scholarly journals Design, Synthesis, and Biological Evaluation of Some Novel Pyrrolizine Derivatives as COX Inhibitors with Anti-Inflammatory/Analgesic Activities and Low Ulcerogenic Liability

Molecules ◽  
2016 ◽  
Vol 21 (2) ◽  
pp. 201 ◽  
Author(s):  
Ahmed Gouda ◽  
Hamed Ali ◽  
Waleed Almalki ◽  
Mohamed Azim ◽  
Mohammed Abourehab ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Cox Inhibitors ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

Design, synthesis and biological evaluation of alantolactone derivatives as potential anti-inflammatory agents

2019 ◽  
Vol 28 (6) ◽  
pp. 849-856 ◽  
Author(s):  
Chetan Kumar ◽  
Anil Kumar ◽  
Yedukondalu Nalli ◽  
Waseem I. Lone ◽  
Naresh K. Satti ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of Polyfluoroalkylated Antipyrines and their Isomeric O-Methylpyrazoles

2019 ◽  
Vol 15 (5) ◽  
pp. 521-536 ◽  
Author(s):  
Natalya Agafonova ◽  
Evgeny Shchegolkov ◽  
Yanina Burgart ◽  
Victor Saloutin ◽  
Alexandra Trefilova ◽  
...  
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Antipyretic Activity ◽  
Starting Point ◽  
Anti Inflammatory ◽  
Analgesic Activities ◽  
Synthesis And Biological Evaluation ◽  
Cox 1

Background: Formally belonging to the non-steroidal anti-inflammatory drug class pyrazolones have long been used in medical practices. Objective: Our goal is to synthesize N-methylated 1-aryl-3-polyfluoroalkylpyrazolones as fluorinated analogs of antipyrine, their isomeric O-methylated derivatives resembling celecoxib structure and evaluate biological activities of obtained compounds. Methods: In vitro (permeability) and in vivo (anti-inflammatory and analgesic activities, acute toxicity, hyperalgesia, antipyretic activity, “open field” test) experiments. To suggest the mechanism of biological activity, molecular docking of the synthesized compounds was carried out into the tyrosine site of COX-1/2. Conclusion: The trifluoromethyl antipyrine represents a valuable starting point in design of the lead series for discovery new antipyretic analgesics with anti-inflammatory properties.

Ethyl benzoate bearing pyrrolizine/indolizine moieties: Design, synthesis and biological evaluation of anti-inflammatory and cytotoxic activities

2020 ◽  
Vol 94 ◽  
pp. 103371 ◽  
Author(s):  
Khalid M. Attalah ◽  
Ashraf N. Abdalla ◽  
Akhmed Aslam ◽  
Muhammad Ahmed ◽  
Mohammed A.S. Abourehab ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Ethyl Benzoate ◽  
Cytotoxic Activities ◽  
Design Synthesis ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Novel pyrazolopyrimidine derivatives targeting COXs and iNOS enzymes; design, synthesis and biological evaluation as potential anti-inflammatory agents

2014 ◽  
Vol 62 ◽  
pp. 197-211 ◽  
Author(s):  
Ahmed H. Abdelazeem ◽  
Shaimaa A. Abdelatef ◽  
Mohammed T. El-Saadi ◽  
Hany A. Omar ◽  
Shabana I. Khan ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation
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