727382-73-2

Upstream product

• 19099-93-5 benzyl 4-oxo-1-piperidinecarboxylate 
• 4637-24-5 N,N-dimethyl-formamide dimethyl acetal 
• 5815-08-7 tert-Butoxybis(dimethylamino)methane 

Downstream Products

• 1355171-29-7 1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-carboxylic acid benzyl ester 
• 1421357-32-5 1-hydroxy-4,5,6,7-tetrahydropyrazolo[4,5-c]pyridine-5-carboxylic acid benzyl ester 
• 1421357-33-6 2-hydroxy-4,5,6,7-tetrahydropyrazolo[4,3-c]pyridine-5-carboxylic acid benzyl ester 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 4-(aminomethyl)-1-hydroxypyrazole analogues of muscimol as γ-aminobutyric acidA receptor agonists

A series of bioisosteric 4-(aminomethyl)-1-hydroxypyrazole (4-AHP) analogues of muscimol, a GABAA receptor agonist, has been synthesized and pharmacologically characterized at native and selected recombinant GABAA receptors. The unsubstituted 4-AHP analogue (2a) (EC 50 19 μM, Rmax 69%) was a moderately potent agonist at human α1β2γ2 GABAA receptors, and in SAR studies substitutions in the 3- and/or 5-position were found to be detrimental to binding affinities. Ligand-receptor docking in an α1β2γ2 GABAA receptor homology model along with the obtained SAR indicate that 2a and muscimol share a common binding mode, which deviates from the binding mode of the structurally related antagonist series based on 4-(piperidin-4-yl)-1- hydroxypyrazole (4-PHP, 1). Selectivity for α1β 2γ2 over ρ1 GABAA receptors was observed for the 5-chloro, 5-bromo, and 5-methyl substituted analogues of 2a illustrating that even small differences in structure can give rise to subtype selectivity.

Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: Synthesis and preliminary SAR analysis

In an attempt to search for a new class of antibacterial agents, we have discovered a series of pyrazole analogs that possess good antibacterial activity for Gram-positive and Gram-negative organisms via inhibition of type II bacterial topoisomerases. We have investigated the structure-activity relationships of this series, with an emphasis on the length and conformation of the linker. This work led to the identification of tetrahydroindazole analogs, such as compound 1, as the most potent class of compounds.

Pyrid-2-one derivatives and methods of use

Selected compounds are effective for treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stroke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.