Literature DB >> 34817768

Design, synthesis and molecular docking studies of some 1-(5-(2-fluoro-5-(trifluoromethoxy)phenyl)-1,2,4-oxadiazol-3-yl)piperazine derivatives as potential anti-inflammatory agents.

B Kulkarni1, K Manjunatha2,3, Muthipeedika Nibin Joy4, Ayyiliath Meleveetil Sajith5, C N Prashantha6, Ranjith Pakkath5, Mohammed B Alshammari7.   

Abstract

We herein report the facile synthesis of a series of 3,5-substituted-1,2,4-oxadiazole derivatives in good to excellent yields. The anti-inflammatory potential of the newly synthesized compounds was evaluated by anti-denaturation assay using diclofenac sodium as the reference standard. Some of the compounds exhibited profound activity profile when compared to the standard drug. The molecular docking and SAR studies were carried out at the later stage for gaining more insights about the promising activity profile of the synthesized molecules.
© 2021. The Author(s), under exclusive licence to Springer Nature Switzerland AG.

Entities:  

Keywords:  Anti-inflammatory activity; Molecular docking; Oxadiazole; SAR

Mesh:

Substances:

Year:  2021        PMID: 34817768     DOI: 10.1007/s11030-021-10340-1

Source DB:  PubMed          Journal:  Mol Divers        ISSN: 1381-1991            Impact factor:   3.364


  22 in total

Review 1.  Structural and functional basis of cyclooxygenase inhibition.

Authors:  Anna L Blobaum; Lawrence J Marnett
Journal:  J Med Chem       Date:  2007-03-07       Impact factor: 7.446

2.  In vivo anti-inflammatory activity and docking study of newly synthesized benzimidazole derivatives bearing oxadiazole and morpholine rings.

Authors:  Ankita Rathore; Raja Sudhakar; Mohamed Jawed Ahsan; Abuzer Ali; Naidu Subbarao; Surender Singh Jadav; Sadiq Umar; M Shahar Yar
Journal:  Bioorg Chem       Date:  2016-11-29       Impact factor: 5.275

3.  3-Formylchromones: potential antiinflammatory agents.

Authors:  Khalid M Khan; Nida Ambreen; Uzma Rasool Mughal; Saima Jalil; Shahnaz Perveen; M Iqbal Choudhary
Journal:  Eur J Med Chem       Date:  2010-06-08       Impact factor: 6.514

4.  Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.

Authors:  Islam Eid; Mohamed M Elsebaei; Haroon Mohammad; Mohamed Hagras; Christine E Peters; Youssef A Hegazy; Bruce Cooper; Joe Pogliano; Kit Pogliano; Hamada S Abulkhair; Mohamed N Seleem; Abdelrahman S Mayhoub
Journal:  Eur J Med Chem       Date:  2017-08-18       Impact factor: 6.514

5.  Synthesis and antibacterial evaluation of a novel library of 2-(thiazol-5-yl)-1,3,4-oxadiazole derivatives against methicillin-resistant Staphylococcus aureus (MRSA).

Authors:  Mohamed H Hannoun; Mohamed Hagras; Ahmed Kotb; Abdul-Aziz M M El-Attar; Hamada S Abulkhair
Journal:  Bioorg Chem       Date:  2019-10-18       Impact factor: 5.275

6.  Synthesis and antiviral evaluation of novel 1,3,4-oxadiazole/thiadiazole-chalcone conjugates.

Authors:  Xiuhai Gan; Deyu Hu; Zhuo Chen; Yanjiao Wang; Baoan Song
Journal:  Bioorg Med Chem Lett       Date:  2017-08-18       Impact factor: 2.823

7.  Discovery of novel dengue virus NS5 methyltransferase non-nucleoside inhibitors by fragment-based drug design.

Authors:  Fatiha Benmansour; Iuni Trist; Bruno Coutard; Etienne Decroly; Gilles Querat; Andrea Brancale; Karine Barral
Journal:  Eur J Med Chem       Date:  2016-10-05       Impact factor: 6.514

8.  Assembly of New Heterocycles through an Effective Use of Bisaldehydes by Using a Sequential GBB/Ugi Reaction.

Authors:  Tanpreet Kaur; Ram Nayan Gautam; Anuj Sharma
Journal:  Chem Asian J       Date:  2016-09-13

9.  From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity.

Authors:  Mohamed H El-Shershaby; Adel Ghiaty; Ashraf H Bayoumi; Ahmed A Al-Karmalawy; Ebtehal M Husseiny; Mona S El-Zoghbi; Hamada S Abulkhair
Journal:  Bioorg Med Chem       Date:  2021-06-05       Impact factor: 3.641

10.  Identification of a novel triterpene saponin from Panax ginseng seeds, pseudoginsenoside RT8, and its antiinflammatory activity.

Authors:  Taewoong Rho; Hyun Woo Jeong; Yong Deog Hong; Keejung Yoon; Jae Youl Cho; Kee Dong Yoon
Journal:  J Ginseng Res       Date:  2018-11-10       Impact factor: 6.060

View more
  1 in total

1.  Exploration of NMI-MsCl mediated amide bond formation for the synthesis of novel 3,5-substituted-1,2,4-oxadiazole derivatives: synthesis, evaluation of anti-inflammatory activity and molecular docking studies.

Authors:  B Kulkarni; K Manjunatha; Muthipeedika Nibin Joy; Ayyiliath Meleveetil Sajith; Sougata Santra; Grigory V Zyryanov; C N Prashantha; Mohammed B Alshammari; K Sunil
Journal:  Mol Divers       Date:  2022-10-11       Impact factor: 3.364

  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.