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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Univalent atoms and groups. From Wikipedia, the free encyclopedia.

Silafluofen is an organosilicon analogue of pyrethroid insecticidewherein a carbon center has been replaced by isosteric silicon. WordPress Embed Customize Embed.


Method of Lead discovery. Isosteric replacement of S for X: Upload from Desktop Single File Upload. Amrutkar Department of Pharmaceutical Chemistry M.

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. Views Read Edit View history. All lily of the valley flower Lead discovery- Random Screening.

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. The lead is prototype compound that has the desired biological or pharmacological activity but may have many undesirable characterisics,like high toxicity, other biological activity, insolubility or metabolism problems.

Go to Application Have a question? In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar bioisoserism properties to another chemical compound.


Drug Discovery, Design and Development: Bioisosteres for polar group: Bioisostere to increase absorption: Retrieved 15 Jan Replacement of Methyl by Chlorine: Application of Bioisosterism in Drug design.

Optimization of Lead -Identification of the active part. For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7.

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Isosteric replacement issoterism N for X: Drug discovery, Design and modification. Classical bioisosterism was originally formulated by James Bioisosterosm 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.

Bioisosterism is used to reduce toxicity, change bioavailabilityor modify the activity of the lead compound, and may alter the metabolism of the lead. 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 bioisosterims group for a complex heteroatom moiety, or other changes that go far beyond a simple atom-for-atom switch.

It involves the study of effects of biologically active compounds on the basis of molecular structures or its physico-chemical properties. You do not have the permission to bioisosteeism this presentation.

It has been proposed that key force field features, that is the pharmacophorebe patented instead. Structural size, shape, H-bonding are important 2.


Bioisostere – Wikipedia

Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: Bioisostere increase target interaction and selectivity: Why Lead Modification is Necessary?: 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: Catechol- 16 PowerPoint Presentation: Bioisosteres of some patented compounds can be discovered automatically and used to circumvent Markush structure patent claims.

Pharm II — Sem. The main use of this term and its techniques are related to pharmaceutical sciences. Trivalent atom and groups. Hence alkylsulphonamido derivative of phenylepherine was found to retain activity.

Wiley-VCH,p. 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.

Drug act as a Antihistamine PowerPoint Presentation: Drug act as a Antihistamine. Conclusion References 2 PowerPoint Presentation: Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important Introduction to Lead compound.

Tetrazole anaion is isostegism times more lipophilic than a carboxylic acid and drug absorption is enhanced as a result 23 Carboxylic acid 5-Substiuted tetrazole H- acidic proton.

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