Synthesis and Carbonic Anhydrase Inhibition of Novel 2 4 Aryl thiazole 2 yl 3a 4 7 7a tetrahydro 1 4 7 methanoisoindole 1 3 2 dione Derivatives
Yazarlar (5)
Cumhuriyet Üniversitesi, Türkiye
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Türkiye
Prof. Dr. Mustafa CEYLAN
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | ARCHIV DER PHARMAZIE |
| Dergi ISSN | 0365-6233 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 12-2016 |
| Cilt No | 349 |
| Sayı | 12 |
| Sayfalar | 955 / 963 |
| DOI Numarası | 10.1002/ardp.201600092 |
| Makale Linki | http://doi.wiley.com/10.1002/ardp.201600092 |
| Özet |
| Carbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO ) and water to bicarbonate (HCO ) and protons (H ) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new molecules 8a-i were confirmed by means of IR, H NMR, C NMR, and elemental analysis. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with K values in the range of 27.07-37.80 nM against hCA I and in the range of 11.80-25.81 nM against hCA II. Our findings suggest that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor with K values of 34.50 and 28.93 nM against the hCA I and hCA II isoenzymes, respectively. |
| Anahtar Kelimeler |
| Carbonic anhydrase | Enzyme inhibition | Isoindole | Thiazole |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 40 |
| Google Scholar | 47 |