An Insight into Rational Drug Design: The Development of In-House Azole Compounds with Antimicrobial Activity

Antimicrobial resistance poses a major threat to global health as the number of efficient antimicrobials decreases and the number of resistant pathogens rises. Our research group has been actively involved in the design of novel antimicrobial drugs. The blueprints of these compounds were azolic hete...

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Main Authors: Daniel Ungureanu (Author), Ovidiu Oniga (Author), Cristina Moldovan (Author), Ioana Ionuț (Author), Gabriel Marc (Author), Anca Stana (Author), Raluca Pele (Author), Mihaela Duma (Author), Brîndușa Tiperciuc (Author)
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Published: MDPI AG, 2024-08-01T00:00:00Z.
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042 |a dc 
100 1 0 |a Daniel Ungureanu  |e author 
700 1 0 |a Ovidiu Oniga  |e author 
700 1 0 |a Cristina Moldovan  |e author 
700 1 0 |a Ioana Ionuț  |e author 
700 1 0 |a Gabriel Marc  |e author 
700 1 0 |a Anca Stana  |e author 
700 1 0 |a Raluca Pele  |e author 
700 1 0 |a Mihaela Duma  |e author 
700 1 0 |a Brîndușa Tiperciuc  |e author 
245 0 0 |a An Insight into Rational Drug Design: The Development of In-House Azole Compounds with Antimicrobial Activity 
260 |b MDPI AG,   |c 2024-08-01T00:00:00Z. 
500 |a 10.3390/antibiotics13080763 
500 |a 2079-6382 
520 |a Antimicrobial resistance poses a major threat to global health as the number of efficient antimicrobials decreases and the number of resistant pathogens rises. Our research group has been actively involved in the design of novel antimicrobial drugs. The blueprints of these compounds were azolic heterocycles, particularly thiazole. Starting with oxadiazolines, our research group explored, one by one, the other five-membered heterocycles, developing more or less potent compounds. An overview of this research activity conducted by our research group allowed us to observe an evolution in the methodology used (from inhibition zone diameters to minimal inhibitory concentrations and antibiofilm potential determination) correlated with the design of azole compounds based on results obtained from molecular modeling. The purpose of this review is to present the development of in-house azole compounds with antimicrobial activity, designed over the years by this research group from the departments of Pharmaceutical and Therapeutical Chemistry in Cluj-Napoca. 
546 |a EN 
690 |a azoles 
690 |a organic synthesis 
690 |a antimicrobial 
690 |a heterocycles 
690 |a structure-activity relationship 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Antibiotics, Vol 13, Iss 8, p 763 (2024) 
787 0 |n https://www.mdpi.com/2079-6382/13/8/763 
787 0 |n https://doaj.org/toc/2079-6382 
856 4 1 |u https://doaj.org/article/beb1c8a910ae46e29bb4d6b6a0f36ad1  |z Connect to this object online.