Posted on March 21, by mcb An excellent J. The author gives a brief introduction to the concept of biosisosterism classical and non-classical but concentrates on pulling together numerous recent examples which together illustrate the use of bioisosteres to address a diverse range of issues that are commonly encountered in the process of drug discovery. A really nice paper and highly recommended reading material. Isosteres of Hydrogen: Deuterium as an isostere of hydrogen. Deuterium substitution to modulate metabolism. Deuterium substitution to modulate metabolism and toxicity.
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This will encourage research and help in the pursuit of a worth-while objective, be it the enrichment of knowledge or the elaboration of a practical purpose. A medicinal scientist who hopes to find a new biologically active drug will have to be guided by such considerations. This process is experimental and the keywords may be updated as the learning algorithm improves.
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Isosterism and bioisosterism in drug design
Dut All lily of the valley flower Bioisostere increase target interaction and selectivity: Drug Discovery, Design and Development: Bioisosterism is used to reduce toxicity, change bioavailabilityor modify the activity of the lead compound, and may alter the metabolism of the lead. The main use of this term and its techniques are related to pharmaceutical sciences. Because the fluorine atom is similar in size to the hydrogen atom the overall topology of the molecule is not significantly affected, leaving the desired biological activity unaffected. Bivalent atom or groups. Structural size, shape, H-bonding are important 2. Alferrd Burger Bioisosteric Replacement. Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: Alpha tocopherol —reduce cardiac damage due to myocardial infraction.
Isosterism and bioisosterism in drug design.
This will encourage research and help in the pursuit of a worth-while objective, be it the enrichment of knowledge or the elaboration of a practical purpose. A medicinal scientist who hopes to find a new biologically active drug will have to be guided by such considerations. This process is experimental and the keywords may be updated as the learning algorithm improves. This is a preview of subscription content, log in to check access. Preview Unable to display preview. Download preview PDF.
ISOSTERISM AND BIOISOSTERISM IN DRUG DESIGN PDF
Bioisosterism: A Useful Strategy for Molecular Modification and Drug Design