Scopus
YÖKSİS DOI Eşleşti
SJR Q2
Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives
Bioorganic and Medicinal Chemistry · Ocak 2017
YÖKSİS Kayıtları
Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives
Bioorganic medicinal chemistry · 2017 SCI-Expanded
Prof. Dr. KAAN KÜÇÜKOĞLU →
YÖKSİS Kayıtları — ISSN Eşleşmesi
Potential inhibitors of human carbonic anhydrase isozymes I and II: Design, synthesis and docking studies of new 1,3,4-thiadiazole derivatives
2017 ISSN: 0968-0896 SCI-Expanded
Prof. Dr. KAAN KÜÇÜKOĞLU →
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
2024 ISSN: 0968-0896 SCI-Expanded Q1
Prof. Dr. BAHADIR ÖZTÜRK →
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
2024 ISSN: 0968-0896 SCI-Expanded Q1
Doç. Dr. MEHMET OĞUZ →
Novel mitochondrial and DNA damaging fluorescent Calix[4]arenes bearing isatin groups as aromatase inhibitors: Design, synthesis and anticancer activity
2024 ISSN: 0968-0896 SCI-Expanded Q2
Prof. Dr. MUSTAFA YILMAZ →
Makale Bilgileri
ISSN09680896
Yayın TarihiOcak 2017
Cilt / Sayfa25 · 3547-3554
Scopus ID2-s2.0-85018860919
Özet
In the last years, inhibition of carbonic anhydrase (CA) has emerged as a promising approach for pharmacologic intervention in a variety of disorders such as glaucoma, epilepsy, obesity, and cancer. As a consequence, the design of CA inhibitors (CAIs) is a highly dynamic field of medicinal chemistry. Due to the therapeutic potential of thiadiazoles as CAIs, new 1,3,4-thiadiazole derivatives were synthesized and investigated for their inhibitory effects on hCA I and hCA II. Although the tested compounds did not carry a sulfonamide group, an important pharmacophore for CA inhibitory activity, it was a remarkable finding that most of them were more effective on hCAs than acetazolamide (AAZ), the reference agent. Among these compounds, N′-((5-(4-chlorophenyl)furan-2-yl)methylene)-2-((5-(phenylamino)-1,3,4-thiadiazol-2-yl)thio)acetohydrazide (3) was found to be the most effective compound on hCA I with an IC50 value of 0.14 nM, whereas N′-((5-(2-chlorophenyl)furan-2-yl)methylene)-2-((5-(phenylamino)-1,3,4-thiadiazol-2-yl)thio)acetohydrazide (1) was found to be the most potent compound on hCA II with an IC50 value of 0.15 nM. According to molecular docking studies, all compounds exhibited high affinity and good amino acid interactions similar to AAZ on the both active sites of hCA I and hCA II enzymes.
Yazarlar (7)
1
Mehlika Dilek Altıntop
ORCID: 0000-0002-8159-663X
2
Belgin Sever
ORCID: 0000-0003-4847-9711
3
Ahmet Özdemir
4
Kaan Kucukoglu
ORCID: 0000-0001-8977-9775
5
Hicran Onem
6
Hayrunnisa Nadaroglu
7
Zafer Asım Kaplancıklı
Anahtar Kelimeler
Carbonic anhydrase
Furan
Hydrazone
Molecular docking
Thiadiazole
Kurumlar
Anadolu Üniversitesi
Eskisehir Turkey
Atatürk Üniversitesi
Erzurum Turkey
Bülent Ecevit University
Zonguldak Turkey
Scimago Dergi (ISSN Eşleşmesi)
Bioorganic and Medicinal Chemistry
Q2
SJR Skoru0,582
H-Index198
YayıncıElsevier Ltd
ÜlkeUnited Kingdom
Drug Discovery (Q2)
Organic Chemistry (Q2)
Pharmaceutical Science (Q2)
Biochemistry (Q3)
Clinical Biochemistry (Q3)
Molecular Biology (Q3)
Molecular Medicine (Q3)
Metrikler
21
Atıf
7
Yazar
5
Anahtar Kelime