Chemical groups which can be substituted to enhance therapeutic activity of drugs
In medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties in the same chemical compound.[1] In drug design,[2] the purpose of exchanging one bioisostere for another is to enhance the desired biological or physical properties of a compound without making significant changes in chemical structure. The main use of this term and its techniques are related to pharmaceutical sciences. Bioisosterism is used to reduce toxicity, change bioavailability, or modify the activity of the lead compound, and may alter the metabolism of the lead.
^IUPAC, Compendium of Chemical Terminology, 2nd ed. (the "Gold Book") (1997). Online corrected version: (1998) "bioisostere". doi:10.1351/goldbook.BT06798
^Nathan Brown. Bioisosteres in Medicinal Chemistry. Wiley-VCH, 2012, p. 237. ISBN 978-3-527-33015-7
In medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological...
compounds containing an isostere is called a bioisostere. This is frequently used in drug design: the bioisostere will still be recognized and accepted by...
in place of one hydrogen atom at the C9α position. Fluorine is a good bioisostere for hydrogen because it is similar in size, with the major difference...
same degree as in synthetic areas.) Chemistry portal Science portal Bioisostere Biological machines Chemoproteomics Drug design Pharmacognosy Pharmacokinetics...
a tetrazole which is being used in place of the carboxylic acid as a bioisostere. Losartan is used for hypertension, including in people with left ventricular...
as alpha-methyldopamine, it was hoped that the difluoromethylenedioxy bioisostere would show increased metabolic stability and less toxicity. These compounds...
agent of the racetam family. It contains a chemical group that is a bioisostere of the 9-amino-tetrahydroacridine family. It was initially developed...
This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemical compound from (often the starting point...
Where melatonin has an indole ring system, agomelatine has a naphthalene bioisostere instead. Agomelatine was discovered and developed by the European pharmaceutical...
small size of fluorine is convenient as fluorine acts as an approximate bioisostere of the hydrogen. Introducing the carbon–fluorine bond to organic compounds...
intense in the mid-1940s. The trifluoromethyl group is often used as a bioisostere to create derivatives by replacing a chloride or a methyl group. This...
nature of rational drug design suppresses serendipity in drug discovery. Bioisostere Bioinformatics Cheminformatics Drug development Drug discovery List of...
biochemistry and medicinal chemistry, phosphonate groups are used as stable bioisosteres for phosphate, such as in the antiviral nucleotide analog, Tenofovir...
including several cephalosporin-class antibiotics. Tetrazoles can act as bioisosteres for carboxylate groups because they have similar pKa and are deprotonated...
MacMillan, David W. C. (June 2023). "General access to cubanes as benzene bioisosteres". Nature. 618 (7965): 513–518. doi:10.1038/s41586-023-06021-8. ISSN 1476-4687...
useful for synthesis to derive bicyclo[1.1.1]pentane which are used a bioisosteres for para-substituted arene systems. [2.1.1]Propellane, C6H8, CAS number...
selective dopaminergics incorporating enyne units as nonaromatic catechol bioisosteres: synthesis, bioactivity, and mutagenesis studies". Journal of Medicinal...
Meanwell NA (April 2011). "Synopsis of some recent tactical application of bioisosteres in drug design". Journal of Medicinal Chemistry. 54 (8): 2529–2591. doi:10...
quinonoids, electrophiles, sulfonylated aminothiazoles and phosphate bioisosteres. Although some progress has been made in developing potent and selective...
via the use of 3-cyclobutene-1,2-dione as an achiral alpha-amino acid bioisostere". Journal of Medicinal Chemistry. 41 (2): 236–46. doi:10.1021/jm970504g...
Global Information