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357547

A novel approach for apoptosis and caspase-3 inhibition using new candidates of 1,5-Diaryl triazole-3-carboxamides

Article

Last updated: 05 Jan 2025

Subjects

-

Tags

Drug discovery and development

Abstract

Decreasing or inhibiting apoptosis is a therapeutic strategy to reduce the pathological states of diseases like stroke, neurodegeneration, retinal cell death, myocardial and liver ischemia, and inflammatory diseases such as sepsis, osteoarthritis, rheumatoid arthritis, and asthma. This study designed and synthesized a new series of apoptosis inhibitors using a 1,5-diaryl-1,2,4-triazole3-carboxamide scaffold. Compounds 8a, 8b, 9a, 10a, and 10b underwent biochemical, histological, immunohistochemical, and morphometric studies on two vital organs, viz. liver and ovary. In vivo, general biomarkers in the liver and ovary were measured and specific biomarkers were. Different stains such as Perl's iron stain, H & E stain and immune stain were utilized to evaluate caspase-3 inhibition. The findings are consistent with the docking study, i.e., compounds with two carbon linkers are better than those with longer or shorter ones as antiapoptotic. The most promising compounds 8a and 10a showed the highest potencies and selectivity against caspase-3 amongst other caspases like caspase -7, -8, -9, and 10 that could be considered for further clinical studies.

DOI

10.21608/odr.2024.287410.1041

Keywords

Antiapoptotic, triazole, Caspase, histopathology, Immunohistochemistry

Authors

First Name

Adel

Last Name

Abdelhakem

MiddleName

Mohamed

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Egypt,

Email

pharmacist_adel2010@yahoo.com

City

minia

Orcid

-

First Name

El-Shimaa

Last Name

Abdelhafez

MiddleName

M.N.

Affiliation

Département of medicinal chemistry, faculty of pharmacy, Minia university, Minia, Egypt.

Email

shimaanaguib_80@mu.edu.eg

City

Elmenya

Orcid

-

First Name

Samar

Last Name

Abbas

MiddleName

H.

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia 61519, Egypt

Email

drsamar77@hotmail.com

City

Elmenya

Orcid

-

First Name

Sara

Last Name

Abdel Hafez

MiddleName

-

Affiliation

Department of Histology and Cell Biology, Faculty of Medicine, Minia University, Egypt

Email

sara.abdelhafez@mu.edu.eg

City

-

Orcid

-

First Name

Walaa

Last Name

Abdelzaher

MiddleName

Yehia

Affiliation

Department of Pharmacology, Faculty of Medicine, Minia University, Egypt

Email

walaayehia22@yahoo.com

City

Elmenya

Orcid

-

First Name

Omar

Last Name

Aly

MiddleName

M.

Affiliation

Department of Medicinal Chemistry, Faculty of Pharmacy, Port Said University

Email

omarsokkar@pharm.psu.edu.eg

City

Port Said

Orcid

0000-0001-9299-920X

Volume

5

Article Issue

1

Related Issue

48068

Issue Date

2024-06-01

Receive Date

2024-05-05

Publish Date

2024-06-01

Page Start

64

Page End

75

Print ISSN

2812-6351

Online ISSN

2812-636X

Link

https://odr.journals.ekb.eg/article_357547.html

Detail API

https://odr.journals.ekb.eg/service?article_code=357547

Order

357,547

Type

Research Articles

Type Code

2,485

Publication Type

Journal

Publication Title

Octahedron Drug Research

Publication Link

https://odr.journals.ekb.eg/

MainTitle

A novel approach for apoptosis and caspase-3 inhibition using new candidates of 1,5-Diaryl triazole-3-carboxamides

Details

Type

Article

Created At

29 Dec 2024