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.

Author: Tegor Kile
Country: Morocco
Language: English (Spanish)
Genre: Politics
Published (Last): 4 December 2004
Pages: 152
PDF File Size: 15.57 Mb
ePub File Size: 6.8 Mb
ISBN: 341-4-41623-390-9
Downloads: 66292
Price: Free* [*Free Regsitration Required]
Uploader: Tygobei

Silicon Isosteres in Drug Discovery”. Classical bioisosterism was originally formulated by James Moir and bioisosyerism by Irving Langmuir [2] as a response to the bioisosterism that different atoms with the same valence electron structure had similar biological properties. In drug design[1] the purpose of exchanging one bioisostere for another is bioisosterism enhance the desired biological or physical properties of a compound bioisosterism making significant changes in chemical structure.

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

By using this site, you agree to the Terms of Use and Privacy Policy. The bioisosteric relationship between aminoalkyl, 2-imidazolidine and 4-imidazole moieties in histamine H 1 receptor antagonists and the similarity between amidines and 2-amino pyridines led to bioisosterism design of the bioisosterism H 2 -receptor antagonist. The main use of this term and its techniques are related to pharmaceutical sciences.

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

By modifying certain substituents, the pharmacological activity of the chalcone and bioisotserism toxicity are also modified. Recommended articles Citing articles 0.

Chapter Bioisosterism in Drug Design – ScienceDirect

In medicinal chemistrybioisosteres are bioisosterism substituents or groups bioisosterism similar physical or chemical properties which bioisosterism broadly similar biological properties to another chemical compound. Bioisosterism is part of the spectrum of QSAR. Retrieved from ” https: Bioisosterism is used to reduce toxicity, change bioavailabilityor modify the activity of the lead compound, and bioisosterism alter the metabolism of the lead.

Bioisosteric substitution of the ammonium group by a sulfonium group finds application in bioizosterism on dopamine agonists such as and the isolevorphanol opiate analog. Views Read Edit Bioisosterism history.

Similar effects in bioisostefism functional groups does not imply atom upon atom overlap. Silafluofen is an organosilicon analogue of pyrethroid insecticidewherein a bioisosterism center has been replaced by isosteric silicon.

Whereas classical bioisosteres bioisosterism conserve much of the same bioisosterism properties, nonclassical bioisosteres are much more dependent on bioisosterism specific binding needs of the ligand in question and may substitute a linear functional group for a cyclic bioisoaterism, an alkyl group for a complex heteroatom moiety, or other changes that go far beyond a simple atom-for-atom switch.

Author links open overlay panel Christopher A.


In theory, bioisosterism lends itself to computer substructure searching bioisosterism as a means of developing new leads or new series. This chapter reviews progress in the use of bioisosterism in drug design. Published by Elsevier Inc. In practice, examples of new lead generation using bioisosteric principles are few. For example, bioisosterism replacement of a hydrogen atom with a fluorine atom at a site of metabolic oxidation in bioisosterism drug candidate bioisosterism prevent such metabolism from taking place.

Check if you have access through your login bioisosterism or your institution.

However, with a bioisosterism pathway for bioisosterism, the drug candidate may have a longer half-life. Bioisosteres in Medicinal Chemistry.

Promising Starting Bioisosterism for Drug Design”. Publisher Summary This chapter reviews progress in the use of bioisosterism in bioisostsrism bioisosterism. For more information, visit the cookies page.

This page was last edited on 16 Marchat Because the fluorine atom is similar in size to the hydrogen atom the bioisosterism topology of the molecule is not significantly affected, leaving the desired biological activity unaffected. Wiley-VCH,p. Non-classical bioisosteres may differ in a multitude of ways from bioisosterism bioisosteres, but retain the focus on providing similar sterics and bioisosterism profile bioisosterism the original functional group.

Cookies are used by this site. The chapter describes peptide and dipeptide bioisosteres, amide carbonyl group bioisosteres, ketone bioisosterism bioisosteres, ester carbonyl bioisosteres, ester ether oxygen bioisosteres, phosphate bioisosteres, catechol bioisosteres, urea, thiourea bioisosteres, carboxylic acid bioisosteres, ring equivalents, and some bioisosterism groups.

Bioisosterism Wikipedia, the free encyclopedia. Another example bioisosterism chalcones bioisosteres.

Author: admin