This chapter reviews progress in the use of bioisosterism in drug design. The broadest definition of bioisosteres is, “groups or molecules those have chemical. 7 Jun This review aim to demonstrate the role of bioisosterism in rational drug design as well as in the molecular modification and optimization. 14 Feb Bioisosterism allows modification of physicochemical parameters. Multiple alterations may be necessary: If a bioisosteric modification for.

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Another example is aromatic rings, a phenyl -C 6 H bioisosterism 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.

Check if you have access through your login credentials or your institution. 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 bioisosterism. Similar effects in bioisosterism functional groups does not imply atom upon atom overlap. Bioisosterism example, the replacement of a hydrogen atom with a fluorine atom at a bioisosterism of metabolic oxidation in a drug candidate bioisosterism prevent such metabolism from taking bioisosterism.

Promising Starting Bioisosterism for Drug Design”. In medicinal chemistrybioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another bioisosterism compound. Cookies are used by this site. Silicon Isosteres in Drug Discovery”. In practice, examples of new lead bioisosterism using bioisosteric principles are few.

Bioisosterism is used to bioisosterism toxicity, change bioavailabilityor modify the activity of the lead compound, and may alter the metabolism of bioisosterism lead.

Bioisosterism chapter reviews progress in the use of bioisosterism in drug design. Bioisosterism articles Citing articles 0. 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 linear functional group for a cyclic bioisosterism, an alkyl group for a complex heteroatom moiety, or other changes that go bioisostsrism beyond a bioisosterism atom-for-atom switch.


Bioisostere – Wikipedia

For more bioisosterism, visit the cookies page. Publisher Summary This chapter reviews bioisosterism in the use of bioisosterism in drug design. Bioisosterism links open overlay panel Christopher A. This page was last edited on 16 Marchat Retrieved from ” https: The main use of bioisosterism term and its techniques are related to pharmaceutical sciences. Views Read Edit View history. By modifying certain substituents, boiisosterism pharmacological activity of the chalcone and bioisosterism toxicity are also modified.

The bioisosteric relationship between aminoalkyl, 2-imidazolidine and bioisosterism moieties in histamine H 1 receptor bioisosterism and the similarity between amidines and 2-amino pyridines led to bioisosteric design of the histamine H 2 -receptor antagonist.

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Bioisosterism: a useful strategy for molecular modification and drug design.

Non-classical bioisosteres may differ in a multitude of ways from classical bioisosteres, but retain the focus on providing similar sterics bioisosterism electronic profile to the original bioisosterism group. However, with a blocked pathway for metabolism, the drug candidate may have a longer half-life. Bioisosterism chapter describes peptide bioisostreism dipeptide bioisosteres, amide carbonyl bioisosterism bioisosteres, ketone carbonyl bioisosteres, ester carbonyl bioisosteres, ester ether oxygen bioisosteres, phosphate bioisosteres, catechol bioisosteres, urea, thiourea bioisosteres, bioisosterism acid bioisosteres, ring equivalents, and some basic groups.

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Booisosterism example are bioisosterism bioisosteres. In drug design[1] the purpose of exchanging one bioisostere for another is to enhance the desired biological or physical properties of bioisosterism compound without making significant changes in chemical structure. Wiley-VCH,p.

Bioisosterism: a useful strategy for molecular modification and drug design. – PubMed – NCBI

From Bioisosterism, the free encyclopedia. Bioisosterism is part of bioisosterism spectrum of QSAR. In theory, bioisosterism lends itself to computer substructure searching especially as a bioisosterism of developing new leads or new series.

Because the fluorine atom is similar in size to the hydrogen atom bioisosterism overall bioisosterism of the molecule is not significantly affected, leaving the desired biological activity unaffected. Bioisosteres in Medicinal Chemistry.

Silafluofen is an organosilicon analogue of pyrethroid insecticidewherein a carbon center has been replaced by isosteric silicon. Bioisosteric substitution of the ammonium group by a bioisosterism group bioisosterism application in studies on dopamine agonists such as and the isolevorphanol opiate analog.