ISOSTERISM AND BIOISOSTERISM PDF

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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Bioisosteres for polar group: Another example are chalcones bioisosteres. 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.

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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. Silicon Isosteres in Drug Discovery”. However, with a blocked pathway for metabolism, the drug candidate may have a longer half-life.

Drug discovery, Design and modification. 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. To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties.

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BIOISOSTERISM AND ISOSTERISM by S.R. BHALERAO |authorSTREAM

Drug act as a Antihistamine. Retrieved 15 Jan 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 bioisosterlsm in chemical structure.

The main use of this term and its techniques are related to pharmaceutical sciences. Optimization of Lead -Identification of the active part.

Bioisostere – Wikipedia

By using this site, you agree to the Terms of Use and Privacy Policy. Why Lead Modification is Necessary?: Lead discovery- Random Screening. You do not have the permission to view this presentation.

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: Burger define Bioisosteres as substituent’s or groups that have similar chemical and physical properties and which produce broadly similar biological propert i es. Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7.

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

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Bioisostere

bloisosterism Another example is aromatic rings, a phenyl -C 6 H 5 ring can often be replaced by a different aromatic ring such as thiophene or naphthalene which may improve efficacy, change specificity of binding, or reduce metabolically labile sites on the molecule, resulting in better pharmacokinetic properties.

Application of Bioisosterism in Drug design. Conclusion References 2 PowerPoint Presentation: Trivalent atom and groups.

Size, shape, electronic distribution, lipid solubility, water solubility, p K achemical reactivity, hydrogen bonding Effects of bioisosteric replacement: 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 bioisossterism electron structure had similar biological properties.

Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: Retrieved from ” https: Isosteric replacement of S for X: For fine tune of biological activity in order to- -Minimize bioisostrrism -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: Structural size, shape, H-bonding are important 2.