What do you mean by bioisostere?
Bioisosteres – A bioisostere is a molecule resulting from the exchange of an atom or of a group of atoms with an alternative, broadly similar, atom or group of atoms. The objective of a bioisosteric replacement is to create a new molecule with similar biological properties to the parent compound.
What are the types of bioisostere?
Bioisosteres are classified into the following two types: Classical bioisosteres. Nonclassical bioisosteres.
What is a bioisostere what is its importance in drug design?
Abstract. Introduction: A bioisostere is a powerful concept for medicinal chemistry. 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 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 Bioisomerism?
Bioisosterism. Bioisosteres – substituents or groups with chemical or physical similarities that produce similar biological properties.
What is Bioisosteric replacement?
Bioisosteric replacement involves swapping functional groups of a molecule with other functional groups that have similar biological properties.
Are carboxylic acids lipophilic?
The most interesting feature of this carboxylic acid surrogate is the relatively high lipophilicity, which makes this moiety potentially attractive for CNS drug discovery programs, where the presence of a carboxylic acid moiety in a drug candidate can result in a limited rate of passive diffusion across the BBB.
Why is fluorine considered an bioisostere of hydrogen?
Unlike the other members of the halogen family, fluorine does not engage in strong halogen bonding interactions and is considered to be nonpolarizable. For these reasons, fluorine has played a prominent role as a bioisostere in drug design to date.
What is bioisosterism Slideshare?
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.
Is lactic acid a carboxylic acid?
lactic acid, also called α-hydroxypropionic acid, or 2-hydroxypropanoic acid, an organic compound belonging to the family of carboxylic acids, present in certain plant juices, in the blood and muscles of animals, and in the soil.
Why carboxylic acid is soluble in nahco3?
Since carboxylate ions have a negative charge, they are more soluble than carboxylic acids. Thus, carboxylic acids readily dissolve in sodium bicarbonate solution.
What is bioisosteres?
Bioisosteres – A bioisostere is a molecule resulting from the exchange of an atom or of a group of atoms with an alternative, broadly similar, atom or group of atoms. The objective of a bioisosteric replacement is to create a new molecule with similar biological properties to the parent compound.
What is an isostere in chemistry?
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.
What is the objective of bioisosteric replacement?
The objective of a bioisosteric replacement is to create a new molecule with similar biological properties to the parent compound. The bioisosteric replacement may be physicochemically or topologically based.
When was The isostere concept developed?
The isostere concept was formulated by Irving Langmuir in 1919, and later modified by Grimm. Hans Erlenmeyer extended the concept to biological systems in 1932.