Scopus
🔓 Açık Erişim
Novel 1,3-thiazolidin-4-one derivatives as promising anti- Candida agents endowed with anti-oxidant and chelating properties
European Journal of Medicinal Chemistry · Temmuz 2016
Makale Bilgileri
DergiEuropean Journal of Medicinal Chemistry
Yayın TarihiTemmuz 2016
Cilt / Sayfa117 · 144-156
Scopus ID2-s2.0-84963811487
Erişim🔓 Açık Erişim
Özet
Pursuing our recent outcomes regarding the antifungal activity of N-substituted 1,3-thiazolidin-4-ones, we synthesized thirty-six new derivatives introducing aliphatic, cycloaliphatic and heteroaromatic moieties at N1-hydrazine connected with C2 position of the thiazolidinone nucleus and functionalizing the lactam nitrogen with differently substituted (NO2, NH2, Cl and F) benzyl groups. These compounds were tested to evaluate their minimum inhibitory concentration (MIC) against several clinical Candida spp. with respect to topical and systemic reference drugs (clotrimazole, fluconazole, ketoconazole, miconazole, tioconazole, amphotericin B). Moreover, anti-oxidant properties were also evaluated by using different protocols including free radical scavenging (DPPH and ABTS), reducing power (CUPRAC and FRAP), metal chelating and phosphomolybdenum assays. Moreover, for the most active derivatives we assessed the toxicity (CC50) against Hep2 human cells in order to characterize them as multi-target agents for fungal infections.
Yazarlar (11)
1
Daniela Secci
2
Simone Carradori
3
Bruna Bizzarri
ORCID: 0000-0002-0822-2842
4
Paola Chimenti
5
Celeste De Monte
6
Adriano Mollica
7
Daniela Rivanera
8
Alessandra Zicari
9
Emanuela Mari
10
Gokhan Zengin
ORCID: 0000-0001-6548-7823
11
Abdurrahman Aktumsek
Anahtar Kelimeler
Anti-Candida activity
Anti-oxidant agents
Cytotoxicity
Metal chelating agents
N-benzyl-4-thiazolidinones
Kurumlar
Facoltà di Farmacia e Medicina
Rome Italy
Sapienza Università di Roma
Rome Italy
Selçuk Üniversitesi
Selçuklu Turkey
University of G. d'Annunzio Chieti and Pescara
Chieti Italy
Metrikler
49
Atıf
11
Yazar
5
Anahtar Kelime