- 8-Hydroxyquinolin-2(1H)-one analogues as potential β2-agonists: Design, synthesis and activity study
-
β2-Agonists that bind to plasmalemmal β2-adrenoceptors causing cAMP accumulation are widely used as bronchodilators in chronic respiratory diseases. Here, we designed and synthesized a group of 8-hydroxyquinolin-2(1H)-one analogues and studied their β2-agonistic activities with a cellular cAMP assay. Compounds B05 and C08 were identified as potent (EC50 2-agonists among the compounds tested. They behaved as partial β2-agonists in non-overexpressed HEK293 cells, and possessed rapid smooth muscle relaxant actions and long duration of action in isolated guinea pig tracheal strip preparations. In summary, B05 and C08 are β2-agonists with potential applicability in chronic respiratory diseases.
- Xing, Gang,Zhi, Zhengxing,Yi, Ce,Zou, Jitian,Jing, Xuefeng,Yiu-Ho Woo, Anthony,Lin, Bin,Pan, Li,Zhang, Yuyang,Cheng, Maosheng
-
-
- Buttressing Salicylaldehydes: A Multipurpose Directing Group for C(sp3)?H Bond Activation
-
A palladium-catalyzed reaction of primary amines with iodoarenes produces γ-arylated primary amines. A bulky salicylaldehyde, which is marked as easily available, installable, removable, and recoverable, plays a key role in directing palladium to site-selectively activate the C?H bond located γ to the amino group.
- Yada, Akira,Liao, Wenqing,Sato, Yuta,Murakami, Masahiro
-
supporting information
p. 1073 - 1076
(2017/01/18)
-
- Catalytic C(sp3)?H Arylation of Free Primary Amines with an exo Directing Group Generated In Situ
-
Herein, we report the palladium-catalyzed direct arylation of unactivated aliphatic C?H bonds in free primary amines. This method takes advantage of an exo-imine-type directing group (DG) that can be generated and removed in situ. A range of unprotected aliphatic amines are suitable substrates, undergoing site-selective arylation at the γ-position. Methyl as well as cyclic and acyclic methylene groups can be activated. Furthermore, when aniline-derived substrates were used, preliminary success with δ-C?H arylation was achieved. The feasibility of using the DG component in a catalytic fashion was also demonstrated.
- Xu, Yan,Young, Michael C.,Wang, Chengpeng,Magness, David M.,Dong, Guangbin
-
supporting information
p. 9084 - 9087
(2016/07/26)
-
- Novel D3 Dopamine Receptor Agonists to Treat Dyskinesia in Parkinson's Disease
-
The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.
- -
-
Page/Page column 31
(2014/08/19)
-
- Hydrogenolysis of 3-methyl-4-phenylmethyl-5(2H)-isoxazolone derivatives: A reinvestigation
-
Hydrogenolysis of 3-methyl-4-phenylmethyl-5(2H)-isoxazolone (2a) and its derivatives 2b-e, 5a-e, 6a-e and 9a,b have been carried out over Pd/C and Raney-nickel.The products have been isolated and characterized.The intermediate products of hydrogenolysis of 2b-e have been trapped and simultaneous cleavage of N - O and C - C bonds in 9a,b has been suggested to explain the formation of the hydrogenolysis products 10a,b and 3a,b.
- Batra, Sanjay,Seth, M,Bhaduri, A P
-
-
- Alpha-(aminoalkyl-4-hydroxy-3-(alkylthio)benzenemethanols
-
Alpha-(aminoalkyl)-4-hydroxy-3-(alkylthio)benzenemethanols useful as intermediates and as antihypertensive agents are prepared by reduction of the corresponding aminoalkyl 4-hydroxy-3-(alkylthio)phenyl ketones.
- -
-
-
- Derivatives related to betaxolol with α- and β-adrenergic activities
-
The paper describes the synthesis and the pharmacological evaluation of some derivatives of betaxolol, all with an N-aralkylamine instead of the tertiobutylamine. These compounds have been tested for β1-adrenergic receptor antagonism on guinea pig atria, β2-adrenergic receptor antagonism on guinea pig trachea and α-adrenergic blocking activity on rat aorta. Compound U12 with a marked α-blocking activity and compound R8 with a β1/α ratio = 1 were selected for a haemodynamic study in the dog. The decrease in cardiac work and the diminution of total peripheral resistance exhibited by U12 are consistent with a dual α/β-blocking agent. Finally, structure-activity relationships are discussed.
- Leclerc,Decker,Schwartz
-
p. 1357 - 1367
(2007/10/02)
-
- α-{[(Arylalkyl)amino]alkyl}-4-hydroxy-3-(lower-alkylsulfinyl)benzenemethanols
-
The instant invention is directed to α-(aminoalkyl)-4-hydroxy-3-(alkylsulfinylbenzenemethanols and to a method of utilizing the compounds for reducing blood pressure in mammals.
- -
-
-