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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WordPress Embed Customize Embed. Pharm II — Sem. Amrutkar Department of Pharmaceutical Chemistry M. Drug discovery, Design and modification. Introduction to Lead compound.
BIOISOSTERISM AND ISOSTERISM by S.R. BHALERAO |authorSTREAM
Method of Lead discovery. Application of Bioisosterism in Drug design. Conclusion Bioisosteridm 2 PowerPoint Presentation: It involves the study of effects of biologically active compounds on the basis of molecular structures or its physico-chemical properties.
Lead discovery- Random Screening. 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. 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 PowerPoint Presentation: Burger define Bioisosteres as substituent’s or groups that have similar chemical and physical properties and which produce broadly similar biological propert i es.
Alferrd Burger Boiisosterism Replacement. All lily of the valley flower 13 Why Bioisosterism? Univalent atoms and groups. Bivalent atom or groups.
Trivalent atom and groups. Non classical bioisosteres Do not have same number of hioisosterism and do not fit the steric and electronic rules of classical isosteres, but they produce similar biological activity Examples- a.
Hydroxy group- -OH d. Catechol- 16 PowerPoint Presentation: Size, shape, electronic distribution, lipid solubility, water solubility, p K achemical reactivity, hydrogen bonding Effects of bioisosteric replacement: Structural size, shape, H-bonding are important 2.
Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important 17 Bioisosterism allows modification of physicochemical parameters: The OH group is replaced by other group having ability to undergo H-bonding. Hence alkylsulphonamido derivative of phenylepherine was found to retain activity. Bioisostere increase target interaction and selectivity: Bioisosteres for polar group: To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties.
Tetrazole anaion is 10 times bioisosteerism 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: Alpha tocopherol —reduce cardiac damage due to myocardial infraction. Drug act as a Antihistamine PowerPoint Presentation: Upload from Desktop Single File Upload.
The presentation is successfully added In Your Favorites. Drug Discovery, Design and Development: Why Lead Modification is Necessary?: For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7. All lily of the valley flower Pharmacokinetics lipophilicity, hydrophilicity, p K aH-bonding are important 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: Replacement of Methyl by Chlorine: Isosteric replacement of N for X: Isosteric replacement of S for X: Isosteric Replacement of Si for C: Isosreric replacement involving cylic vs noncylic analog: Drug act as a Antihistamine. You do not have the permission to view this presentation. In order to view it, please contact the author of the presentation.
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