The Future of Prodrugs Design | Chapter 03 | Modern Advances in Pharmaceutical Research Vol. 2

When knowledge fails to provide answers to important questions such as how to improve the bioavailability of vital medications, “Imagination is more important than knowledge,” as Albert Einstein once said. Ingenuity in the design of effective prodrugs has been lacking in quantity and quality. The reasons behind the low quality of ingenuity could be related to the fact that medicinal chemists have expertise in organic and organometalic chemistry not in biochemistry and biology. On the other hand, pharmaceutical chemists, biologists and biochemists do not have the expertise to make sophisticated chemical devices. Therefore, in order for a prodrug strategy to work, a team consisting of all this expertise is necessary.

Author(s) Details

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, Viadell’Ateneo Lucano 10, 85100, Potenza, Italy.

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Prodrugs-Current and Future Drug Development Strategy | Chapter 7 | Modern Advances in Pharmaceutical Research Vol. 1

The  focus  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.

Author(s) Details

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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View Volume: https://doi.org/10.9734/bpi/mapr/v1