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作为ADAMTS7抑制剂的阿里硫胺的设计,合成和生物评估

Doretta Cuffaro1, Tina Burkhard2, Bianca Laura Bernardoni1

  • 1Department of Pharmacy, University of Pisa Via Bonanno 6 56126 Pisa Italy elisa.nuti@unipi.it +39 0502219551.

RSC medicinal chemistry
|August 16, 2024
PubMed
概括

研究人员开发了一种针对ADAMTS7的新型抑制剂,ADAMTS7是一种与动脉样硬化和冠心病相关的酶. 这种强大而有选择性的化合物显示出治疗心血管疾病治疗的治疗潜力.

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Sulfation and α-amino acid conjugation are two critical biotransformation reactions in drug metabolism. Sulfation, a phase II biotransformation reaction, involves adding a polar sulfate group to a drug, enhancing its water solubility and promoting excretion. This process can either co-occur with or occur independently of glucuronidation. Nonmicrosomal sulfotransferase enzymes catalyze the process. The reaction involves 3'-phosphoadenosine-5'-phosphosulfate or PAPS coenzyme...
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