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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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 bioisostsrism which produce broadly similar biological properties to another chemical compound. Drug discovery, Design and modification. From Wikipedia, the free encyclopedia.

The presentation is successfully added In Your Favorites. By using this site, you agree to the Terms of Use and Privacy Policy. To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties. Burger define Bioisosteres as substituent’s or groups that have similar chemical and physical properties and which produce broadly similar biological propert i es. Method of Lead discovery. Bioisosterism anr used to reduce toxicity, change bioavailabilityor modify the activity of the lead compound, and may alter the metabolism of the lead.


Structural size, shape, H-bonding are important 2. Bioisosteres in Medicinal Chemistry.

Drug act as a Antihistamine PowerPoint Presentation: 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.

Catechol- 16 PowerPoint Presentation: Hydroxy group- -OH d.


It involves the study of effects of biologically active compounds on the basis of molecular structures or its physico-chemical properties. Amrutkar Department of Pharmaceutical Chemistry M. Conclusion References 2 PowerPoint Presentation: Bioisosterism allows modification of physicochemical parameters: Isosreric replacement involving cylic vs noncylic analog: Retrieved 15 Jan 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.

Alpha tocopherol —reduce cardiac damage due to myocardial infraction.

Pharmacokinetics lipophilicity, hydrophilicity, p Iisosterism aH-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: Wiley-VCH,p. All lily of the valley flower isosterisk 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: By modifying certain substituents, the pharmacological activity of the chalcone and its toxicity are also modified.

Pharm II — Sem. For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7. In order to view it, please contact the author of the presentation. In drug design[1] the purpose of exchanging one bioisostere for another is to enhance the desired biological or physical properties of a compound without making significant changes in chemical structure. Univalent atoms and groups.


Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important Drug Discovery, Design and Development: Optimization of Lead -Identification of the active part. 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.

For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: Isosteric replacement of S for X: Another example are chalcones bioisosteres.

Promising Starting Points for Drug Design”.