Back to Search Start Over

Skin Damages—Structure Activity Relationship of Benzimidazole Derivatives Bearing a 5-Membered Ring System

Authors :
Ernestine Nicaise Djuidje
Elisa Durini
Sabrina Sciabica
Elena Serra
Jan Balzarini
Sandra Liekens
Stefano Manfredini
Silvia Vertuani
Anna Baldisserotto
Source :
Molecules, Vol 25, Iss 18, p 4324 (2020)
Publication Year :
2020
Publisher :
MDPI AG, 2020.

Abstract

In the search for scaffolds for multifunctional compounds we investigated the structure activity relationship of a class of benzimidazole derivatives bearing 5-membered ring. The newly synthesized and the already known compounds were divided into three classes that present different substituent at 5 position of the benzimidazole ring (-H, -COOH or –SO3H) and different heterocycle at position 2 (thiophene, furan or pyrrole). All the derivatives were synthesized and tested to determine their photoprotective profile against UV rays, in vitro antioxidant capacity against different radicals (DPPH and FRAP test), antifungal inhibitory activity (dermatophytes and Candida albicans), antiviral and antiproliferative activity. A Structure-Activity Relationship study indicated compound 10, bearing a pyrrole heterocycle on the benzimidazole ring, as the best multifunctional derivative of the series and as potential candidate for the development of drugs especially in case of melanoma.

Details

Language :
English
ISSN :
14203049
Volume :
25
Issue :
18
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.79ce588d2ec24ee8bfeb47fe1bba81d1
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules25184324