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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To overcome this problem, replacement of carboxylic acid with bioisostere which has similar physicochemical properties.
anv Trivalent atom and groups. The presentation is successfully added In Your Favorites. You do not have the permission to view this presentation. Why Lead Modification is Necessary?: For fine tune of biological activity in order to- -Minimize toxicity -Modify the activity -Alter metabolism -Maximize bioavailability 7 PowerPoint Presentation: Go to Application Have a question?
BIOISOSTERISM AND ISOSTERISM by S.R. BHALERAO |authorSTREAM
iwosterism Upload from Desktop Single File Upload. Retrieved from ” https: In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound. Hydroxy group- -OH d. Structural size, shape, H-bonding are important 2. Burger define Bioisosteres as substituent’s or groups that have similar chemical and physical properties and which produce broadly similar biological propert i es.
However, with a blocked pathway for metabolism, the drug candidate may have a longer half-life.
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. All lily of the valley flower Replacement of Methyl by Chlorine: 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 – Wikipedia
Drug act as a Isostfrism. WordPress Embed Customize Embed. The main use of this term and its techniques are related to pharmaceutical sciences. Alferrd Burger Bioisosteric Replacement. Automatically changes to Flash or non-Flash embed.
Optimization of Lead -Identification of the active part. Isosteric Replacement of Si for C: It involves the study of effects of biologically active compounds on the basis of molecular structures or its physico-chemical properties.
It has been proposed that key force field features, that is the pharmacophorebe patented instead. 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 N for X: Bioisosteres in Medicinal Chemistry. 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.
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.