Synthesis, Characterization, Carbonic Anhydrase Inhibitor Activity, and Docking Studies of phenylthiazol-2 (3h)-ylidene-isoquinoline-5-amine Derivatives
JOURNAL OF MOLECULAR STRUCTURE, cilt.1291, sa.2023, ss.1-11, 2023 (SCI-Expanded)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 1291 Sayı: 2023
- Basım Tarihi: 2023
- Dergi Adı: JOURNAL OF MOLECULAR STRUCTURE
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier, Chemical Abstracts Core, INSPEC
- Sayfa Sayıları: ss.1-11
- Açık Arşiv Koleksiyonu: AVESİS Açık Erişim Koleksiyonu
- Çanakkale Onsekiz Mart Üniversitesi Adresli: Evet
Özet
Phenylthiazol-2(3h)-ylidene-isoquinoline-5-amine derivatives(5a-r) were easily prepared from 5-aminoisoquinoline, thioisocyanate, and phenacyl bromide derivatives in the presence of triethylamine in tetrahydrofuran
(THF), and dimethyl formamide (DMF) in two steps. In the first step, thiourea was synthesized in THF reflux, 24
h and then in the second step, the formation of thiazole ring was ensured in EtOH-DMF (5:5 v/v), reflux, 24 h.
The newly synthesized compounds were characterized using 1
H NMR, 13C NMR, IR, and elemental analysis. The
inhibitory effects of 18 newly synthesized compounds (5a-r) on hydratase and esterase activities of carbonic
anhydrase isoenzymes (hCA I, II, IX, and X) were studied in vitro.