Literature DB >> 26844536

Synthesis and in silico investigation of thiazoles bearing pyrazoles derivatives as anti-inflammatory agents.

Rahul D Kamble1, Rohan J Meshram2, Shrikant V Hese1, Rahul A More2, Sonali S Kamble2, Rajesh N Gacche2, Bhaskar S Dawane3.   

Abstract

Searching novel, safe and effective anti-inflammatory agents has remained an evolving research enquiry in the mainstream of inflammatory disorders. In the present investigation series of thiazoles bearing pyrazole as a possible pharmacophore were synthesized and assessed for their anti inflammatory activity using in vitro and in vivo methods. In order to decipher the possible anti-inflammatory mechanism of action of the synthesized compounds, cyclooxygenase I and II (COX-I and COX-II) inhibition assays were also carried out. The results obtained clearly focus the significance of compounds 5d, 5h and 5i as selective COX-II inhibitors. Moreover, compound 5h was also identified as a lead molecule for inhibition of the carrageenin induced rat paw edema in animal model studies. Molecular docking results revealed significant interactions of the test compounds with the active site of COX-II, which perhaps can be explored for design and development of novel COX-II selective anti-inflammatory agents.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Anti-inflammatory; COX; In silico; In vivo; Pyrazole; Thiazole

Mesh:

Substances:

Year:  2016        PMID: 26844536     DOI: 10.1016/j.compbiolchem.2016.01.007

Source DB:  PubMed          Journal:  Comput Biol Chem        ISSN: 1476-9271            Impact factor:   2.877


  9 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Dietary flavonoids inhibit the glycation of lens proteins: implications in the management of diabetic cataract.

Authors:  Rohan J Meshram; Kapil K Patil; Sagar H Barage; Rajesh N Gacche
Journal:  3 Biotech       Date:  2019-01-23       Impact factor: 2.406

Review 3.  Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents.

Authors:  Mohammed F Arshad; Aftab Alam; Abdullah Ayed Alshammari; Mohammed Bader Alhazza; Ibrahim Mohammed Alzimam; Md Anish Alam; Gulam Mustafa; Md Salahuddin Ansari; Abdulelah M Alotaibi; Abdullah A Alotaibi; Suresh Kumar; Syed Mohammed Basheeruddin Asdaq; Mohd Imran; Pran Kishore Deb; Katharigatta N Venugopala; Shahamah Jomah
Journal:  Molecules       Date:  2022-06-21       Impact factor: 4.927

Review 4.  Thiazole Ring-A Biologically Active Scaffold.

Authors:  Anthi Petrou; Maria Fesatidou; Athina Geronikaki
Journal:  Molecules       Date:  2021-05-25       Impact factor: 4.411

5.  Synergism of fused bicyclic 2-aminothiazolyl compounds with polymyxin B against Klebsiella pneumoniae.

Authors:  Rong Wang; Shuang Hou; Xiaojing Dong; Daijie Chen; Lei Shao; Liujia Qian; Zhong Li; Xiaoyong Xu
Journal:  Medchemcomm       Date:  2017-09-14       Impact factor: 3.597

6.  New Series of Thiazole Derivatives: Synthesis, Structural Elucidation, Antimicrobial Activity, Molecular Modeling and MOE Docking.

Authors:  Ismail Althagafi; Nashwa El-Metwaly; Thoraya A Farghaly
Journal:  Molecules       Date:  2019-05-04       Impact factor: 4.411

7.  New Substituted 5-Benzylideno-2-Adamantylthiazol[3,2-b][1,2,4]Triazol-6(5H)ones as Possible Anti-Inflammatory Agents.

Authors:  Christophe Tratrat; Michelyne Haroun; Aliki Paparisva; Charalmpos Kamoutsis; Anthi Petrou; Antonis Gavalas; Phaedra Eleftheriou; Athina Geronikaki; Katharigatta N Venugopala; Hafedh Kochkar; Anroop B Nair
Journal:  Molecules       Date:  2021-01-27       Impact factor: 4.411

8.  Design, synthesis and docking studies of novel thiazole derivatives incorporating pyridine moiety and assessment as antimicrobial agents.

Authors:  Rizk E Khidre; Ibrahim Ali M Radini
Journal:  Sci Rep       Date:  2021-04-12       Impact factor: 4.379

9.  5-Benzyliden-2-(5-methylthiazol-2-ylimino)thiazolidin-4-ones as Antimicrobial Agents. Design, Synthesis, Biological Evaluation and Molecular Docking Studies.

Authors:  Michelyne Haroun; Christophe Tratrat; Aggeliki Kolokotroni; Anthi Petrou; Athina Geronikaki; Marija Ivanov; Marina Kostic; Marina Sokovic; Alejandro Carazo; Přemysl Mladěnka; Nagaraja Sreeharsha; Katharigatta N Venugopala; Anroop B Nair; Heba S Elsewedy
Journal:  Antibiotics (Basel)       Date:  2021-03-17
  9 in total

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