22713-97-9Relevant academic research and scientific papers
Oxidative azacyclization of 1-monosubstituted thioureas in reaction with [bis(acyloxy)iodo]arenes to form 1,2,4-thiadiazole derivatives
Mamaeva, Elena A.,Bakibaev, Abdigali A.
, p. 7521 - 7525 (2003)
For the first time, derivatives of 1,2,4-thiadiazoles have been obtained by the reaction of [bis(acyloxy)iodo]arenes with 1-monosubstituted thioureas. 1-Acetylthiourea is subject to intermolecular azacyclization to form 3,5-bis-(acetylamino)-1,2,4-thiadia
External oxidant-free electrooxidative intramolecular S-N bond formation for one-pot synthesis for 3,5-disubstituted 1,2,4-thiadiazoles
Zhong, Qihao,Sheng, Shouri,Chen, Junmin
, p. 988 - 993 (2020/07/04)
An electrochemical oxidative reaction protocol for the synthesis of 5-amino and 3,5-diamino substituted 1,2,4-thiadiazole derivatives has been developed under undivided electrolytic conditions. The newly developed one-pot methodology involves the reaction
Synthesis of 5-Amino and 3,5-Diamino Substituted 1,2,4-Thiadiazoles by I2-Mediated Oxidative N-S Bond Formation
Wang, Bingnan,Meng, Yinggao,Zhou, Yiming,Ren, Linning,Wu, Jie,Yu, Wenquan,Chang, Junbiao
, p. 5898 - 5903 (2017/06/07)
An oxidative N-S bond formation reaction has been established for 1,2,4-thiadiazole synthesis employing molecular iodine as the sole oxidant. The features of the present reaction include no use of transition metals, mild reaction conditions, simple operat
Non-ATP competitive glycogen synthase kinase 3β (GSK-3β) inhibitors: Study of structural requirements for thiadiazolidinone derivatives
Castro, Ana,Encinas, Arantxa,Gil, Carmen,Braese, Stefan,Porcal, Williams,Perez, Concepcion,Moreno, Francisco J.,Martinez, Ana
, p. 495 - 510 (2008/04/05)
The 2,4-disubstituted thiadiazolidinones (TDZD) were described as the first non-ATP competitive GSK-3β inhibitors. New modifications in this heterocyclic ring are here reported to study the influence on the biological activity. The basic skeleton of 1,2,4-thiadiazole and also one of the carbonyl groups are kept, while different modifications are introduced in positions 3 and 5, respectively. The GSK-3β activity of the new thiadiazole derivatives here synthesized showed IC50 values for some of the compounds in the micromolar range. Additionally, ATP competition studies have been carried out, showing that as well as the first generation of TDZD, these new compounds act in a non-competitive manner. With this study, additional requirements for the biological activity of the TDZD family have been delineated.
