Synthesis and Characterization of New 1,2,4-Triazolo[1,5-a]pyridines That Extend the Life Span of Caenorhabiditis elegans via Their Anti-Inflammatory/Antioxidant Effects

Ramadan A Mekheimer; Ahmed A Radwan Sayed; Eltaib A Ahmed; Kamal U Sadek

doi:10.1002/ardp.201500069

Synthesis and Characterization of New 1,2,4-Triazolo[1,5-a]pyridines That Extend the Life Span of Caenorhabiditis elegans via Their Anti-Inflammatory/Antioxidant Effects

Arch Pharm (Weinheim). 2015 Sep;348(9):650-65. doi: 10.1002/ardp.201500069. Epub 2015 Jun 18.

Authors

Ramadan A Mekheimer^{1

2}, Ahmed A Radwan Sayed^{2

3}, Eltaib A Ahmed⁴, Kamal U Sadek²

Affiliations

¹ Department of Chemistry, Faculty of Science for Girls, King Abdulaziz University, Jeddah, Saudi Arabia.
² Department of Chemistry, Faculty of Science, El-Minia University, El-Minia, Egypt.
³ Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
⁴ Department of Chemistry, Faculty of Education, AlFashir University, AlFashir, Sudan.

PMID: 26088545
DOI: 10.1002/ardp.201500069

Abstract

In the present study, we describe the synthesis of a new set of 1,2,4-triazolo[1,5-a]pyridines and their fused ring systems. The products were assayed for various types of biological activities like anti-inflammatory and antioxidative activity. Compounds 4c, 4f, 12a, 14, 16, and 19 were found to reduce carrageenan- and dextran-induced inflammation in rats. In addition, compounds 4f and 12a were found to have antioxidative radical scavenging activity. Furthermore, these compounds were tested in the model system Caenorhabiditis elegans and there increased heat stress resistance, reduced the formation of advanced glycation end products, and finally extended the life span.

Keywords: 1,2,4-Triazolo[1,5-a]pyridines; Anti-inflammatory; Antioxidant; Caenorhabiditis elegans; Synthesis.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anti-Inflammatory Agents / chemical synthesis*
Anti-Inflammatory Agents / pharmacology*
Antioxidants / chemical synthesis*
Antioxidants / pharmacology*
Biphenyl Compounds / chemistry
Caenorhabditis elegans / drug effects*
Caenorhabditis elegans / metabolism
Carrageenan
Dextrans
Disease Models, Animal
Dose-Response Relationship, Drug
Drug Design
Edema / chemically induced
Edema / prevention & control
Glycation End Products, Advanced / metabolism
Glycosylation
Heat-Shock Response / drug effects
Longevity / drug effects
Male
Molecular Structure
Oxidative Stress / drug effects
Picrates / chemistry
Pyridines / chemical synthesis*
Pyridines / pharmacology*
Rats
Structure-Activity Relationship
Time Factors
Triazoles / chemical synthesis*
Triazoles / pharmacology*

Substances

Anti-Inflammatory Agents
Antioxidants
Biphenyl Compounds
Dextrans
Glycation End Products, Advanced
Picrates
Pyridines
Triazoles
1,2,4-triazole
Carrageenan
1,1-diphenyl-2-picrylhydrazyl