prodrugs in cardiovascular therapy高活性化合物在心血管治疗.pdfVIP

Molecules 2008, 13, 1156-1178; DOI: 10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /molecules Review Prodrugs in Cardiovascular Therapy Marinella G. Sandros 1,3, Chady B. Sarraf 4,5 and Maryam Tabrizian 1,2,3,* 1 Department of Biomedical Engineering, McGill University, 3775 University Street, Montreal, QC, Canada H3A2B4 2 Faculty of Dentistry, McGill University, 3640 University Street, Montreal, QC, Canada, H3A 2B2 3 Center for Biorecognition and Biosensors, McGill Institute for Advanced Materials, 3775 University Street, Montreal, QC, Canada H3A2B4 4 Department of Medical Education, Seton Hall University, 400 South Orange Avenue, South Orange, NJ 07079, USA 5 St. Michael’s Medical Center, 111 Central Avenue, Newark, NJ 070102, USA * Author to whom correspondence should be addressed; E-mail: Maryam.tabrizian@mcgill.ca Received: 5 February 2008; in revised form: 14 May 2008 / Accepted: 14 May 2008 / Published: 14 May2008 Abstract: Prodrugs are biologically inactive derivatives of an active drug intended to solve certain problems of the parent drug such as toxicity, instability, minimal solubility and non-targeting capabilities. The majority of drugs for cardiovascular diseases undergo first- pass metabolism, resulting in drug inactivation and generation of toxic metabolites, which makes them appealing targets for prodrug design. Since prodrugs undergo a chemical reaction to form the parent drug once inside the body, this makes them very effective in controlling the release o