- The synthesis of 4-(3,3-dimethyl-3H-pyrrolo[2,3-f] quinolin-2-yl)pyrazoles and 4-(3,3-dimethyl-3H-pyrrolo[3,2-h] quinolin-2-yl)pyrazoles
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(Chemical Equation Presented) 5-Hydrazinoquinoline and 8-hydrazinoquinoline were converted via Fischer syntheses with 3-methylbutan-2-one into pyrido-indolenines 2,3,3-trimethyl-3H-pyrrolo[2,3-f]quinoline 7 and 2,3,3-trimethyl-3H-pyrrolo[ 3,2-h]quinoline 11, respectively. Exposure of the indolenines to the Vilsmeier reagent produced aminomethylene-malondialdehydes 8 and 12, which reacted with hydrazine or arylhydrazines to give 4-(3H-pyrrolo[2,3-f]quinolin-2-yl)- and 4-(3H-pyrrolo[3,2-h]quinolin-2-yl)- pyrazoles, 9 and 13.
- Rashidi,Afghan,Baradarani, Mehdi M.,Jouleb, John A.
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body text
p. 428 - 431
(2009/09/25)
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- Structure-activity relationship studies on N′-aryl carbohydrazide P2X7 antagonists
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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.
- 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.
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experimental part
p. 3030 - 3034
(2009/04/10)
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- ACYLHYDRAZIDE P2X7 ANTAGONISTS AND USES THEREOF
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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
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Page/Page column 42-43
(2008/06/13)
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- METHODS FOR PREPARING SODIUM-HYDROGEN EXCHANGER TYPE-1 INHIBITORS
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This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.
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- Preparation of sodium-hydrogen exchanger type-1 inhibitors
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This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ 1intermediates of the NHE-1 inhibitors and a new almost colorless form of the NHE-1 inhibitor N-(5-cyclopropyl-1-quinolin-5-yl-1H-pyrazole-4-carbonyl)-guanidine.
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