Scopus
🔓 Açık Erişim YÖKSİS Eşleşti
Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II)
Journal of Enzyme Inhibition and Medicinal Chemistry · Şubat 2015
YÖKSİS Kayıtları
Synthesis and Evaluation of New Thiadiazole Derivatives as Potential Inhibitors of Human Carbonic Anhydrase Isozymes hCA I and hCA II
Journal of Enzyme Inhibition and Medicinal Chemistry · 2015 SCI
PROFESÖR KAAN KÜÇÜKOĞLU →
Makale Bilgileri
DergiJournal of Enzyme Inhibition and Medicinal Chemistry
Yayın TarihiŞubat 2015
Cilt / Sayfa30 · 32-37
Scopus ID2-s2.0-84921288608
Erişim🔓 Açık Erişim
Özet
2-[[5-(2,4-Difluoro/dichlorophenylamino)-1,3,4-thiadiazol-2-yl]thio] acetophenone derivatives (3a-s) were designed as human carbonic anhydrase isozymes (hCA-I and hCA-II) inhibitors and synthesized. hCA-I and hCA-II were purified from erythrocyte cells by the affinity chromatography. The inhibitory effects of 18 newly synthesized acetophenones on hydratase activity of these isoenzymes were studied in vitro. The average IC50 values of the new compounds for hydratase activity ranged from 0.033 to 0.14 μM for hCA-I and from 0.030 to 0.11 μM for hCA-II. Among the newly synthesized compounds, 2-[[5-(2,4-dichlorophenylamino)-1,3,4-thiadiazol-2-yl]thio]-4′-bromoacetophenone (3n) can be considered as a promising hCA-II inhibitor owing to its selective and potent inhibitory effect on hCA-II.
Yazarlar (6)
1
Mehlika Dilek Altıntop
ORCID: 0000-0002-8159-663X
2
Ahmet Özdemir
3
Kaan Kucukoglu
ORCID: 0000-0001-8977-9775
4
Gülhan Turan-Zitouni
5
Hayrunnisa Nadaroglu
6
Zafer Asım Kaplancıklı
Anahtar Kelimeler
Carbonic anhydrase
Hydratase activity
Thiadiazole
Kurumlar
Anadolu Üniversitesi
Eskisehir Turkey
Atatürk Üniversitesi
Erzurum Turkey
Metrikler
15
Atıf
6
Yazar
3
Anahtar Kelime