102852-56-2Relevant academic research and scientific papers
Synthesis of new heterocyclic compounds using 2-(3,3-dimethyl-1H- pyrroloisoquinolin-2(3H)-ylidene)malonaldehydes
Afghan, Arash,Roohi, Laia,Baradarani, Mehdi M.,Joule, John A.
, p. 706 - 712 (2014/06/10)
Isoquinolin-5-ylhydrazinium chloride 13 and 5-bromoisoquinolin-8- ylhydrazinium chloride 14 were converted via Fischer syntheses with 3-methylbutan-2-one into indolenines, 2,3,3-trimethyl-3H-pyrrolo[2,3-f] isoquinoline 15 and 5-bromo-2,3,3-trimethyl-3H-pyrrolo[3,2-h]isoquinoline 16, respectively. Exposure of the indolenines to the Vilsmeier reagent produced diformyl compounds 17 and 18, which reacted with arylhydrazines to give the corresponding pyrazoles 19a, 19b, 19c, 19d, 19e, 19f, 19g, 19h, 19i and 20a, 20b, 20c, 20d, 20e, 20f, 20g. Reaction of 17 with thiourea gave a pyrimidine-2(1H)-thione 23 or with hydroxylamine hydrochloride, an isoxazole 24.
Structure-activity relationship studies on N′-aryl carbohydrazide P2X7 antagonists
Nelson, Derek W.,Sarris, Kathy,Kalvin, Douglas M.,Namovic, Marian T.,Grayson, George,Donnelly-Roberts, Diana L.,Harris, Richard,Honore, Prisca,Jarvis, Michael F.,Faltynek, Connie R.,Carroll, William A.
experimental part, p. 3030 - 3034 (2009/04/10)
N′-Aryl acyl hydrazides were identified as P2X7 receptor antagonists. Structure-activity relationship (SAR) studies evaluated functional activity by monitoring calcium flux inhibition in cell lines expressing recombinant human and rat P2X7 receptors. Selected analogs were assayed in vitro for their capacity to inhibit release of cytokine IL-1β. Compounds with potent antagonist function were evaluated in vivo using the zymosan-induced peritonitis model. A representative compound effectively attenuated mechanical allodynia in a rat model of neuropathic pain.
ACYLHYDRAZIDE P2X7 ANTAGONISTS AND USES THEREOF
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Page/Page column 44, (2008/06/13)
The present invention discloses a compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein D, A, m, n, Rx and Ry are defined in the description. The present invention also relates to pharmaceutical compositions of compound
