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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Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2020-09, Vol.25 (18), p.4324
Hauptverfasser: Djuidje, Ernestine Nicaise, Durini, Elisa, Sciabica, Sabrina, Serra, Elena, Balzarini, Jan, Liekens, Sandra, Manfredini, Stefano, Vertuani, Silvia, Baldisserotto, Anna
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Sprache:eng
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Zusammenfassung: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