The Effect of Phenyl Substituents on the Release Rates of Esterase-Sensitive Coumarin-Based Prodrugs

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概要

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• A coumarin-based prodrug system has been recently developed in our laboratory for the preparation of esterase-sensitive prodrugs of amines, peptides, and peptidomimetics. The drug release rates from this prodrug system were found to be dependent on the structural features of the drug moiety. In certain cases, the release can be undesirably slow for drugs that are secondary amines with relatively high pK_a's. Aimed at finding ways to manipulate the release rates to suit the need of different drugs, we have examined the effect of the phenyl ring substitutions on the release kinetics of such prodrugs and found that appropriately positioned alkyl substituents on the phenyl ring could help to facilitate the release by as much as 16-fold. Therefore, introduction of alkyl substituents on the phenyl ring should allow us to manipulate the release rates and, therefore, time profiles for different drugs.

• 公益社団法人日本薬学会の論文
• 2000-08-01

著者

• BAE Sung

  Department of Materials Science and Engineeing, KAIST

• Bae Sung

  Department Of Chemistry North Carolina State University

• WANG Binghe

  Department of Chemistry, North Carolina State University

• Hendrata Siska

  Department Of Chemistry North Carolina State University

• Wang Binghe

  Department Of Chemistry North Carolina State University

• LIAO Yuan

  Department of Chemistry, North Carolina State University

• Liao Y

  Department Of Chemistry North Carolina State University

• Liao Yuan

  Department Of Chemistry North Carolina State University

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