[1
]}

机构：

[1] Dr Babasaheb Ambedkar Marathwada Univ, Dept Chem, Aurangabad 431004, Maharashtra, India

[2] Radhabai Kale Mahila Mahavidyalaya, Dept Chem, Ahmednagar, India

[3] Khopoli Municipal Council Coll, Dept Chem, Khopoli, India

[4] Vishwakarma Univ, Sch Pharm, Dept Pharmaceut Chem, Pune, Maharashtra, India

[5] CSIR Natl Chem Lab, Combi Chem Resource Ctr, Pune, Maharashtra, India

来源：

POLYCYCLIC AROMATIC COMPOUNDS | 2022年 / 42卷 / 04期

关键词：

1,2,3-Triazole; antimicrobial; antioxidant; docking study; ADME prediction; CLICK CHEMISTRY; ANTIMALARIAL ACTIVITY; MYCOBACTERIUM-TUBERCULOSIS; ANTIBACTERIAL ACTIVITY; QUINOLINE DERIVATIVES; FACILE SYNTHESIS; INHIBITORS; DESIGN; 1,2,3-TRIAZOLES;

D O I：

10.1080/10406638.2020.1821229

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In search of new active molecules, a small focused library of tetrazoloquinoline-based 1,2,3-triazoles has been efficiently preparedviaclick chemistry approach. Several derivatives were found to be exhibiting promising antimicrobial and antioxidant activity characterized by their lower minimum inhibitory concentration values. All the synthesized compounds exhibited excellent antibacterial activity against Gram negative bacteriaE. coliandF. devoransand antifungal activity againstC. albicansandA. niger. Further, these compounds were tested for their antitubercular activity against dormantMTB H37Raand dormantM. bovis BCGusing XRMA assay protocol and showed no significant activity. Also, the synthesized compounds were found to have potential antioxidant activity with IC(50)range = 12.48-50.20 mu g/mL. Furthermore, to rationalize the observed biological activity data, the molecular docking study also been carried out against the active site of fungalC. albicansenzyme P450 cytochrome lanosterol 14 alpha-demethylase, which revealed a significant correlation between the binding score and biological activity for these compounds. The results of thein vitroandin silicostudy suggest that the triazole-incorporated tetrazoloquinolines may possess the ideal structural requirements for further development of novel therapeutic agents.

引用

页码：1920 / 1941

页数：22

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