40877-17-6Relevant academic research and scientific papers
Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase
Ngu, Khehyong,Weinstein, David S.,Liu, Wen,Langevine, Charles,Combs, Donald W.,Zhuang, Shaobin,Chen, Xing,Madsen, Cort S.,Harper, Timothy W.,Ahmad, Saleem,Robl, Jeffrey A.
scheme or table, p. 4141 - 4145 (2011/08/06)
A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays.
Synthesis and structure-affinity relationships of 1-[ω-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones as 5-HT7 receptor ligands
Perrone, Roberto,Berardi, Francesco,Colabufo, Nicola A.,Lacivita, Enza,Leopoldo, Marcello,Tortorella, Vincenzo
, p. 646 - 649 (2007/10/03)
Structural requirements for 5-HT7 receptor affinity and selectivity over that for the 5-HT1A receptor were studied on a series of 1-[ω-(4-aryl-1-piperazinyl)alkyl]-1-aryl ketones. The presence of a hydroxy or methoxy substituent on aryl ketone moiety, alkyl chain length, and the nature of N-1-piperazine substituent were explored. 6-[4-(3-Benzisoxazolyl)-1-piperazinyl]-1-(2-hydroxyphenyl)-1-hexanone (40) and its methoxy analogue 43 exhibited high 5-HT7 receptor affinities (Ki = 2.93 nM and 0.90 nM, respectively) and agonist properties when tested for 5-HT7 receptor-mediated relaxation of substance P-induced guinea-pig ileum contraction.
INHIBITION OF MATRIX METALLOPROTEASES BY 2-(OMEGA-AROYLALKYL)-4-BIARYL-OXOBUTYRIC ACIDS
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, (2008/06/13)
The present invention provides pharmaceutical compositions and methods for treating certain conditions comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metal
