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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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Isosterism and bioisosterism in drug design.

Replacement of Methyl by Chlorine: 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.

Drug act as a Antihistamine. Pharm Bioisosterksm — Sem. Bioisosterism allows modification of physicochemical parameters: 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. Bivalent atom or groups. Isosteric Replacement of Si for C: 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.

Retrieved from ” https: Pharmacokinetics lipophilicity, hydrophilicity, p K a bioiisosterism, H-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: Structural size, shape, H-bonding are important 2.

Drug Discovery, Design and Development: For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7. Why Lead Modification is Necessary?: By using this site, you agree to the Terms of Use and Privacy Policy. In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound.


Conclusion References 2 PowerPoint Presentation: Amrutkar Department of Pharmaceutical Chemistry M. You do not have the permission to view this presentation. Isosreric replacement involving cylic vs noncylic analog: Bioisostere increase target interaction and selectivity: Catechol- 16 PowerPoint Presentation: By modifying certain substituents, the pharmacological activity of the chalcone and its toxicity are also modified. Alferrd Burger Bioisosteric Replacement.

To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties. It has been proposed that key force field features, that is the pharmacophorebe patented instead.

Alpha tocopherol —reduce cardiac damage due to myocardial infraction. From Wikipedia, the free encyclopedia. Application of Bioisosterism in Drug design. Upload from Desktop Single File Upload. Lead discovery- Random Screening.

Bioisosteres for polar group: Introduction to Lead compound. The main use of this term and its techniques are related to pharmaceutical sciences. This page was last edited on 31 Octoberat The presentation is successfully added In Your Favorites. Wiley-VCH,p. In order to view it, please contact the author of the presentation.

Bioisostere – Wikipedia

It involves the study of effects of biologically active compounds on the basis of molecular structures or its physico-chemical properties. Whereas classical bioisosteres commonly conserve much of the same structural properties, nonclassical bioisosteres are much more dependent on the isosteerism binding needs of the ligand in question and may substitute a linear functional group for a cyclic moiety, xrug alkyl group for a complex heteroatom moiety, or other changes that go far beyond a simple atom-for-atom switch.


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.

Isosteric replacement of S for X: Bioisostere to increase absorption: 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. Hydroxy group- -OH d. 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: WordPress Embed Customize Embed.


For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: Non-classical 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.

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Retrieved 15 Jan However, with a blocked pathway for metabolism, the drug candidate may have isosterim longer half-life. Promising Starting Points for Drug Design”.