Isosterism and Bioisosterism – Download as PDF File .pdf), Text File .txt) or read online. Pharmacology. Download Citation on ResearchGate | Isosterism and bioisosterism in drug design | In every scientific undertaking that is to break new ground, one has to have a. Aug 1, Isosterism and bioisosterism in drug design. By Alfred Burger. University of Virginia, Department of Chemistry,. Charlottesville, Virgina

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The main use of this term and its techniques are related to pharmaceutical sciences. In drug design[1] the purpose of exchanging one bioisostere for another is to enhance the desired biological or physical properties isosgerism a compound without making significant changes in chemical structure. It has been proposed that key force field features, that is the pharmacophorebe patented instead.

Another example is aromatic isoaterism, a phenyl -C 6 H 5 ring can often be replaced by a different aromatic ring such as thiophene or naphthalene which may improve efficacy, change specificity of binding, or reduce metabolically labile sites on the molecule, resulting in better pharmacokinetic properties. Why Lead Modification is Necessary?: You do not have the permission to view this presentation.


Drug act as a Antihistamine PowerPoint Presentation: Bioisostere increase target interaction and selectivity: Replacement of Methyl by Chlorine: Bivalent atom or groups. 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.



Bioisosterism allows modification of physicochemical parameters: The lead is prototype compound that has the desired isosteris or pharmacological activity but may have many undesirable characterisics,like high toxicity, other biological activity, insolubility or metabolism problems. All lily of the valley flower 13 Why Bioisosterism?

Optimization of Lead -Identification of the active part.

Wiley-VCH,p. Automatically changes to Flash or non-Flash embed. Isosteric Replacement of Si for C: However, with a blocked pathway for metabolism, the drug candidate may have a longer half-life. Whereas classical bioisosteres commonly conserve much of the same structural properties, nonclassical bioisosteres are much more dependent on the specific binding needs of the ligand in question and may substitute a linear functional group for a cyclic moiety, an alkyl group for a complex heteroatom moiety, or other changes that go far beyond a simple atom-for-atom switch.

Upload from Desktop Single File Upload. Application of Bioisosterism in Drug design.

All lily of the valley flower WordPress Embed Customize Embed. Classical bioisosterism was originally formulated by James Moir and refined by Irving Langmuir [2] as a response to the observation that different atoms with the same valence electron structure had similar biological properties.


Hence alkylsulphonamido derivative of phenylepherine was found to retain activity. Catechol- 16 PowerPoint Presentation: The OH group is replaced by other group having ability to undergo H-bonding. Conclusion References 2 PowerPoint Presentation: Drug act as a Antihistamine. Retrieved from ” https: Alpha tocopherol —reduce cardiac damage due to myocardial an. Views Read Edit View history. Another example are chalcones bioisosteres.


Silicon Isosteres in Drug Discovery”. For example, the replacement of a hydrogen atom with a fluorine atom at a site of metabolic oxidation in a drug candidate may prevent such metabolism from taking place. For fine tune of biological activity in order to- -Minimize toxicity -Modify the isostegism -Alter metabolism -Maximize bioavailability 7.

Trivalent atom and groups. By using this site, you agree to the Terms of Use and Privacy Policy. This page was last edited on 31 Octoberat Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: Hydroxy group- -OH d.