308243-58-5Relevant articles and documents
Novel benzodiazepines derivatives as analgesic modulating for Transient receptor potential vanilloid 1
Liu, Yan,Liao, Chen,Zhou, Jiaqi,Liu, Chunxia,Li, Qifei,Jiang, Yue,Qian, Hai
, p. 4567 - 4573 (2018)
A new series of derivatives of 3-(7-chloro-5-(2-fluorophenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)propanoic acid were designed and synthesized as analgesic modulating for Transient receptor potential vanilloid 1. They were investigated for TRPV1 antagonistic activity in vitro, analgesic activity and sedative activity in vivo and aqueous solubility. Preliminary studies identified 3-(7-chloro-5-(2-fluorophenyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-N,N-dimethylpropanamide(Compound 11), as a potent analgesic modulating for TRPV1 with potent activity and good aqueous solubility.
Identification and structure-activity studies of novel ultrashort-acting benzodiazepine receptor agonists
Stafford,, Jeffrey A.,Pacofsky,, Gregory J.,Cox, Richard F.,Cowan, Jill R.,Dorsey Jr., George F.,Gonzales, Stephen S.,Jung, David K.,Koszalka, George W.,McIntyre, Maggie S.,Tidwell, Jeffrey H.,Wiard, Robert P.,Feldman, Paul L.
, p. 3215 - 3218 (2007/10/03)
The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists are described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The USA BZDs were characterized by full agonism profiles.