Design, Synthesis, Investigation, and Biological Activity Assessments of (4-Substituted-Phenyl)-N-(3-morpholinopropyl)-3-phenylthiazol-2(3H)-imine Derivatives as Antifungal Agents
Year: 2024
Type: article
Abstract: High Resolution Image Download MS PowerPoint Slide In this study, a series of novel thiazol-2(3 H )-imine ( 2a – 2j ) were designed, synthesized, and characterized by means of 1 H NMR, 13 C NMR, and HRMS spectral analyses. In vitro antifungal activity was performed using a modified EUCAST protocol. Two of the synthesized compounds ( 2d and 2e ) showed activity against Candida albicans and Candida parapsilosis . Compound 2e showed activity against C. parapsilosis (MIC 50 = 1.23 μg/mL) for 48 h. This value is very similar to ketoconazole. The dynamic analysis of the potential compounds 2d and 2e revealed notable stability while interacting with the 14α-demethylase enzyme substrate. The absorption, distribution, metabolism, and excretion (ADME) studies of the candidate compound showed acceptable ADME parameter data and verified their drug-likeness characteristics. According to the results of this study, compound 4-(4-fluorophenyl)- N -(3-morpholinopropyl)-3-phenylthiazol-2(3 H )-imine ( 2e ) and its derivatives as 14α-demethylase inhibitors can be used as a new antifungal for further structural improvements and additional research.
Source: ACS Omega
Institutions: Anadolu University, Hawler Medical University
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $1,935
Funder: Anadolu Üniversitesi
OpenAlex ID: W4402806990