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

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...

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Published in:Molecules (Basel, Switzerland) Switzerland), 2020-09, Vol.25 (18), p.4324
Main Authors: Djuidje, Ernestine Nicaise, Durini, Elisa, Sciabica, Sabrina, Serra, Elena, Balzarini, Jan, Liekens, Sandra, Manfredini, Stefano, Vertuani, Silvia, Baldisserotto, Anna
Format: Article
Language:English
Subjects:
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
benzimidazole
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Candida albicans - drug effects
Cell Line, Tumor
Cell Proliferation - drug effects
Free Radical Scavengers - chemistry
Free Radical Scavengers - pharmacology
Humans
melanoma
Radiation-Protective Agents - chemistry
Radiation-Protective Agents - pharmacology
Skin - drug effects
Skin - radiation effects
Structure-Activity Relationship
Ultraviolet Rays - adverse effects
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Summary: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 -SO H) 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 ), antiviral and antiproliferative activity. A Structure-Activity Relationship study indicated compound , 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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25184324