83019-57-2Relevant academic research and scientific papers
Esters of thiadiazole oxypropanolaine derivatives and pharmaceutical uses
-
, (2008/06/13)
Novel compounds of the general formula STR1 wherein R1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the STR2 group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR2 COR3, --NR2 CONR3 R4, --NR2 SO2 R3, --NR2 SO2 NR3 R4, or --NR2 COOR5, wherein R2, R3, R4 and R5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R3 and R5 are not hydrogen when B is --NR2 SO2 R3 or --NR2 COOR5, or R3 and R4 may together with N form a 5 to 7 membered heterocyclic group; and the pharmaceutically acceptable salts thereof.
Ultra-Short-Acting β-Adrenergic Receptor Blocking Agents. 3. Ethylenediamine Derivatives of (Aryloxy)propanolamines Having Esters on the Aryl Function
Erhardt, Paul W.,Woo, Chi M.,Matier, William L.,Gorczynski, Richard J.,Anderson, William G.
, p. 1109 - 1112 (2007/10/02)
Various ethylenediamine derivatives have been incorporated into the nitrogen substituent of certain short-acting (aryloxy)propanolamine systems that contain esters on their aryl functions.Although several of these compounds showed durations of action comparable to their prototypes, most of the nitrogen substituents significantly prolonged the duration of β-adrenergic blockade.Similarly, while one of the compounds showed appreciable cardioselectivity in vitro, generally, little enhancement of cardioselectivity was obtained.A brief discussion of structure-activity relationships observed for the ethylenediamine derivatives is presented.
β-Adrenergic Blocking Agents. 22. 1-Phenoxy-3-amino>-2-propanols
Large, M.S.,Smith, L.H.
, p. 1286 - 1292 (2007/10/02)
The synthesis of a series of 1-phenoxy-3-amino>-2-propanols is described.Many of the compounds are more potent than propanolol as β blockers, while having cardioselectivity comparable to that of practolol, when given intravenous
