Potent and selective inhibitors of long chain l-2-Hydroxy acid oxidase reduced blood pressure in DOCA salt-treated rats

DA Barawkar, A Meru, A Bandyopadhyay…

文献索引：Barawkar, Dinesh A.; Meru, Ashwin; Bandyopadhyay, Anish; Banerjee, Abir; Deshpande, Anil M.; Athare, Chandrashekhar; Koduru, Chandrasekhar; Khose, Goraksha; Gundu, Jayasagar; Mahajan, Koshu; Patil, Pradeep; Kandalkar, Sachin R.; Niranjan, Sanjay; Bhosale, Shubhangi; De, Siddhartha; Mukhopadhyay, Sudit; Chaudhary, Sumit; Koul, Summon; Singh, Umesh; Chugh, Anita; Palle, Venkata P.; Mookhtiar, Kasim A.; Vacca, Joseph; Chakravarty, Prasun K.; Nargund, Ravi P.; Wright, Samuel D.; Roy, Sophie; Graziano, Michael P.; Singh, Sheo B.; Cully, Doris; Cai, Tian-Quan ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 12 p. 919 - 923

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被引用次数: 11

摘要

l-2-Hydroxy acid oxidase (Hao2) is a peroxisomal enzyme with predominant expression in the liver and kidney. Hao2 was recently identified as a candidate gene for blood pressure quantitative trait locus in rats. To investigate a pharmacological role of Hao2 in the management of blood pressure, selective Hao2 inhibitors were developed. Optimization of screening hits 1 and 2 led to the discovery of compounds 3 and 4 as potent and selective ...