What are the types of Bioisoster?
What are the types of Bioisoster?
Bioisosteres are classified into the following two types: Classical bioisosteres. Nonclassical bioisosteres.
What is a classical isostere?
Classical Isosteres are molecules or ions with similar shape and often electronic properties. Many definitions are available. but the term is usually employed in the context of bioactivity and drug development. Such biologically-active compounds containing an isostere is called a bioisostere.
How do you identify bioisosteres?
Application of Molecular Fields to Bioisostere Finding The principle behind fragment replacement methods to identify bioisosteres is simple: remove a portion of an active molecule, search a fragment database for a replacement moiety that will physically fit into the vacated space, and score the replacement for …
What is bioisosterism give example?
Another example is aromatic rings, a phenyl -C6H5 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.
What is Bioisosterism give example?
Which pairs are isosteres?
Isosters are molecules or ions that have a similar shape and often have similar electronic properties. CO2 and N2O can form set of isosters.
Which of the following is isosteres with CO2?
N2O5
Which is an isostere of CH2 / O in PGI2?
CH2/O isosterism in non-prostanoid PGI2 mimetics. Silicon as an isostere of carbon. Silicon in p38α MAP kinase inhibitors. Silicon as a carbon isostere in biogenic amine reuptake inhibitors. Silicon as a carbon isostere in haloperidol.
How are bioisosteres used in the design of drugs?
CH2, O, and S isosterism. CH2/O isosterism in PGI2 mimetics. CH2/O isosterism in non-prostanoid PGI2 mimetics. Silicon as an isostere of carbon. Silicon in p38α MAP kinase inhibitors. Silicon as a carbon isostere in biogenic amine reuptake inhibitors.
Which is an isosterism used in PGI2 mimetics?
CH2/O isosterism in PGI2 mimetics. CH2/O isosterism in non-prostanoid PGI2 mimetics. Silicon as an isostere of carbon. Silicon in p38α MAP kinase inhibitors. Silicon as a carbon isostere in biogenic amine reuptake inhibitors.
Which is an alkyl isostere in a drug?
Cyclopropyl rings as alkyl isosteres. Cyclopropyl in T-Type calcium channel antagonists. Cyclopropyl in CRF-1 antagonists. Oxetanes as mimetics of alkyl moieties. CF3 as a substitute for methyl in a tert -butyl moiety.