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吡唑并[3,4-]吡啶和三唑的分子杂合体:设计、合成与体外抗菌研究。

Molecular Hybrids of Pyazolo[3,4-]pyridine and Triazole: Design, Synthesis and In Vitro Antibacterial Studies.

机构信息

Department of Chemistry, GITAM School of Science, GITAM Deemed to be University Hyderabad, Rudraram 502329, India.

Department of Chemistry, School of Applied and Life Sciences, Uttaranchal University, Arcadia Grant, Chandanwari, Premnagar, Dehradun 248007, India.

出版信息

Molecules. 2022 Nov 7;27(21):7647. doi: 10.3390/molecules27217647.

DOI:10.3390/molecules27217647
PMID:36364469
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9655101/
Abstract

Antimicrobial resistance is on the rise, and there aren't enough new treatments to combat it. This might send the modern world back to the pre-antibiotic age. The molecular hybrids of pyrazolo[3,4-]pyridine and triazole have been designed, synthesized, and analyzed for their drug-like molecule nature and in vitro analyses for their inhibition potentials against and . The compounds and have been identified as the high potential molecules in this series based on in vitro experiments. Compound has zone of inhibition values of 15 ± 0.82 mm and 14 ± 0.7 mm, whilst compound has zone of inhibition values of 18 ± 0.95 mm and 16 ± 0.82 mm against and , respectively. MIC and MIB values for compounds and against and are 0.25 and 0.5, respectively.

摘要

抗菌药物耐药性正在上升,而对抗耐药菌的新疗法却不够用。这可能使现代社会倒退到抗生素前时代。本文设计、合成了吡唑并[3,4-]吡啶和三唑的分子杂合体,并对其类药性分子性质和体外分析进行了分析,以评估其对和的抑制潜力。基于体外实验,化合物和被确定为该系列中具有高潜力的分子。化合物对和的抑菌环直径值分别为 15±0.82mm 和 14±0.7mm,而化合物对和的抑菌环直径值分别为 18±0.95mm 和 16±0.82mm。化合物和对和的 MIC 和 MIB 值分别为 0.25 和 0.5。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/61499a855f4c/molecules-27-07647-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/70be6c93a3a1/molecules-27-07647-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/4b6538f2fcac/molecules-27-07647-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/04b55ae5a543/molecules-27-07647-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/6f2092ed9d74/molecules-27-07647-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/4086a0fa08c8/molecules-27-07647-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/1894484debd8/molecules-27-07647-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/61499a855f4c/molecules-27-07647-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/70be6c93a3a1/molecules-27-07647-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/4b6538f2fcac/molecules-27-07647-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/04b55ae5a543/molecules-27-07647-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/6f2092ed9d74/molecules-27-07647-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/4086a0fa08c8/molecules-27-07647-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/1894484debd8/molecules-27-07647-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3d5b/9655101/61499a855f4c/molecules-27-07647-g006.jpg

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