Discovery, Synthesis and Activity Evaluation of Novel Compounds Bearing 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine Moiety: A Review

Year 2019, , 60 - 70, 06.09.2019

Efe Doğukan Dincel Nuray Ulusoy Güzeldemirci

https://doi.org/10.26650/JARHS2019-616357

Abstract

Lately, much interest has been focused on the chemistry and the biological activity of fused heterocyclic compounds carrying nitrogen atoms because of their utility in various applications, and over the years N-bridged heterocyclic systems derived from 1,2,4-triazoles attracted the interest of researchers owing to the hopeful promise of their pharmacological activities such as antimicrobial, antifungal, molluscicidal, nematicidal, analgesic, anti-inflammatory, anticancer, phosphodiesterase 4 inhibitor, acetylcholinesterase, butyrylcholinesterases and alkaline phosphatase inhibitor. The fused ring of triazole and thiadiazines, named as triazolothiadiazines, represents a specific and important class of N-bridged heterocycles with their remarkable and wide range of biological activity and there are not enough studies that include the current developments associated with the new synthesis techniques and novel biological evaluation results of 1,2,4-triazolo[3,4-b][1,3,4] thiadiazine derivatives. In an attempt to overcome this deficiency in the literature, we deeply researched the literature and formed a review study about the discovery, synthesis and activity evaluation of new compounds bearing 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine moiety within the years of 1996-2019. We aimed to provide scientists with a wide data resource about 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine derivatives, thus helping them perform a more organized and fertile drug discovery operation during their experimental studies. 

Keywords

synthesis, biological activity, 1,2,4-triazolo[3,4-b][1,3,4]thiadiazine

1,2,4-triazolo[3,4-b][1,3,4]tiyadiazin Artığı İçeren Yeni Bileşiklerin Keşfi, Sentezi ve Biyolojik Aktiviteleri: Bir Derleme

Abstract

Son zamanlarda, geniş ölçekte çeşitlilik gösteren uygulamalardaki kullanımları nedeniyle azot atomu taşıyan kaynaşmış heterosiklik bileşiklerin kimyası ve biyolojik aktivitesi üzerine olan ilgi artmış ve yoğunlaşmıştır. Yıllar boyunca 1,2,4-triazollerden türetilen azot köprülü heterosiklik sistemler antimikrobiyal, antifungal, mollusisidal, nematisidal, analjezik, anti-inflamatuvar, antikanser, fosfodiesteraz-4 inhibitörü, asetilkolinesteraz, butirilkolinesteraz ve alkalen fosfataz inhibitörü gibi farklı biyolojik yönlerde, umut vadeden farmakolojik aktiviteler göstermiş ve buna bağlı olarak araştırmacıların ilgisini çekmiştir. Triazol ve tiyadiazin halkalarının kaynaşmasıyla oluşan triazolotiyadiazinler azot köprülü heterosiklik bileşikler arasında önemli ve dikkat çekici bir alt sınıfı oluşturmaktadır, buna karşın 1,2,4-triazolo[3,4-b][1,3,4]tiyadiazin türevlerinie ait güncel sentez teknikleri ve yeni biyolojik aktivite bulgularını içeren çalışmalar literatürde yeterli oranda bulunmamaktadır. Bu noktadan hareketle 1996-2019 tarih aralığını referans alarak 1,2,4-triazolo[3,4-b][1,3,4] tiyadiazin yapısı taşıyan yeni bileşiklerin keşfi, sentezi ve aktivite değerlendirmeleri ile ilişkili bir derleme çalışması yürütülmüştür. Araştırmacıların daha organize ve verimli bir ilaç keşif prosesi gerçekleştirmelerine yardımcı olmak amaçlanmıştır.

Keywords

sentez, biyolojik aktivite, 1,2,4-triazolo[3,4-b][1,3,4]tiyadiazin

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