Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	The triazole ring as a privileged scaffold for putative antifungals: Synthesis and evaluation of a series of new analogues
Δημιουργός/Συγγραφέας:	Zoidis, Grigoris Kritsi, Eftichia Lecinska, Paulina Ivanov, Marija [EL] Ζουμπουλάκης, Παναγιώτης[EN] Zoumpoulakis, Panagiotis Sokovic, Marina Catto, Marco
Εκδότης:	Wiley
Ημερομηνία:	2021-01-08
Γλώσσα:	Αγγλικά
ISSN:	1860-7179 1860-7187
DOI:	10.1002/cmdc.202000312
Άλλο:	33428335
Περίληψη:	The significant antifungal activity of a series of novel 1,2,4-triazole derivatives against different strains of Candida albicans, Candida krusei and Aspergillus fumigatus, compared to the commercial fungicides ketoconazole and itraconazole, is reported. Systemic mycosis and invasive fungal infections, whether from immunodeficiency or hospital-acquired infection, have been on an upward trend for several years. The 1,2,4-triazole ring substituted with other aromatic and heteroaromatic systems plays an important role in the field of antifungal drug discovery and development. Thus, an extensive series of 29 triazoles, substituted in different positions with a variety of aromatic rings, has been designed, synthesized, and evaluated for their fungicidal activity. Almost all the agents tested in vitro showed high activity against all examined fungal strains. It is noteworthy that, in the case of A. fumigatus, all the examined compounds achieved equal or higher antifungal activity than ketoconazole, but less activity than itraconazole. Among all the derivatives studied, the dichlorourea analogue and bromo-substituted triazole stand out as the most promising compounds. Quantitative structure-activity relationship (QSAR) models were built for a systematic structure-activity relationship (SAR) profile to explain and potentially explore the potency characteristics of 1,2,4-triazole analogues.
Τίτλος πηγής δημοσίευσης:	ChemMedChem
Τόμος/Κεφάλαιο:	16
Τεύχος:	1
Σελίδες:	134-144
Θεματική Κατηγορία:	[EL] Χημική Βιολογία[EN] Chemical Biology [EL] Μικροβιολογία[EN] Microbiology [EL] Χημεία (Γενικά)[EN] Chemistry (General) [EL] Βιοτεχνολογία[EN] Biotechnology
Λέξεις-Κλειδιά:	MIC values QSAR Antifungal activity Synthesis Triazoles Antifungal Agents Aspergillus fumigatus Candida albicans Itraconazole Microbial Sensitivity Tests Quantitative Structure-Activity Relationship
Κάτοχος πνευματικών δικαιωμάτων:	Copyright © 2020 Wiley‐VCH GmbH
Ηλεκτρονική διεύθυνση στον εκδότη (link):	https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/cmdc.202000312
Ηλεκτρονική διεύθυνση περιοδικού (link) :	https://chemistry-europe.onlinelibrary.wiley.com/journal/18607187
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο