Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 21, 2009, Pages 6053-6058

  Lee, Ju Yeon ^a   Yu, Juan ^a   Cho, Won Je ^b   Ko, Hyojin ^a   Kim, Yong Chul ^a  

^a Gwangju Institute of Science and Technology (GIST)   (South Korea)

^b Chonnam National University   (South Korea)

Author keywords

IL 1 ; P2X7 Receptor; Privileged structure; Pyrazolodiazepine

Indexed keywords

1 [N,O BIS(5 ISOQUINOLINESULFONYL) N METHYLTYROSYL] 4 PHENYLPIPERAZINE; 2'(3') O (4 BENZOYLBENZOYL)ATP; ADENOSINE TRIPHOSPHATE DERIVATIVE; ANTIINFLAMMATORY AGENT; BENZYL DERIVATIVE; DIAZEPINE DERIVATIVE; ETHIDIUM; INDOLE DERIVATIVE; INTERLEUKIN 1BETA; PURINERGIC P2X7 RECEPTOR; PURINERGIC RECEPTOR BLOCKING AGENT; PYRAZOLODIAZEPINE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CELL ACTIVATION; CELL DIFFERENTIATION; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOKINE RELEASE; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; EMBRYO; FLUORESCENCE ANALYSIS; HUMAN; HUMAN CELL; ISOMER; STEREOCHEMISTRY; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

ANTI-INFLAMMATORY AGENTS; CELL LINE; ETHIDIUM; HUMANS; INTERLEUKIN-1BETA; PYRAZOLES; RECEPTORS, PURINERGIC P2; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 71749104255     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.09.053     Document Type: Article

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29. + was determined by measuring fluorescence with a fluorescent plate reader (excitation filter of 530/20 and emission filter of 590/20).
30. IL-1β release was measured in differentiated THP-1 cells primed for 3 h with 25 ng/mL LPS and 10 ng/ml IFNγ, and then was stimulated with 1 mM BzATP for 30 min. Synthesized pyrazolodiazepin-8-one derivatives at 10 μM were treated for 30 min prior to BzATP. Supernatants were collected by centrifugation at 1000 rpm for 5 min and assayed for the presence of mature human IL-1β using an ELISA kit.