Scopus
🔓 Açık Erişim YÖKSİS Eşleşti
Synthesis and evaluation of novel 2-[(1,2,4-triazol-3-yl)thio]acetamide derivatives as potential serum paraoxonase-1 (PON1) activators
Marmara Pharmaceutical Journal · Ocak 2017
YÖKSİS Kayıtları
Synthesis and evaluation of novel 2-[(1,2,4-triazol-3-yl)thio]acetamide derivatives as potential serum paraoxonase-1 (PON1) activators
Marmara Pharmaceutical Journal · 2017 ESCI
PROFESÖR KAAN KÜÇÜKOĞLU →
Makale Bilgileri
DergiMarmara Pharmaceutical Journal
Yayın TarihiOcak 2017
Cilt / Sayfa21 · 967-977
Scopus ID2-s2.0-85031431511
Erişim🔓 Açık Erişim
Özet
Coronary artery disease and low-density lipoprotein (LDL) levels in the blood have long been known to be associated with peripheral vascular diseases. Paraoxonase-1 (PON1) enzyme is related to serum levels of high-density lipoprotein (HDL) and protects LDL from oxidation which may result in development of microvascular disease in diabetes. The enzyme has a major role in the prevention of atherosclerosis besides antioxidant properties. Additionally, PON1 is important in the detoxification of organophosphate insecticides from the body. In this study, we aimed to synthesize highly active new compounds which can be a drug candidate and evaluate their effects on PON1 activity. Nine novel triazole compounds bearing thioacetamide moiety (5a-i) were synthesized and their in vitro PON1 activity was investigated. The PON1 enzyme was purified from human serum using ammonium sulfate precipitation method. Also, it was further purified using Sepharose 4B-L-tyrosine- 1-naphthylamine affinity chromatography. Among the synthesized triazole compounds, 5b, 5c, 5f and 5h have been determined to increase PON1 activity, remarkably. Compounds 5b, 5c, 5f and 5h bearing 5-nitrothiazole, benzothiazole, 6-ethoxybenzothiazole and 6-florobenzothiazole moieties could be considered to proceed in vivo investigations which is a further stage for a drug candidate.
Yazarlar (4)
1
Leyla Yurttaş
2
Kaan Kucukoglu
ORCID: 0000-0001-8977-9775
3
Hayrunnisa Nadaroglu
4
Zafer Asım Kaplancıklı
Anahtar Kelimeler
Antioxidant defence
Oxidative stress
Paraoxonase (PON1)
Thioacetamide
Triazole
Kurumlar
Anadolu Üniversitesi
Eskisehir Turkey
Atatürk Üniversitesi
Erzurum Turkey
Bülent Ecevit University
Zonguldak Turkey
Metrikler
3
Atıf
4
Yazar
5
Anahtar Kelime