What are isosteres in medicinal chemistry?
In medicinal chemistry, bioisosteres are chemical substituents or groups with similar physical or chemical properties which produce broadly similar biological properties to another chemical compound.
What does isosteres mean?
Isosteres are atoms, molecules, or ions of similar size containing the same number of atoms and valence electrons. In general, isosteric molecules have the same shape. This is a consequence of their identical electron arrangements.
Who introduced concept of Bioisosteric group?
Based on its application in biological systems, Harris Friedman introduced the term “bioisostere” in 1950 that included all atoms and molecules which fit the broadest definition for isosteres and have similar biological activity, either agonistic or antagonistic [5].
What are the applications of Bioisosteres that will continue to play an important role in drug discovery?
It allows the improvement of the stability; oral absorption; membrane permeability; and absorption, distribution, metabolism and excretion (ADME) of drug candidate, while retaining their biological properties.
What are classical isosteres?
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.
Which of the following are isosteres?
NO₂⁻ and O₃ are isosteres because both specifies have same (=3) and number of electrons (24).
What are Isosters?
Classical isosteres are defined as being atoms, ions and molecules that had identical outer shells of electrons, This definition has now been broadened to include groups that produce compounds that can sometimes have similar biological activities.
What are classical Isosteres?
What is Bioisomerism?
Bioisosterism is a strategy of Medicinal Chemistry for the rational design of new drugs, applied with a lead compound (LC) as a special process of molecular modification [1].
What is the difference between Isosteres and Bioisosteres?
What is Bioisosterism explain about classical Bioisosteres?
ABSTRACT. Bioisosteres are atoms or group of molecules that fit the broadest definition for isosteres. They. have chemical and physical similarities thus producing broadly similar biological properties. Many heterocycles, when appropriately substituted exhibits bioisosterism.
Are CO and N2O Isosteres?
CO and N2 molecules have same number of atoms as well as same number of electrons.
Where to find isomers with different medical properties?
Isomers having different medical properties can be easily found. For example, in the placement of methyl groups.
Which is an example of an organometallic isomerisation?
An example of an organometallic isomerisation is the production of decaphenylferrocene, [ (η 5 -C 5 Ph 5) 2 Fe] from its linkage isomer. This is usually employed in organic chemistry, where fuels, such as pentane, a straight-chain isomer, are heated in the presence of a platinum catalyst.
Which is the best definition of bioisosterism?
Definition of Bioisosterism Friedman (1951): Bioisosteresare atoms or molecules that fit the broadest definition for isosteresand have the same type of biological activity. Thornber(1979): Groups or molecules which have chemical and physical similarities producing broadly similar biological effects.
What are the different types of isomerism in hydrocarbons?
This group includes chain isomerism whereby hydrocarbon chains have variable amounts of branching; position isomerism which deals with the position of a functional group on a chain; and functional group isomerism in which one functional group is split up into different ones.