89866-55-7Relevant academic research and scientific papers
Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents
Bare,McLaren,Campbell,Firor,Resch,Walters,Salama,Meiners,Patel
, p. 2561 - 2573 (2007/10/02)
A series of 1-substituted 4-amino-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid esters and amides were synthesized and screened for anxiolytic activity in the shock-induced suppression of drinking (SSD) test. The compounds were also tested for their ability to displace [3H]flunitrazepam (FLU) from brain benzodiazepine (BZ) binding sites. Many compounds were active in these screens and, additionally, demonstrated a selectivity for the type 1 BZ (BZ1) receptor over the type 2 BZ (BZ2) receptor as indicated by Hill coefficients significantly less than unity and analysis of [3H]FLU binding results from different brain regions. Based on the results of structure-activity studies of these compounds, a hypothesis was proposed to explain the structural features necessary for optimal interaction with brain BZ receptors. A detailed pharmacological evaluation of one of the most potent behaviorally active compounds (27) demonstrated it to be BZ1 selective; also, in comparison to diazepam, 27 showed minimal sedative and alcohol interactive properties at therapeutically effective doses.
Pyrazolo[3,4-b]pyridine carboxylic acid esters and their pharmaceutical use
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, (2008/06/13)
Compounds of the formula (I): STR1 wherein R1, R3, R4, R5 and R6 have defined values and the N-oxides at the 7-position of the pyrazolo[3,4-b]pyridine ring system and the pharmaceutically-acceptable acid-addition salts thereof, processes for their preparation and use, pharmaceutical compositions, and intermediates for preparing said compounds of the formula (I). The compounds of formula (I) are central nervous system depressants, for example anxiolytic agents.
