In vivo assessment of newly synthesized achiral copper(ii) and zinc(ii) complexes of a benzimidazole derived scaffold as a potential analgesic, antipyretic and anti-inflammatory

RSC Advances ◽  
2016 ◽  
Vol 6 (23) ◽  
pp. 19475-19481 ◽  
Author(s):  
Mohamed F. AlAjmi ◽  
Afzal Hussain ◽  
Ali Alsalme ◽  
Rais Ahmad Khan

Two new complexes of copper(ii) and zinc(ii) were synthesized and characterized using various spectroscopic techniques. The newly synthesized compounds were screened for analgesic, antipyretic and anti-inflammatory activities.

2021 ◽  
Vol 18 ◽  
Author(s):  
Iqra Hamid ◽  
Humaira Nadeem ◽  
Sameen Fatima Ansari ◽  
Sonia Khiljee ◽  
Inzamam Abbasi ◽  
...  

Background: Non-steroidal anti-inflammatory drugs (NSAIDs) are the commonly used therapeutic interventions of inflammation and pain that competitively inhibit the cyclooxygenase (COX) enzymes. Several side effects like gastrointestinal and renal toxicities are associated with the use of these drugs. The therapeutic anti-inflammatory benefits of NSAIDs are produced by the inhibition of COX-2 enzymes, while undesirable side effects arise from the inhibition of COX-1 enzymes. Objectives: In the present study, a new series of 2-substituted benzoxazole derivatives 2(a-f) and 3(a-e) were synthesized in our lab as potent anti-inflammatory agents with outstanding gastro-protective potential. The new analogs 2(a-f) and 3(a-e) were designed depending upon the literature review to serve as ligands for the development of selective COX-2 inhibitors. Methods: The synthesized analogs were characterized using different spectroscopic techniques (FTIR, 1HNMR, 13CNMR) and elemental analysis. All synthesized compounds were screened for their binding potential in the protein pocket of COX-2 and evaluated for their anti-inflammatory potential in animals using the carrageenan-induced paw edema method. Further 5 compounds were selected to assess the in vivo anti-ulcerogenic activity in an ethanol-induced anti-ulcer rat model. Results: Five compounds (2a, 2b, 3a, 3b and 3c) exhibited potent anti-inflammatory activity and significant binding potential in the COX-2 protein pocket. Similarly, these five compounds demonstrated a significant gastro-protective effect (p<0.01) in comparison to the standard drug, Omeprazole. Conclusion: Depending upon our results, we hypothesize that 2-substituted benzoxazole derivatives have excellent potential to serve as candidates for the development of selective anti-inflammatory agents (COX-2 inhibitors). However, further assessments are required to delineate their underlying mechanisms.


2017 ◽  
Vol 198 ◽  
pp. 608-609
Author(s):  
Jelena Katanić ◽  
Tatjana Boroja ◽  
Vladimir Mihailović ◽  
Stefanie Nikles ◽  
San-Po Pan ◽  
...  

Author(s):  
H Khan ◽  
I Khan ◽  
NK Khalil ◽  
A Shahidullah ◽  
A Aziz ◽  
...  

2016 ◽  
Vol 193 ◽  
pp. 627-636 ◽  
Author(s):  
Jelena Katanić ◽  
Tatjana Boroja ◽  
Vladimir Mihailović ◽  
Stefanie Nikles ◽  
San-Po Pan ◽  
...  

2016 ◽  
Vol 2016 ◽  
pp. 1-6 ◽  
Author(s):  
Ashwani Kumar Dhingra ◽  
Bhawna Chopra ◽  
Rameshwar Dass ◽  
Sanjeev K. Mittal

In search of novel effective potent therapeutic agents delivered by oral route for inflammation treatment, some novel O-propargylated-N-acetylpyrazole analogs (5a–j) were prepared by treating N-acetylpyrazole (4a–j) derived from 1,3-diarylpropenones (3a–j) with propargyl bromide. Claisen-Schmidt condensation of a series of substituted aryl ketones 1 and benzaldehydes 2 in glacial acetic acid afforded 1,3-diarylpropenones which on further treatment with hydrazine hydrate in acetic acid under reflux conditions afforded 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles (4a–j). The products were characterized by using spectroscopic techniques such as IR and NMR. In addition, the in vivo anti-inflammatory activity of the synthesized compounds was determined using the carrageenan-induced paw oedema method in rats.


2022 ◽  
Vol 144 ◽  
pp. 10-17
Author(s):  
Emanuelle G. Machado ◽  
Nerilson M. Lima ◽  
Maria Patricia Nascimento ◽  
Heberson T. Silva ◽  
Cleonice Aparecida Souza ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document