Recent Effective Application of Bioisosterism
A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (31 January 2021)
Special Issue Editors
Interests: bioisosterism; hydroxyazoles; hit to lead; drug design; DHODH inhibitors; leukaemia; prostate cancer; GABAerigic and glutaminergic neurotransmissions
Interests: medicinal chemistry; drug discovery; chemical synthesis; PROTAC; anticancer agents; cancer metabolism; endocannabinoid system
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Special Issue Information
Dear Colleagues,
Since the introduction of the term “bioisostere” in 1950 by Harris Friedman, the application of bioisosterism has become a fundamental tactical approach in the contemporary practice of medicinal chemistry. During hit-to-lead processes, bioisosterism is often the winning approach to improve potency and selectivity, achieve optimal ADME-T profiles, and acquire novel intellectual properties. In some instances, the eternal confrontation between the definitions of Isostere and Bioisostere well represents the real soul of a medicinal chemist. Isosteres represent the connection with chemistry, being groups describable by chemico-physical parameters. On the contrary, the possibility of applying the bioisosteric definition to an isostere will depend on the biological context, an often brutal remind of how difficult the translation of a chemistry-based design into a living organism activity can be. Since a bioisostere found to be effective for a biochemical application cannot be translated to another setting, the effective application of a bioisosteric approach needs a continuous refinement of its isosteric counterpart, sharpening the tool by introducing structural changes in size, shape, electronic distribution, polarizability, dipole, polarity, lipophilicity (logP), and pKa. All these variables can potentially play a role, in a beneficial or deleterious way, in effectively reaching a bioisosteric definition.
Authors are invited to submit original and review articles describing basic science, preclinical, and clinical findings, that contribute to the understanding of the current and future potential applications of bioisosterism, to be published in this Special Issue of Pharmaceuticals.
Dr. Marco L. Lolli
Dr. Carlotta Granchi
Guest Editors
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Keywords
- Bioisosterism
- Scaffold hopping
- Drug design
- Hit to lead
- Heterocycles
- Chemico-physical descriptors
- Structure-based design
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