Thiazoles with Cyclopropyl Fragment As Antifungal, Anticonvulsant, and Anti- Agents: Synthesis, Toxicity Evaluation, and Molecular Docking Study

Overview

Journal Med Chem Res

Publisher Springer

Specialty Chemistry

Date 2018 Sep 18

PMID 30220831

Citations 13

Authors

Krzysztof Z Laczkowski

Natalia Konklewska

Anna Biernasiuk

Anna Malm

Kinga Salat

Anna Furgala

Katarzyna Dzitko

Adrian Bekier

Angelika Baranowska-Laczkowska

Agata Paneth

Affiliations

Soon will be listed here.

Abstract

Synthesis and investigation of antifungal, anticonvulsant and anti- activities of ten novel (2-(cyclopropylmethylidene)hydrazinyl)thiazole - are presented. Among the derivatives, compounds - and - possess very high activity against spp. ATCC with MIC = 0.015-7.81 µg/ml. Compounds - and - possess also very high activity towards most of strains of spp. isolated from clinical materials with MIC = 0.015-7.81 µg/ml. The activity of these compounds is similar and even higher than the activity of nystatin used as positive control. Additionally, compounds and showed interesting anticonvulsant activities in the MES test, whereas compounds and demonstrated the anticonvulsant activity in PTZ-induced seizures. Noteworthy, none of these compounds impaired animals' motor skills in the rotarod test. Moreover, thiazoles , , and showed significant anti- activity, with IC values 31-52 times lower than those observed for sulfadiazine. The results of the cytotoxicity evaluation, spp. and anti- activity studies showed that spp. and growth was inhibited at non-cytotoxic concentrations for the mouse L929 fibroblast and the African green monkey kidney (VERO) cells. Molecular docking studies indicated secreted aspartic proteinase (SAP) as possible antifungal target.

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