Azabicyclo[3.1.0]hexane-1-carbohydrazides as potent and selective GHSR1a ligands presenting a specific invivo behavior

ChemMedChem

Volumn 6, Issue 11, 2011, Pages 1981-1985

  Sabbatini, Fabio Maria ^a   Melotto, Sergio ^a   Bernasconi, Giovanni ^a   Bromidge, Steve M ^a   D'Adamo, Lucilla ^a   Rinaldi, Marilisa ^a   Savoia, Chiara ^a   Mundi, Claudia ^a   di Francesco, Carla ^a   Zonzini, Laura ^a   Costantini, Vivian J A ^a   Perini, Benedetta ^a   Valerio, Enzo ^a   Pozzan, Alfonso ^a   Perdonà, Elisabetta ^a   Visentini, Filippo ^a   Corsi, Mauro ^a   di Fabio, Romano ^a  

^a Aptuit Inc   (United States)

Author keywords

Body weight; Food intake; Ghrelin; GHSR1a antagonists

Indexed keywords

AZABICYCLO[3.1.0]HEXANE 1 CARBOHYDRAZIDE DERIVATIVE; BICYCLO COMPOUND; GHRELIN; GHRELIN RECEPTOR; GSK 1614343; HORMONE RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ANIMALS; APPETITE STIMULANTS; BODY WEIGHT; CIRCULAR DICHROISM; EATING; FEMALE; GHRELIN; HYDRAZINES; LIGANDS; MOLECULAR STRUCTURE; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, GHRELIN; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80055024313     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201100285     Document Type: Article

References (15)

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12. Modeling studies were carried using MOE software from Chemical Computing Group. In particular, the Flexible Alignment module was used to superimpose and compare the 3.1.0 structures with the reference GHSR antagonist GSK1614343. Standard settings were used as implemented in the MOE 2008.10 release of the software, and the MMFF94 force field was used for conformational analysis.
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15. Biology and pharmacokinetics: All work involving animals was carried out in compliance with Italian national legislation (DL 116/92), which acknowledges the European Directive 86/609, and was performed according to internal review by the GSK Committee on Animal Research and Ethics (CARE).