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3 results on '"Fliur Macaev"'

1. Cyclodextrins in Asymmetric and Stereospecific Synthesis

Author

Fliur Macaev and Veaceslav Boldescu

Subjects
cyclodextrin, asymmetric synthesis, enantioselective organocatalysis, transition metal complexes, asymmetric catalysis, catalytic systems, Mathematics, QA1-939
Abstract

Since their discovery, cyclodextrins have widely been used as green and easily available alternatives to promoters or catalysts of different chemical reactions in water. This review covers the research and application of cyclodextrins and their derivatives in asymmetric and stereospecific syntheses, with their division into three main groups: (1) cyclodextrins promoting asymmetric and stereospecific catalysis in water; (2) cyclodextrins’ complexes with transition metals as asymmetric and stereospecific catalysts; and (3) cyclodextrins’ non-metallic derivatives as asymmetric and stereospecific catalysts. The scope of this review is to systematize existing information on the contribution of cyclodextrins to asymmetric and stereospecific synthesis and, thus, to facilitate further development in this direction.

Published
2015
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2. Facile and Convenient One-Pot Process for the Synthesis of Spirooxindole Derivatives in High Optical Purity Using (−)-(S)-Brevicolline as an Organocatalyst

Author

Vsevolod Pogrebnoi, Felix Shepeli, Natalia Sucman, Fliur Macaev, and Marina Zveaghintseva

Subjects
organocatalyzed reactions, spiro[oxindole-3,4'-4'H-pyrane], Brevicolline, Cinchonidine, Cinchonine, Mathematics, QA1-939
Abstract

The paper presents an application of the asymmetry approach to spirooxindoles via Brevicolline, Cinchonidine or Cinchonine catalyzed one-pot multicomponent synthesis. Brevicolline, in comparison with Cinchonidine or Cinchonine, catalyzes the reaction of isatins, acetylacetone/ethyl 3-oxobutanoate and malononitrile, with the formation of spiro[oxindole-3,4'-4'H-pirane] derivatives in an optically active form in very good to excellent yields.

Published
2011
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3. Chromenol Derivatives as Novel Antifungal Agents: Synthesis, In Silico and In Vitro Evaluation

Author

Vladimir Poroikov, Přemysl Mladěnka, Victor Ch. Kravtsov, Alejandro Carazo, Fliur Macaev, Marina Soković, Anthi Petrou, Elena Melnic, Eugenia Stingaci, Marina Zveaghintseva, Anastasia Smetanscaia, Vladimir Valica, Serghei Pogrebnoi, Athina Geronikaki, Jasmina Glamočlija, and Livia Uncu

Subjects
Antifungal Agents, In silico, Bifonazole, Drug Evaluation, Preclinical, Triazole, Pharmaceutical Science, Organic chemistry, 010402 general chemistry, 01 natural sciences, Article, Analytical Chemistry, Aspergillus fumigatus, chemistry.chemical_compound, QD241-441, In vivo, Drug Discovery, medicine, Physical and Theoretical Chemistry, C. albicans CYP51, biology, 010405 organic chemistry, Chemistry, antifungal activity, Biological activity, molecular docking, biology.organism_classification, chromenol, PASS, 3. Good health, 0104 chemical sciences, Molecular Docking Simulation, Biochemistry, Chromones, Chemistry (miscellaneous), Docking (molecular), Hypocreales, Molecular Medicine, Ketoconazole, vinyl-1,2,4-triazole, Mitosporic Fungi, medicine.drug
Abstract

Herein we report the synthesis of some new 1H-1,2,4-triazole functionalized chromenols (3a–3n) via tandem reactions of 1-(alkyl/aryl)-2-(1H-1,2,4-triazole-1-yl) with salicylic aldehydes and the evaluation of their antifungal activity. In silico prediction of biological activity with computer program PASS indicate that the compounds have a high novelty compared to the known antifungal agents. We did not find any close analog among the over 580,000 pharmaceutical agents in the Cortellis Drug Discovery Intelligence database at the similarity cutoff of 70%. The evaluation of antifungal activity in vitro revealed that the highest activity was exhibited by compound 3k, followed by 3n. Their MIC values for different fungi were 22.1–184.2 and 71.3–199.8 µM, respectively. Twelve from fourteen tested compounds were more active than the reference drugs ketoconazole and bifonazole. The most sensitive fungus appeared to be Trichoderma viride, while Aspergillus fumigatus was the most resistant one. It was found that the presence of the 2-(tert-butyl)-2H-chromen-2-ol substituent on the 4th position of the triazole ring is very beneficial for antifungal activity. Molecular docking studies on C. albicans sterol 14α-demethylase (CYP51) and DNA topoisomerase IV were used to predict the mechanism of antifungal activities. According to the docking results, the inhibition of CYP51 is a putative mechanism of antifungal activity of the novel chromenol derivatives. We also showed that most active compounds have a low cytotoxicity, which allows us to consider them promising antifungal agents for the subsequent testing activity in in vivo assays.

Published
2021

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