Açık Akademik Arşiv Sistemi

Synthesis, characterization, biological evaluation, and molecular docking studies of some piperonyl-based 4-thiazolidinone derivatives

Show simple item record

dc.contributor.authors Bilgicli, HG; Taslimi, P; Akyuz, B; Tuzun, B; Gulcin, I;
dc.date.accessioned 2020-02-24T14:21:17Z
dc.date.available 2020-02-24T14:21:17Z
dc.date.issued 2019
dc.identifier.citation Bilgicli, HG; Taslimi, P; Akyuz, B; Tuzun, B; Gulcin, I; (2019). Synthesis, characterization, biological evaluation, and molecular docking studies of some piperonyl-based 4-thiazolidinone derivatives. ARCHIV DER PHARMAZIE, , -
dc.identifier.issn 0365-6233
dc.identifier.uri https://doi.org/10.1002/ardp.201900304
dc.identifier.uri https://hdl.handle.net/20.500.12619/45277
dc.description.abstract Heterocyclic compounds are of particular importance among pharmacologically active compounds. In this study, some piperonyl-based 4-thiazolidinone derivatives (2a-i) were synthesized and characterized by spectroscopic assays. All molecules were tested as enzyme inhibitory factors. These compounds were effective inhibitors of the enzymes acetylcholinesterase (AChE), alpha-glycosidase (alpha-Gly), and the human carbonic anhydrase I and II isoforms (hCA I and II), with K-i values in the range of 8.90-66.51 nM for alpha-Gly, 94.8-289.5 nM for hCA I, 106.3-304.6 nM for hCA II, and 0.55-2.36 nM for AChE. The synthesized molecules were also studied theoretically. Molecular docking calculations were performed to investigate the interaction between the target protein and molecules. CA inhibitor compounds have been clinically used for almost 60 years as antiglaucoma and diuretic drugs. The inhibition of the AChE enzyme results in the blockage of ACh hydrolysis. On the contrary, the design of inhibitor compounds or/and modulators for AChE is of major interest as it is one of the most popular tools to prevent Alzheimer's disease.
dc.language English
dc.publisher WILEY-V C H VERLAG GMBH
dc.subject Chemistry
dc.title Synthesis, characterization, biological evaluation, and molecular docking studies of some piperonyl-based 4-thiazolidinone derivatives
dc.type Early Access
dc.contributor.department Sakarya Üniversitesi/Fen-Edebiyat Fakültesi/Kimya Bölümü
dc.contributor.saüauthor Genç Bilgiçli, Hayriye
dc.relation.journal ARCHIV DER PHARMAZIE
dc.identifier.wos WOS:000499004600001
dc.identifier.doi 10.1002/ardp.201900304
dc.identifier.eissn 1521-4184
dc.contributor.author Genç Bilgiçli, Hayriye
dc.contributor.author Parham Taslimi
dc.contributor.author Busra Akyuz
dc.contributor.author Burak Tuzun
dc.contributor.author Ilhami Gulcin


Files in this item

Files Size Format View

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record