183303-71-1Relevant academic research and scientific papers
4-CYCLOPROPYL-1,2,3-THIADIAZOLE COMPOUND, AGROHORTICULTURAL PLANT DISEASE CONTROLLING AGENT AND METHOD OF USING THE SAME
-
Page/Page column 32, (2010/11/28)
The present invention relates to 1,2,3-thiadiazole compounds represented by formula (I): wherein R1, R2, R3, R4 and R5 each represents H, halogen, CN, alkyl, alkoxyalkyl, aryl, arylalkyl, alkylcarbony
Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors
Teng, Xin,Keys, Heather,Jeevanandam, Arumugasamy,Porco Jr., John A.,Degterev, Alexei,Yuan, Junying,Cuny, Gregory D.
, p. 6836 - 6840 (2008/03/14)
Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling non-regulated necrosis. This form of cell death can be induced in an array of cell types in apoptotic deficient conditions with death receptor family ligands. A series of [1,2,3]thiadiazole benzylamides was found to be potent necroptosis inhibitors (called necrostatins). A structure-activity relationship study revealed that small cyclic alkyl groups (i.e. cyclopropyl) and 2,6-dihalobenzylamides at the 4- and 5-positions of the [1,2,3]thiadiazole, respectively, were optimal. In addition, when a small alkyl group (i.e. methyl) was present on the benzylic position all the necroptosis inhibitory activity resided with the (S)-enantiomer. Finally, replacement of the [1,2,3]thiadiazole with a variety of thiophene derivatives was tolerated, although some erosion of potency was observed.
