Synthesis, antimicrobial activity and modeling studies of thiazoles bearing pyridyl and triazolyl scaffolds

Basit Öğe Kaydı
dc.authorid0000-0001-6047-2796
dc.authorid0000-0003-1896-2729
dc.authorid0000-0002-0841-1299
dc.contributor.authorTay, Naime Funda
dc.contributor.authorBerk, Barkın
dc.contributor.authorDuran, Murat
dc.contributor.authorKayagil, İsmail
dc.contributor.authorYurttaş, Leyla
dc.contributor.authorBiltekin Kaleli, Sevde Nur
dc.contributor.authorYamaç, Mustafa
dc.contributor.authorKaraduman, Ayşe Betül
dc.contributor.authorDemirayak, Şeref
dc.date.accessioned2022-12-06T09:59:07Z
dc.date.available2022-12-06T09:59:07Z
dc.date.issued2022
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmasötik Kimya Ana Bilim Dalı
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Temel Eczacılık Bilimleri Bölümü, Farmasötik Mikrobiyoloji Ana Bilim Dalı
dc.description.abstractIn this study, novel 4-(5-((2/3/4-substituted benzyl)thio)-4-(4-substituted phenyl)-4H-1,2,4-triazol-3-yl)-2-(pyridin-3/4-yl)thiazoles were synthesized following a multi-step synthetic procedure. All the compounds were screened with a panel of gram positive/negative bacteria, yeasts, and molds for antimicrobial activity using the disc diffusion method. Then, the minimum inhibitor concentration (MIC) and the minimum bactericidal concentration (MBC) values of active compounds were determined against Micrococcus luteus, Bacillus cereus, Listeria monocytogenes, and Staphylococcus aureus using the broth microdilution technique. These compounds were also screened for their inhibitory activities against S. aureus DNA gyrase by supercoiling assay. Furthermore, the crystal structure of S. aureus DNA gyrase B ATPase was subjected to a docking experiment to identify the possible interactions between the most active ligand and the active site. Lastly, the in silico technique was performed to analyze and predict the drug-likeness, molecular and ADME properties of the synthesized molecules.
dc.description.sponsorshipEskisehir Osmangazi Universityen_US
dc.identifier.citationTay, N. F., Berk, B., Duran, M., Kayagil, İ., Yurttaş, L., Biltekin Kaleli, S. N. ... Demirayak, Ş. (2022). Synthesis, antimicrobial activity and modeling studies of thiazoles bearing pyridyl and triazolyl scaffolds. Zeitschrift fur Naturforschung - Section C Journal of Biosciences, 77(9-10), 429-446. https://doi.org/10.1515/znc-2022-0002
dc.identifier.doi10.1515/znc-2022-0002
dc.identifier.endpage446
dc.identifier.issn0939-5075
dc.identifier.issn1865-7125
dc.identifier.issue45574
dc.identifier.pmid35472438
dc.identifier.scopus2-s2.0-85129737809
dc.identifier.scopusqualityQ3
dc.identifier.startpage429
dc.identifier.urihttps://doi.org/10.1515/znc-2022-0002
dc.identifier.urihttps://hdl.handle.net/20.500.12511/10081
dc.identifier.volume77
dc.identifier.wos000788350300001en_US
dc.identifier.wosqualityQ4
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.institutionauthorBerk, Barkın
dc.institutionauthorBiltekin Kaleli, Sevde Nur
dc.institutionauthorDemirayak, Şeref
dc.language.isoen
dc.publisherWalter de Gruyter GmbH
dc.relation.ispartofZeitschrift fur Naturforschung - Section C Journal of Biosciencesen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAntimicrobial Activity
dc.subjectATPase
dc.subjectDocking
dc.subjectPyridine
dc.subjectThiazole
dc.subjectTriazole
dc.titleSynthesis, antimicrobial activity and modeling studies of thiazoles bearing pyridyl and triazolyl scaffolds
dc.typeArticle

Dosyalar

Lisans paketi
Listeleniyor 1 - 1 / 1
Küçük Resim Yok
İsim:
license.txt
Boyut:
1.44 KB
Biçim:
Item-specific license agreed upon to submission
Açıklama:
İndir

Koleksiyon

Eczacılık Fakültesi Makale Koleksiyonu
PubMed İndeksli Yayınlar Koleksiyonu
Scopus İndeksli Yayınlar Koleksiyonu
WoS İndeksli Yayınlar Koleksiyonu