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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You do not have the permission to view this presentation. All lily of the valley flower 13 Why Bioisosterism?

Retrieved 15 Jan Alferrd Burger Bioisosteric Replacement. Conclusion References 2 PowerPoint Presentation: This page was last edited on 31 Octoberat Optimization of Lead -Identification of the active part.


Replacement of Bioisosteriism by Chlorine: Bioisosteres in Medicinal Chemistry. Silafluofen is an organosilicon analogue of pyrethroid insecticidewherein a carbon center has been replaced by isosteric silicon. It has been proposed that key force field features, that is the pharmacophorebe patented instead. In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound.


Bioisostere – Wikipedia

Drug Discovery, Design and Development: Introduction to Lead compound. Bioisostere to increase absorption: For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: Method of Lead discovery.

Wiley-VCH,p. Retrieved from ” https: Application of Bioisosterism in Drug design.

Go to Application Have a question? However, with a blocked pathway for metabolism, the drug candidate may have a longer half-life. Hydroxy group- -OH d. Tetrazole anaion is 10 times more lipophilic than a carboxylic acid and drug absorption is enhanced snd a result 23 Carboxylic acid 5-Substiuted tetrazole H- acidic proton Bioisostere to increase absorption: Trivalent atom and groups.


To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties. Catechol- 16 PowerPoint Presentation: For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7.

Boiisosterism lipophilicity, hydrophilicity, p K aH-bonding are important 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.


Bivalent atom or groups.

The OH group is replaced by other group having ability to undergo H-bonding. Drug act as a Antihistamine PowerPoint Presentation: Hence alkylsulphonamido derivative of phenylepherine was found to retain activity.

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.

Bioisosteres for polar group: Promising Starting Points for Drug Design”. By using this site, you agree to the Terms abd Use and Privacy Policy.

Isosteric Replacement of Si for C: Size, shape, electronic distribution, lipid solubility, water solubility, p K achemical reactivity, hydrogen bonding Effects of bioisosteric replacement: Automatically changes to Flash or non-Flash embed.