Synthesis, Biological Activity and Structure-Activity Relationship of Novel Diphenylurea Derivatives Containing Tetrahydroquinoline as Carbonic Anhydrase I and II Inhibitors
Yazarlar (9)
Düzce Üniversitesi, Türkiye
Sakarya Üniversitesi, Türkiye
Sakarya Uygulamalı Bilimler Üniversitesi, Türkiye
Sakarya Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Sakarya Üniversitesi, Türkiye
| Makale Türü |
Özgün Makale
|
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | CHEMISTRYSELECT |
| Dergi ISSN | 2365-6549 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 01-2018 |
| Cilt No | 3 |
| Sayı | 2 |
| Sayfalar | 529 / 534 |
| DOI Numarası | 10.1002/slct.201702562 |
| Makale Linki | http://doi.wiley.com/10.1002/slct.201702562 |
| Özet |
| A series of novel tetrahydroquinoline derivatives containing urea moiety was synthesized and their in vitro inhibitory effects on the human carbonic anhydrase isoenzymes (hCA−I and hCA‐II) were evaluated by using the CO2 hydration method. All the synthesized compounds exhibited inhibitory activity against both hCA I and hCA II with 1‐(4‐fluorophenyl)‐3‐(4‐(4‐p‐tolyl‐5,6,7,8‐tetrahydroquinolin‐2‐yl)phenyl)urea (7 k, IC50 value of 5.28 μM and 5.51 μM, against hCA I and hCA II, respectively) as the strongest inhibitor in this study. Structure‐activity relationships were also investigated. The results showed that most of synthesized compounds have a higher inhibitory activity against hCA I than hCA II. Also the substituents, containing two or more pairs of non‐bonding electrons, generally increased the hCA I and II inhibitory activity. Furthermore, some electronic parameters such as the highest occupied … |
| Anahtar Kelimeler |
| Carbonic anhydrase | enzyme inhibition | tetrahydroquinoline | urea |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 14 |
| Google Scholar | 18 |