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具有抗炎和抗菌活性潜力的吡啶和噻唑基酰肼及其研究

Pyridine- and Thiazole-Based Hydrazides with Promising Anti-inflammatory and Antimicrobial Activities along with Their Studies.

作者信息

Kamat Vinuta, Santosh Rangappa, Poojary Boja, Nayak Suresh P, Kumar Banoth Karan, Sankaranarayanan Murugesan, Khanapure Sheela, Barretto Delicia Avilla, Vootla Shyam K

机构信息

Department of Post-Graduate Studies & Research in Chemistry, Mangalore University, Dakshina Kannada, Mangalagangothri 574199, Karnataka, India.

Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani Campus, Pilani, Rajasthan 333031, India.

出版信息

ACS Omega. 2020 Sep 25;5(39):25228-25239. doi: 10.1021/acsomega.0c03386. eCollection 2020 Oct 6.

DOI:10.1021/acsomega.0c03386
PMID:33043201
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7542836/
Abstract

A new class of compounds formed by the linkage of -C(O)-NH- with pyridine and thiazole moieties was designed, synthesized, and characterized by various spectral approaches. The newly characterized compounds were evaluated for their antimicrobial as well as anti-inflammatory properties. The anti-inflammatory activity of these compounds was evaluated by denaturation of the bovine serum albumin method and showed inhibition in the range of IC values-46.29-100.60 μg/mL. Among all the tested compounds, compound has the highest IC value and compound has the least IC value. On the other hand, antimicrobial results revealed that compound showed the lowest MIC values and compound has the highest MIC values. Furthermore, molecular docking of the active compounds demonstrated a better docking score and interacted well with the target protein. Physicochemical parameters of the titled compounds were found suitable in the reference range only. The molecular docking study revealed their COX-inhibitory action. Compound emerged as a significant bioactive molecule among the synthesized analogues.

摘要

设计、合成了一类由 -C(O)-NH- 与吡啶和噻唑部分相连形成的新型化合物，并通过各种光谱方法对其进行了表征。对新表征的化合物进行了抗菌和抗炎性能评估。这些化合物的抗炎活性通过牛血清白蛋白变性法进行评估，IC值在46.29 - 100.60 μg/mL范围内显示出抑制作用。在所有测试化合物中，化合物 具有最高的IC值，化合物 具有最低的IC值。另一方面，抗菌结果表明化合物 显示出最低的MIC值，化合物 具有最高的MIC值。此外，活性化合物的分子对接显示出更好的对接分数，并与靶蛋白良好相互作用。标题化合物的物理化学参数仅在参考范围内合适。分子对接研究揭示了它们的COX抑制作用。化合物 在合成类似物中成为一种重要的生物活性分子。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/296d/7542836/69116a9da988/ao0c03386_0011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/296d/7542836/c7873e76b65b/ao0c03386_0006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/296d/7542836/f9e37a98bbc4/ao0c03386_0007.jpg
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