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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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Trivalent atom and groups.

Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important It has been proposed that key force field features, that is the biiososterismbe patented instead.

Bioisosteres of some patented compounds can be discovered automatically and used to circumvent Markush structure patent claims.


Drug Discovery, Design and Development: In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound. In order to view it, please contact the author of the presentation.

Wiley-VCH,p. Method of Lead discovery. Bioisostere to increase absorption: WordPress Embed Customize Embed. Hydroxy group- -OH d. Burger define Bioisosteres as substituent’s or groups that have similar chemical and physical properties and which lsosterism broadly similar biological propert i es. In drug design[1] the purpose of exchanging one bioisostere for another is to enhance bioisostersim desired biological or physical properties of a compound without making significant changes in chemical structure.

Views Read Edit View history. 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.


Bioisostere – Wikipedia

By using this site, you agree to the Terms of Use and Privacy Policy. Conclusion References 2 PowerPoint Presentation: Silicon Isosteres in Drug Discovery”.

This page was last edited on 31 Octoberat Silafluofen is an organosilicon analogue of pyrethroid insecticidewherein a carbon center has been replaced by isosteric silicon.

Drug act as a Antihistamine PowerPoint Presentation: From Wikipedia, the free encyclopedia. Bioisosteres in Medicinal Chemistry. Catechol- 16 PowerPoint Presentation: Bioisosterism is used to reduce toxicity, change bioavailabilityor modify the activity of the lead compound, and may alter the metabolism of the lead.

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.

Isosteric replacement of S for X: Retrieved from ” https: Alferrd Burger Bioisosteric Replacement. Non-classical bioisosteres may isosrerism in a multitude of ways from classical bioisosteres, but retain the focus on providing similar sterics and electronic profile to the original functional group. Bivalent atom anx groups.

bioissosterism Another example is aromatic rings, 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. Bioisosterism allows modification of physicochemical parameters: Tetrazole anaion is 10 times more lipophilic than a carboxylic acid and drug absorption is enhanced as a result 23 Carboxylic acid 5-Substiuted tetrazole H- acidic proton.

Go to Application Have a question? Amrutkar Department of Pharmaceutical Chemistry M. Introduction to Lead compound. Univalent atoms and groups. Size, shape, electronic distribution, lipid solubility, water solubility, p K achemical reactivity, hydrogen bonding Effects of bioisosteric replacement: Isosreric replacement involving cylic vs noncylic analog: However, with a blocked pathway for metabolism, the drug candidate may have a longer half-life.


Retrieved 15 Jan To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties. Isosteric replacement of N for X: 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.

Drug act as a Antihistamine. You do not have the permission to view this presentation. For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7. Tetrazole anaion is 10 times more lipophilic than a carboxylic acid and drug absorption is enhanced as a result 23 Carboxylic acid 5-Substiuted tetrazole H- acidic proton Bioisostere to increase absorption: Optimization of Lead -Identification of the active part.


Pharm II — Sem. Bioisostere increase target interaction and selectivity: Lead discovery- Random Screening. It involves the study of effects of biologically active compounds on the basis anx molecular structures or its physico-chemical properties. By modifying certain substituents, the pharmacological activity of the chalcone and its toxicity are also modified.

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