3394-24-9Relevant academic research and scientific papers
Thiocyanation and 2-Amino-1,3-thiazole Formation in Water Using Recoverable and Reusable Glycosylated Resorcin[4]arene Cavitands
Husain, Ali A.,Bisht, Kirpal S.
, p. 9928 - 9935 (2020/09/03)
A family of three spatially directional resorcin[4]arene cavitand glycoconjugates (RCGs) have been applied as efficient recoverable and reusable inverse phase transfer catalysts for eco- A nd environmentally friendly thiocyanation and 2-amino-1,3-thiazole formation reactions in water. The results show that RCGs (1 mol %) were capable of hosting and catalyzing various water-insoluble bromo/thiocyanato substrates in water without the use of any co-organic solvents. The recoverability and reusability of RCG catalytic systems, that is, RCG1 and RCG3, were also examined upon a simple extraction of the desired products using DCM or ethyl acetate, followed by subjecting the recovered aqueous solution containing the RCG catalysts to the next reaction cycles.
A library of novel allosteric inhibitors against fructose 1,6-bisphosphatase
Heng, Sabrina,Gryncel, Kimberly R.,Kantrowitz, Evan R.
experimental part, p. 3916 - 3922 (2009/10/02)
The identification of a proper lead compound for fructose 1,6-bisphosphatase (FBPase) is a critical step in the process of developing novel therapeutics against type-2 diabetes. Herein, we have successfully generated a library of allosteric inhibitors against FBPase as potential anti-diabetic drugs, of which, the lead compound 1b was identified through utilizing a virtual high-throughput screening (vHTS) system, which we have developed. The thiazole-based core structure was synthesized via the condensation of α-bromo-ketones with thioureas and substituents on the two aryl rings were varied. 4c was found to inhibit pig kidney FBPase approximately fivefold better than 1b. In addition, we have also identified 10b, a tight binding fragment, which can be use for fragment-based drug design purposes.
RING TRANSFORMATIONS OF OXAZOLES AND THEIR BENZO ANALOGUES. NEW SYNTHETIC ROUTE FOR 2H-IMIDAZOTHIADIAZINE AND N-HETEROARYL-o-AMINOPHENOL
Sasaki, Tadashi,Ito, Eikoh,Shimizu, Ikuo
, p. 2119 - 2129 (2007/10/02)
Ring transformations of certain functionalized oxazoles and their benzo analogues were studied.The α-(oxazol-2-ylthio) ketones 3a, b, c, and e gave 2H-imidazothiadiazines (4a, b, c, and e) on treatment with hydrazine hydrate in acetic acid.S
