The accumulation of knowledge on
intramolecular processes, enzymes and transporters along with the vast progress
in molecular revolution have accelerated the search for prodrugs having the
capability to replace their corresponding current marketed drugs and to provide
therapeutics with better pharmacological profiles. Utilizing the different
available computational methods has led to the design and synthesis of a
variety of prodrugs to replace their corresponding parent drugs.
It has been proven that prodrugs can significantly improve the life quality of patients.
The directed enzyme prodrug therapy (DEPT) approach to employ the design of artificial enzymes to activate prodrugs at specific sites along with use of intramolecular processes to design prodrugs are the most attractive strategies to obtain more efficient therapeutics.
Professor Rafik Karaman
Department of Bioorganic Chemistry, Faculty of Pharmacy, Al-Quds University, P.O.Box 20002, Jerusalem, Palestine and Department of Sciences, University of Basilicata, Via dell’ateneo Lucano 10, 85100, Potenza, Italy.
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of traditional prodrug
approach was on
altering various physiochemical parameters, whereas the current modern computational
approach considers designing prodrugs through attaching appropriate linkers
with drugs having
poor bioavailability which
upon exposure to
physiological environments release the parent active drugs in a
programmable (controlled) manner resulting in an improvement of their
bioavailability. With the possibility of designing prodrugs with different
linkers, the release rate of the parent active drugs can be controlled. The
future of prodrug technology
is exciting and
yet challenging. Advances must be
made in understanding the chemistry of many organic reactions that can be
effectively utilized to enable the development of more types of prodrugs. The
understanding of organic reaction mechanisms of certain processes, particularly
intramolecular reactions, will be the next major milestone in this field. It is
envisioned that the future of prodrug technology holds the ability
to create safe and
efficacious delivery of a wide range of active small molecules and
biotherapeutics. This goal can be achieved using computational chemistry
methods such as ab initio, semi-empirical and density functional theory (DFT),
and molecular mechanics (MM) to calculate physicochemical and molecular properties of current marketed drugs suffer
low bioavailability or/and unpleasant taste or odor.
Professor Rafik Karaman
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Quds
University, P.O. Box 20002, Jerusalem, Palestine and Department of Science,
University of Basilicata, Potenza, Italy.
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