Synthesis, characterization, carbonic anhydrase inhibitor activity, and docking studies of phenylthiazol-2 (3h)-ylidene-isoquinoline-5-amine Derivatives

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Tarih

2023

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Elsevier

Erişim Hakkı

info:eu-repo/semantics/closedAccess

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 1H 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.

Açıklama

Anahtar Kelimeler

Isoquinoline, Thiazole, Thiourea, Carbonic anhydrase, Enzyme inhibitor

Kaynak

Journal of Molecular Structure

WoS Q Değeri

Q2

Scopus Q Değeri

Q1

Cilt

1291

Sayı

Künye