Journal
CHEMMEDCHEM
Volume 11, Issue 12, Pages 1197-1198Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201500406
Keywords
active metabolites; designed multiple ligands (DMLs); drug design; metabolism-activated multitargeting (MAMUT); synergism
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Multitargeting is a valuable concept in drug design for the development of effective drugs for the treatment of multifactorial diseases. This concept has most frequently been realized by incorporating two or more pharmacophores into a single hybrid molecule. Many such hybrids, due to the increased molecular size, exhibit unfavorable physicochemical properties leading to adverse effects and/or an inappropriate ADME (absorption, distribution, metabolism, and excretion) profile. To avoid this limitation and achieve additional therapeutic benefits, here we describe a novel multitargeting strategy based on the synergistic effects of a parent drug and its active metabolite(s). The concept of metabolism-activated multitargeting (MAMUT) is illustrated using a number of examples.
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