A study of the structure-activity relationship of GABAA-benzodiazepine receptor bivalent ligands by conformational analysis with low temperature NMR and X-ray analysis

Bioorganic and Medicinal Chemistry

Volumn 16, Issue 19, 2008, Pages 8853-8862

  Han, Dongmei ^a   Holger Forsterling F ^a   Li, Xiaoyan ^a   Deschamps, Jeffrey R ^b   Parrish, Damon ^b   Cao, Hui ^a   Rallapalli, Sundari ^a   Clayton, Terry ^a   Teng, Yun ^a   Majumder, Samarpan ^c   Sankar, Subramaniam ^d   Roth, Bryan L ^c   Sieghart, Werner ^e   Furtmuller, Roman ^e   Rowlett, James K ^f   Weed, Michael R ^g   Cook, James M ^a  

^a UNIVERSITY OF WISCONSIN MILWAUKEE   (United States)

^b NAVAL RESEARCH LABORATORY   (United States)

^c UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^d CASE WESTERN RESERVE UNIVERSITY SCHOOL OF MEDICINE   (United States)

^e MEDICAL UNIVERSITY OF VIENNA   (Austria)

^f HARVARD MEDICAL SCHOOL   (United States)

^g JOHNS HOPKINS BAYVIEW MEDICAL CENTER   (United States)

Author keywords

Benzodiazepines; Conformation; GABA; NMR

Indexed keywords

1,3 BIS(8 ACETYLENO 5,6 DIHYDRO 5 METHYL 6 OXO 4H IMIDAZO[1,5 A][1,4]BENZODIAZEPINE 3 CARBOXY)PROPYL DIESTER; 1,3 BIS(8 ACETYLENYL 6 PHENYL 4H BENZO[F]IMIDAZO[1,5 A][1,4]DIAZEPINE 3 CARBOXY)PROPYL DIESTER; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID ALPHA5 RECEPTOR; BENZODIAZEPINE RECEPTOR; DMH D 053; FLUNITRAZEPAM; LIGAND; METHYLAL; OXYGEN; RECEPTOR SUBTYPE; RY 080; UNCLASSIFIED DRUG; XLI 093;

ARTICLE; BINDING SITE; CRYSTAL STRUCTURE; DRUG POTENCY; IN VITRO STUDY; LIGAND BINDING; LOW TEMPERATURE PROCEDURES; MOLECULAR STABILITY; NONHUMAN; PROTEIN CONFORMATION; RECEPTOR BINDING; SOLID STATE; STRUCTURE ACTIVITY RELATION; X RAY ANALYSIS;

BENZODIAZEPINES; BINDING SITES; COLD TEMPERATURE; CRYSTALLOGRAPHY, X-RAY; DIMERIZATION; LIGANDS; MAGNETIC RESONANCE SPECTROSCOPY; MOLECULAR CONFORMATION; OXYGEN; RECEPTORS, GABA-A; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 52949130952     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2008.08.072     Document Type: Article

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