New 1,3,4-thiadiazole analogues: Synthesis, structural characterization, sar and qsar analysis studies
Küçük Resim Yok
Tarih
2018
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Karabük Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Tiyadiazol halkası içeren bileşikler uzun yıllardan beri çeşitli biyolojik aktivite gösterdiği için heterosiklik kimyada önemli bir yere sahiptir. Bu bileşikler antikanser, antimikrobiyal, antidepresan, antiparkinson, antioksidan, antifungal, antienflamatuar, antikonvülsan, antitüberküler, antidiyabetik aktivite gibi çeşitli biyolojik aktivite sergilemektedir. Bu araştırmanın amacı, biyolojik olarak aktivif olan tiyadiazol halkası ve sübstitüe açil grupları ihtiva eden bileşiklerin sentezi, yapısal karakterizasyonu, biyolojik aktivite çalışmaları, SAR ve QSAR çalışmaları olmak üzere çeşitli kısımlarda değerlendirilebilir. Bunun için, ilk olarak 3 ve 4 bileşikleri yüksek verimlerle (81 and 88%) sentezlendi. Ardından bu bileşiklerin çeşitli açil klorür türevleriyle (5a-n) olan reaksiyonlarından orta-yüksek verimlerle (%56-87) hedef bileşikler 6a-n ve 7a-n sentezlendi. Sentezlenen bileşikler; IR, 1H-NMR, 13C-NMR, kütle, X-Ray ve Elemantel Analiz teknikleri kullanılarak yapıları karakterize edilmiştir. Seztezlenen bileşiklerin in vitro antifungal aktivite değerleri belirlenmiştir. Bileşiklerin test funguslarına karşı göstermiş oldukları inhibisyon zonları, Minimum Fungisidal aktivite, Minimum inhibisyon konsantrasyonları ve lethal doz (LD50) değerleri belirlenmiştir. Bileşikler, test edilen bütün patojenlere karşı yüksek ve orta düzeyde aktivite göstermiştir.
Compounds containing thiadiazole rings have been of great importance in heterocyclic chemistry for many years since they exhibit variant biological activities such as anticancer, antimicrobial, antidepressant, anti-Parkinson's, antioxidant, antifungal, anti-inflammatory, anticonvulsant, anti-tubercular, and antidiabetic activities. The purpose of this study can be evaluated in various chapters such as the synthesis of new compounds containing thiadiazole rings and the acyl substitute groups of them, which have biological activity, their structural characterization, biological activity research, and SAR and QSAR studies. In order to attain this purpose, the first 3 and 4 compounds were synthesised with high yields (81 and 88%). Later, the target compounds 6a-n and 7a-n were synthesised from the reaction of these compounds with various acyl chloride derivatives (5a-n) with moderate yields (56-87%). The synthesised compounds were characterised using the IR, 1H-NMR, 13C-NMR, mass, X-Ray and Elemental Analysis techniques. The in vitro antifungal activities of the synthesised compounds were determined. The inhibition zones exhibited by the compounds against the test fungi, their Minimum Fungicidal activities, minimum inhibition concentration and the lethal dose (LD50) values were determined. The compounds exhibited high and moderate levels of activity against all testes pathogens.
Compounds containing thiadiazole rings have been of great importance in heterocyclic chemistry for many years since they exhibit variant biological activities such as anticancer, antimicrobial, antidepressant, anti-Parkinson's, antioxidant, antifungal, anti-inflammatory, anticonvulsant, anti-tubercular, and antidiabetic activities. The purpose of this study can be evaluated in various chapters such as the synthesis of new compounds containing thiadiazole rings and the acyl substitute groups of them, which have biological activity, their structural characterization, biological activity research, and SAR and QSAR studies. In order to attain this purpose, the first 3 and 4 compounds were synthesised with high yields (81 and 88%). Later, the target compounds 6a-n and 7a-n were synthesised from the reaction of these compounds with various acyl chloride derivatives (5a-n) with moderate yields (56-87%). The synthesised compounds were characterised using the IR, 1H-NMR, 13C-NMR, mass, X-Ray and Elemental Analysis techniques. The in vitro antifungal activities of the synthesised compounds were determined. The inhibition zones exhibited by the compounds against the test fungi, their Minimum Fungicidal activities, minimum inhibition concentration and the lethal dose (LD50) values were determined. The compounds exhibited high and moderate levels of activity against all testes pathogens.
Açıklama
Fen Bilimleri Enstitüsü, Kimya Ana Bilim Dalı, Organik Kimya Bilim Dalı
Anahtar Kelimeler
Kimya, Chemistry
