1384129-37-6Relevant articles and documents
Discovery of pyrazole carboxylic acids as potent inhibitors of rat long chain l-2-hydroxy acid oxidase
Barawkar, Dinesh A.,Bandyopadhyay, Anish,Deshpande, Anil,Koul, Summon,Kandalkar, Sachin,Patil, Pradeep,Khose, Goraksha,Vyas, Samir,Mone, Mahesh,Bhosale, Shubhangi,Singh, Umesh,De, Siddhartha,Meru, Ashwin,Gundu, Jayasagar,Chugh, Anita,Palle, Venkata P.,Mookhtiar, Kasim A.,Vacca, Joseph P.,Chakravarty, Prasun K.,Nargund, Ravi P.,Wright, Samuel D.,Roy, Sophie,Graziano, Michael P.,Cully, Doris,Cai, Tian-Quan,Singh, Sheo B.
, p. 4341 - 4347 (2012/07/17)
Long chain l-2-hydroxy acid oxidase 2 (Hao2) is a peroxisomal enzyme expressed in the kidney and the liver. Hao2 was identified as a candidate gene for blood pressure (BP) quantitative trait locus (QTL) but the identity of its physiological substrate and its role in vivo remains largely unknown. To define a pharmacological role of this gene product, we report the development of selective inhibitors of Hao2. We identified pyrazole carboxylic acid hits 1 and 2 from screening of a compound library. Lead optimization of these hits led to the discovery of 15-XV and 15-XXXII as potent and selective inhibitors of rat Hao2. This report details the structure activity relationship of the pyrazole carboxylic acids as specific inhibitors of Hao2.
