The chemistry of catechol-O-methyltransferase inhibitors.
作者： David A. Learmonth , László E. Kiss , Patrício Soares-da-Silva
DOI: 10.1016/B978-0-12-381326-8.00006-5
关键词:
摘要: Despite several drawbacks, levodopa (L-dopa) remains the gold standard drug for treatment of symptoms Parkinson's disease (PD). L-dopa is a pro-drug dopamine and used to elevate striatal levels neurotransmitter. One approach provide more continuous sustained delivery has targeted one principal enzymes responsible metabolic deactivation L-dopa, namely catechol-O-methyltransferase (COMT). The chapter will perspective medicinal chemistry behind discovery COMT inhibitors discuss how certain physicochemical parameters, including aqueous solubility lipophilicity, are thought influence pharmacokinetic properties such as absorption, distribution, bioavailability.
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