33207-69-1Relevant academic research and scientific papers
Heterocyclic acylamide derivative and preparation method and pharmaceutical application thereof
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Paragraph 0443; 0450; 0451; 0452; 0453; 0454, (2017/07/19)
The invention relates to a heterocyclic acylamide derivative and a preparation method and pharmaceutical application thereof, in particular to a heterocyclic acylamide derivative shown as a general formula (I) or a stereoisomer and a pharmaceutically-acce
HETEROCYCLIC INHIBITORS OF NECROPTOSIS
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Page/Page column 36, (2009/04/25)
The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-α) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-α induce
Structure-activity relationship and liver microsome stability studies of pyrrole necroptosis inhibitors
Teng, Xin,Keys, Heather,Yuan, Junying,Degterev, Alexei,Cuny, Gregory D.
body text, p. 3219 - 3223 (2009/04/06)
Necroptosis is a regulated caspase-independent cell death pathway resulting in morphology reminiscent of passive non-regulated necrosis. Several diverse structure classes of necroptosis inhibitors have been reported to date, including a series of [1,2,3]thiadiazole benzylamide derivatives. However, initial evaluation of mouse liver microsome stability indicated that this series of compounds was rapidly degraded. A structure-activity relationship (SAR) study of the [1,2,3]thiadiazole benzylamide series revealed that increased mouse liver microsome stability and increased necroptosis inhibitory activity could be accomplished by replacement of the 4-cyclopropyl-[1,2,3]thiadiazole with a 5-cyano-1-methylpyrrole. In addition, the SAR and the cellular activity profiles, utilizing different cell types and necroptosis-inducing stimuli, of representative [1,2,3]thiadiazole and pyrrole derivatives were very similar suggesting that the two compound series inhibit necroptosis in the same manner.
