Open Journal of Medicinal Chemistry

Volume 5, Issue 4 (December 2015)

ISSN Print: 2164-3121   ISSN Online: 2164-313X

Google-based Impact Factor: 0.71  Citations  

Synthesis of Pyrroles and Condensed Pyrroles as Anti-Inflammatory Agents with Multiple Activities and Their Molecular Docking Study

HTML  XML Download Download as PDF (Size: 1539KB)  PP. 49-96  
DOI: 10.4236/ojmc.2015.54005    5,165 Downloads   8,057 Views  Citations

ABSTRACT

We herein disclose a series of novel pyrrole derivatives as well as fused pyrrolopyridines 6a,b and 7a,b, pyrrolopyrazoles 8a, b, pyrrolo[2,3-d]pyrimidine derivatives 10a-d, 12a,b, 14a,b, 18a,b, 20a,b, 21a,b, 22a,b, 23a,b, 24a,b, 31a,b, 36a,b, 40a,b, pyrrolo[1,2,6]thiadiazine derivatives 19a,b, pyrrolotriazolopyrimidines 25a,b, 26a,b, 27a,b and 28a,b, pyrrolo[2,3-d][1,2,3]triazine derivatives 32a,b and pyrrolo[2,3-d][1,3]oxazine derivatives 39a,b as novel compounds. All compounds were evaluated for their anti-inflammatory, analgesic (compared to the reference drug Indomethacin) and antimicrobial activities (compared to the reference drug Ampicillin and Fluconazole). Compounds 4d, 5b-d, 6a,b, 9c,d, 10d, 12ab, 13b, 19a,b, 21b, 23b, 31a,b, 38b and 40a were found to be the most active anti-inflammatory drugs exhibiting potency ranging from 1 - 1.01 compared to the reference drug indomethacin. In addition to docking study of these highly active twenty compounds against the active site of cyclooxygenase-2 enzyme (COX-2), among the tested compounds, compounds 5d, 9d, 11b, 12a, 13b and 32a showed multiple activities; anti-inflammatory, analgesic and anti-bacterial activities.

Share and Cite:

Sarg, M. , Koraa, M. , Bayoumi, A. and Gilil, S. (2015) Synthesis of Pyrroles and Condensed Pyrroles as Anti-Inflammatory Agents with Multiple Activities and Their Molecular Docking Study. Open Journal of Medicinal Chemistry, 5, 49-96. doi: 10.4236/ojmc.2015.54005.

Cited by

[1] New Pyrrole Derivatives as Promising Biological Agents: Design, Synthesis, Characterization, In Silico, and Cytotoxicity Evaluation
International Journal of …, 2022
[2] Acetic Acid‐Catalyzed Selective Synthesis of N‐Substituted 2‐Amino‐3‐Cyanopyrroles via a Three‐Component Reaction Between Carbohydrates, Primary Amines …
Asian Journal of Organic …, 2022
[3] (E)-1-(3-Benzoyl-4-phenyl-1H-pyrrol-1-yl)-3-phenylprop-2-en-1-one
Litina - Molbank, 2022
[4] Synthesis of novel pyrroles and fused pyrroles as antifungal and antibacterial agents
Hameed, AI Sayed… - Journal of enzyme …, 2021
[5] Contemporary advances of cyclic molecules proposed for inflammation
2021
[6] E/Z isomerization of ethyl 2-amino-1-(3-(ethoxycarbonyl)-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)-4-oxo-5-(2-oxo-2-phenylethylidene)-4,5-dihydro-1H-pyrrole-3 …
2020
[7] Synthesis and Anticancer Activity Study of Some Novel Substituted and Fused Pyridotriazepine Derivatives
2019
[8] Synthesis and highly potent anti-inflammatory activity of licofelone-and ketorolac-based 1-arylpyrrolizin-3-ones
2019
[9] Design, synthesis, molecular docking and biological screening of N-ethyl-N-methylbenzenesulfonamide derivatives as effective antimicrobial and antiproliferative …
2019
[10] Assessment of Anti-inflammatory Activity of Novel Compound of Indole Derivatives and Elucidation of Possible Mechanisms of Action
2019
[11] Evaluation of novel pyrrolopyrimidine derivatives as antiviral against gastroenteric viral infections
European Journal of Pharmaceutical Sciences, 2018
[12] Pyrrole and Fused Pyrrole Compounds with Bioactivity against Inflammatory Mediators
Molecules, 2017
[13] Preparation of novel pyrrol-2-one derivatives via an effective synthesis of new oxazole scaffold
Tetrahedron, 2017
[14] Synthesis and Structure Activity Relationship of Some Indole Derivatives as Potential Anti-inflammatory Agents
2017
[15] 4, 5, 6-7-ТЕТРАГИДРОБЕНЗО [b] ТИОФЕН-2-ИЛ) 4, 5-ДИГИДРО-1Н-ПИРРОЛ-3-КАРБОНОВОЙ КИСЛОТЫ, ОБЛАДАЮЩИЙ ПРОТИВОМИКРОБНОЙ …
2015

Copyright © 2024 by authors and Scientific Research Publishing Inc.

Creative Commons License

This work and the related PDF file are licensed under a Creative Commons Attribution 4.0 International License.