Synthesis, molecular docking and biological evaluation of some novel tetrazolo[1,5-a]quinoline incorporated pyrazoline and isoxazoline derivatives

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• 作者：Mukesh D. Nikam ; Pravin S. Mahajan ; Manoj G. Damale…
• 关键词：Tetrazole ; Pyrazolines ; Isoxazolines ; Antimicrobial activity ; Antioxidant activity ; Docking study
• 刊名：Medicinal Chemistry Research
• 出版年：2015
• 出版时间：September 2015
• 年：2015
• 卷：24
• 期：9
• 页码：3372-3386
• 全文大小：1,152 KB
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• 作者单位：Mukesh D. Nikam (1) r> Pravin S. Mahajan (1) r> Manoj G. Damale (2) r> Jaiprakash N. Sangshetti (3) r> Sanjay K. Dabhade (1) r> Dadasaheb W. Shinde (1) r> Charansingh H. Gill (1) r>r>1. Department of Chemistry, Dr. Babasaheb Ambedkar Marathwada University, Aurangabad, 431 004, MS, India r> 2. MGM Institute of Biosciences and Technology, Aurangabad, 431003, MS, India r> 3. Dr. Rafiq Zakaria Campus, Y. B. Chavan College of Pharmacy, Aurangabad, 431 001, MS, India r>
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120

文摘

A series of new pyrazolines (4a-strong class="EmphasisTypeBold">4g) and isoxazolines (5a-strong class="EmphasisTypeBold">5g) have been synthesized in good-to-excellent yield from the corresponding chalcones (3a-strong class="EmphasisTypeBold">3g) under ultrasound irradiation. The newly synthesized compounds were characterized and screened for their in vitro antimicrobial activity against different bacterial and fungal strains by standard agar dilution method and in vitro antioxidant activity by using DPPH method. Some of the synthesized compounds displayed significant antimicrobial and antioxidant activity. Docking study of the synthesized compounds has been performed, and results showed good binding mode in the active site of fungal enzyme P450 cytochrome lanosterol 14 α-demethylase. ADMET properties of synthesized compounds showed good drug-like properties.