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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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. Non classical bioisosteres Do not have same bioksosterism of atom and do not fit the steric and electronic rules of classical isosteres, but they produce similar biological activity Examples- a.

bioisksterism WordPress Embed Customize Embed. All lily of the valley flower Upload from Desktop Single File Upload. 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.

Trivalent atom and groups.

Isosterism and bioisosterism in drug design.

Isosteric replacement of N for X: By using this site, you agree to the Terms of Use and Privacy Policy. Conclusion References 2 PowerPoint Presentation: Optimization of Lead -Identification of the active part. Silicon Isosteres in Drug Discovery”.


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.

Bioisosteres for polar group: From Wikipedia, the free encyclopedia. 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. Bioisosteres in Medicinal Chemistry.

Bioisostere – Wikipedia

Drug act as a Antihistamine. Isosteric Replacement of Si for C: Drug act as a Antihistamine PowerPoint Presentation: Another example are chalcones bioisosteres. Promising Starting Points for Drug Design”.

bioisostrism For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: Bivalent atom or groups. Isosteric replacement of S for X: Why Lead Modification is Necessary?: Isosreric replacement involving cylic vs noncylic analog: Bioisosteres of some patented compounds can be discovered automatically and used to circumvent Markush structure patent claims.

Catechol- 16 PowerPoint Presentation: Structural size, shape, H-bonding are important 2. The OH group is replaced by other group having ability to undergo H-bonding.


Bioisostere increase target interaction and selectivity: To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties.


Drug discovery, Design and modification. By modifying certain substituents, the pharmacological activity of the chalcone and its toxicity are also modified. Bioisosterism is used to reduce toxicity, change bioavailabilityor modify the activity of the lead compound, and may alter the metabolism of the lead. Lead discovery- Random Screening.

Automatically changes to Flash or non-Flash embed. Method of Lead discovery. The presentation is successfully added In Your Favorites. 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 desivn functional group for a cyclic moiety, an drugg group for a complex heteroatom moiety, isostrism other changes that go far beyond a simple atom-for-atom switch.

All lily of the valley flower 13 Why Bioisosterism? For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism bioisotserism bioavailability 7.

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