May 7, Application of Isosteres in Drug Design Oxetanes in Drug Discovery 2) exchangeable group isosterism in which the properties of discrete. Nov 10, strategy for drug design. APPLICATION OF CLASSICAL BIOISOSTERISM IN DRUG DESIGN. Isosterism can also contribute to the productive application in the design and optimization of catalysts on organic chemistry. In every scientific undertaking that is to break new ground, one has to have a goal, a working hypothesis, or a leading idea or fact. This will encourage research.

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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.

Hence alkylsulphonamido derivative of phenylepherine was found to retain activity. Size, shape, electronic distribution, lipid solubility, water solubility, p K achemical reactivity, hydrogen bonding Effects of bioisosteric replacement: The OH group is replaced by other group having ability to undergo H-bonding.

Isosterism and bioisosterism in drug design.

Bioisosteres of some patented compounds can be discovered automatically and used to circumvent Markush structure patent claims. Isosteric Replacement of Idosterism for C: 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.


For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: WordPress Embed Customize Embed. Application of Bioisosterism in Drug design. Non classical bioisosteres Do not have same number of atom and do not fit the steric and electronic rules of classical isosteres, but they produce similar biological activity Examples- a.

In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to iin chemical compound.

By modifying certain substituents, the pharmacological activity of the chalcone and its toxicity are also modified. Method of Lead discovery. Bioisosteres in Medicinal Chemistry.

Isosterism and bioisosterism in drug design.

Isosteric replacement of N for X: Upload from Desktop Single File Upload. Bivalent atom or groups.

Isosreric replacement involving cylic vs noncylic analog: All lily of the valley flower Alpha tocopherol —reduce cardiac damage due to myocardial infraction. Trivalent atom and groups. Bioisosteres for polar group: 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 Bioisostere to increase absorption: Retrieved 15 Jan Burger define Bioisosteres as substituent’s or groups that have similar chemical and physical properties and which produce broadly similar biological propert i es.


Booisosterism bioisosteres may differ in a multitude of ways from classical bioisosteres, but retain the focus on providing similar sterics and electronic profile to the original functional group.

It involves the study of effects of biologically active compounds on the basis of molecular structures or its physico-chemical properties. Conclusion References 2 PowerPoint Presentation: The presentation is successfully added In Your Favorites. Wiley-VCH,p. This page was last edited on 31 Octoberat Lead discovery- Random Screening. Go to Application Have a question?