Literature DB >> 25311566

Synthesis and evaluation of pyrazolines bearing benzothiazole as anti-inflammatory agents.

Chetna Kharbanda1, Mohammad Sarwar Alam2, Hinna Hamid1, Kalim Javed1, Sameena Bano1, Abhijeet Dhulap3, Yakub Ali1, Syed Nazreen1, Saqlain Haider1.   

Abstract

The present study aims at the synthesis of pyrazolines bearing benzothiazole and their evaluation as anti-inflammatory agents. The synthesized compounds were evaluated for their anti-inflammatory potential using carrageenan induced paw edema model. Two compounds 5a and 5d alleviated inflammation more than the standard drug celecoxib. Eight compounds 5 b, 5 c, 5 e, 5 g, 5 h, 6 b, 6 e and 6 f showed anti-inflammatory activity comparable to celecoxib. To understand the mode of action, COX-2 enzyme assay and TNF-α assay were carried out. All the active compounds were assessed for their cytotoxicity. The ulcerogenic risk evaluation was performed on the active compounds that were not found to be cytotoxic. Out of ten active compounds, two compounds (5 d and 6 f) were finally found to be the most potent anti-inflammatory agents attributing to the suppression of the COX-2 enzyme activity and TNF-α production without being either cytotoxic or ulcerogenic.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anti-inflammatory; COX-2; Molecular docking; Pyrazolines; TNF-α

Mesh:

Substances:

Year:  2014        PMID: 25311566     DOI: 10.1016/j.bmc.2014.09.028

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  5 in total

1.  Novel quinolinone-pyrazoline hybrids: synthesis and evaluation of antioxidant and lipoxygenase inhibitory activity.

Authors:  Ioanna Kostopoulou; Antonia Diassakou; Eleni Kavetsou; Eftichia Kritsi; Panagiotis Zoumpoulakis; Eleni Pontiki; Dimitra Hadjipavlou-Litina; Anastasia Detsi
Journal:  Mol Divers       Date:  2020-02-17       Impact factor: 2.943

2.  Synthesis, In Vitro α-Glucosidase Inhibitory Activity and Molecular Docking Studies of Novel Benzothiazole-Triazole Derivatives.

Authors:  Zipeng Gong; Yaping Peng; Jie Qiu; Anbai Cao; Guangcheng Wang; Zhiyun Peng
Journal:  Molecules       Date:  2017-09-15       Impact factor: 4.411

Review 3.  A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors.

Authors:  Wenjing Liu; Min He; Yongjun Li; Zhiyun Peng; Guangcheng Wang
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.051

4.  Synthesis and Antidepressant Activity Profile of Some Novel Benzothiazole Derivatives.

Authors:  Ümide Demir Özkay; Ceren Kaya; Ulviye Acar Çevik; Özgür Devrim Can
Journal:  Molecules       Date:  2017-09-07       Impact factor: 4.411

5.  Antimicrobial, Antioxidant, and Anticancer Activities of Some Novel Isoxazole Ring Containing Chalcone and Dihydropyrazole Derivatives.

Authors:  Afzal Shaik; Richie R Bhandare; Kishor Palleapati; Srinath Nissankararao; Venkata Kancharlapalli; Shahanaaz Shaik
Journal:  Molecules       Date:  2020-02-26       Impact factor: 4.411

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.