Synthesis of Novel Amide Containing Schiffs Bases of 5-(4- Chloro-Phenyl)-Furan-2-Carboxaldehyde: Their In Vivo Anti- Inflammatory, Antioxidant and Antinociceptive Activities with Ulcerogenic Risk Evaluation
Authors
Abstract
A library of eighteen amide containing Schiffs bases has been synthesized and screened for their anti-inflammatory, antioxidant and antinociceptive activities. The compound 2 (COX-1 IC50 = 63.23 μM; COX-2 IC50 = 1.80 μM; SI = 35.12) exhibited potent selective COX-2 inhibition as compared to indomethacin (COX-1 IC50 = 3.60 μM; COX-2 IC50 = 7.50 μM; SI = 0.48). The compounds 2 and 7 reduced the COX-2 level to 7.5 ±0.35 nmole/min/ml and 6.8 ± 0.32nmole/min/ml respectively. The compounds 6 exhibited reduced the TNF-α level to 3.36 ± 0.18pg/ml. The compounds 2, 6, 7, 13 and 17 did not induce any gastric ulceration in comparison to the standard drug indomethacin.
Highlights
Copyright
© 2018, Author(s). This open-access article is available under the Creative Commons Attribution 4.0 (CC BY 4.0) International License (https://creativecommons.org/licenses/by/4.0/), which allows for unrestricted use, distribution, and reproduction in any medium, provided that the original work is properly cited.
Similar Articles
Synthesis of N-arylidene-2-(2-Phenoxyphenyl) Acetohydrazides as Anti-Inflammatory Agents
Shekarchi M, Navidpour L, Rajabi Khorami A, shekarchi M, Partoazar A, et al. Synthesis of N-arylidene-2-(2-Phenoxyphenyl) Acetohydrazides as Anti-Inflammatory Agents. Iran J Pharm Res. 2011;10(2):e125976. doi: https://doi.org/10.22037/ijpr.2011.968
Synthesis, Characterization and Anti-Inflammatory Activity of Some 1, 3,4 -Oxadiazole Derivatives
Kumar Singh A, Lohani M, Parthsarthy R. Synthesis, Characterization and Anti-Inflammatory Activity of Some 1, 3,4 -Oxadiazole Derivatives. Iran J Pharm Res. 2013;12(2):e125702. doi: https://doi.org/10.22037/ijpr.2013.1305
Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships
Zarghi A, Arfaei S. Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships. Iran J Pharm Res. 2011;10(4):e125993. doi: https://doi.org/10.22037/ijpr.2011.1047
Dual COX-2/TNF-α Inhibitors as Promising Anti-inflammatory and Cancer Chemopreventive Agents: A Review
Tajdari M, Peyrovinasab A, Bayanati M, Ismail Mahboubi Rabbani M, Abdolghaffari AH, et al. Dual COX-2/TNF-α Inhibitors as Promising Anti-inflammatory and Cancer Chemopreventive Agents: A Review. Iran J Pharm Res. 2024;23(1):e151312. doi: https://doi.org/10.5812/ijpr-151312
![Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-Substituted-4-(Thiophenyl) Thiazolyl] Acetates](https://brieflands.com/journals/ijpr/articles/125068/figures/thumbnail.webp)
Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-Substituted-4-(Thiophenyl) Thiazolyl] Acetates
Attimarad MV, Khedr MA, Aldhubiab BE. Microwave Assisted Synthesis, Pharmacological Activities, and Molecular Docking Studies of Ethyl 2-[2-Substituted-4-(Thiophenyl) Thiazolyl] Acetates. Iran J Pharm Res. 2017;16(4):e125068. doi: https://doi.org/10.22037/ijpr.2017.2122
- Scopus by DOI: 0
Last Update: 1 day ago
- Scopus by Title: 2
Last Update: 1 day ago
- Scopus by Title (Ref): 0
Last Update: 1 day ago
- CrossRef: 0
Last Update: 7 hours ago
- OpenAlex: 0
Last Update: 10 hours ago
- OpenCitations: 0
Last Update: 4 days ago