Romanian Society of Pharmaceutical Sciences
 

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DEVELOPMENT OF NEW 2-METHYL-4-SALICYLAMIDE THIAZOLE DERIVATIVES: SYNTHESIS, ANTIMICROBIAL ACTIVITY EVALUATION, LIPOPHILICITY AND MOLECULAR DOCKING STUDY

BIANCA POP 1, IOANA IONUȚ 1, GABRIEL MARC 1*, DAN CRISTIAN VODNAR 2, ADRIAN PÎRNĂU 3, LAURIAN VLASE 1, OVIDIU ONIGA 1

1“Iuliu Hațieganu” University of Medicine and Pharmacy, Faculty of Pharmacy, 12 Ion Creangă Street, 400010, Cluj-
Napoca, Romania
2University of Agricultural Sciences and Veterinary Medicine, Department of Food Science and Technology, 3-5 Mănăștur Street, 400372, Cluj-Napoca, Romania
3National Institute for Research and Development of Isotopic and Molecular Technologies, 67-103 Donath Street, 400293,
Cluj-Napoca, Romania

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A series of 15 new thiazolyl-salicylamide ethers were obtained through an alkylation reaction in alkaline medium. The compounds were physico-chemically and spectrally characterized. The evaluation of their antimicrobial activity highlighted the antifungal effect of compound 5n, which was equivalent to that of fluconazole. A molecular docking study revealed the structurally important elements for a better interaction with target lanosterol 14α-fungal demethylase. Given the importance of the lipophilicity for the penetration of biological membranes of bioactive molecules, this was evaluated in silico.