Synthesis, carbonic anhydrase I and II isoenzymes inhibition properties, and antibacterial activities of novel tetralone-based 1,4-benzothiazepine derivatives
Yazarlar (7)
Prof. Dr. Mustafa CEYLAN
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Necibe Canan USTA
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Türkiye
Atatürk Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY |
| Dergi ISSN | 1095-6670 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 04-2017 |
| Cilt No | 31 |
| Sayı | 4 |
| Sayfalar | 21872 / 0 |
| DOI Numarası | 10.1002/jbt.21872 |
| Makale Linki | http://doi.wiley.com/10.1002/jbt.21872 |
| Özet |
| Benzothiazepine compounds have a wide range of applications such as antibacterial, antidepressants, anticonvulsants, antihypertensives, antibiotics, antifungal, hypnotic, enzyme inhibitors, antitumor, anticancer and anti-HIV agents. In this study, the synthesis of novel tetralone-based benzothiazepine derivatives (1-16) and their in vitro antibacterial activity and human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibitory effects were investigated. Both isoenzymes were purified by sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography from fresh human red blood cells. All compounds demonstrated the low nanomolar inhibitory effects on both isoenzymes using esterase activity. Benzothiazepine derivative 2 demonstrated the best hCA I inhibitory effect with K value of 18.19 nM. Also, benzothiazepine derivative 7 showed the best hCA II inhibitory effect with K value of 11.31 nM. On the other hand, acetazolamide clinically used as CA inhibitor, showed K value of 19.92 nM against hCA I and 33.60 nM against hCA II, respectively. |
| Anahtar Kelimeler |
| Antibacterial activity | Benzothiazepine | Carbonic anhydrase | Enzyme inhibition | Enzyme purification |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 43 |
| Google Scholar | 58 |