What is Bioisosterism examples?
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 in drug design?
BIOISOTERISM:A useful strategy for drug design 1. 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 is the Grimm concept of Bioisosterism?
Grimm’s Hydride Displacement Law is an early hypothesis to describe bioisosterism, the ability of certain chemical groups to function as or mimic other chemical groups.
Is used for Bioisosteric replacement of benzene?
The replacement of para-substituted benzenes with saturated bi- and polycyclic bioisosteres – bicyclo[1.1. 1]pentane, bicyclo[2.2. 2]octane and cubane, – often increases the potency, selectivity and metabolic stability of bioactive compounds.
What is bioisosterism easy?
Filters. (pharmacology) The relationship between bioisosteres, substituents or groups with similar physical or chemical properties that impart similar biological properties to a chemical compound.
What is the difference between Isosteres and bioisosteres?
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 many types is classified bioisosterism?
Bioisosteres are classified into the following two types: Classical bioisosteres. Nonclassical bioisosteres.
What is language concept of bioisosterism?
Wiktionary. bioisosterismnoun. The relationship between bioisosteres, substituents or groups with similar physical or chemical properties that impart similar biological properties to a chemical compound.
How many types of classical Isosteres are their?
Classical bioisosteres can be further subdivided into five classes: 1) monovalent atoms or groups (D and H; F and H; C and Si; Cl, Br, SH, and OH; NH and OH; RSH and ROH, –Cl, –PH2, –SH), 2) divalent atoms or groups (–CH2, –NH, –O, –S, –Se–, -COCH2-), 3) trivalent atoms or groups (–CH=, –N=, -P=, -As=), 4) tetravalent …
Why is it important to study medicinal chemistry?
By imparting an exclusive knowledge base, medicinal chemistry plays a vital role in providing critical thinking and evidence-based problem-solving skills to pharmacy students, enabling them to make optimal patient-specific therapeutic decisions.
What are the types of Bioisoster?
3.10. For instance, Birch et al. were able to evaluate the effect of the common bioisosteric change of carboxylic acid with tetrazole and discovered that a significant increase in plasma protein binding is generally associated with this change.
How does pKa affect drug?
The pKa of a drug is the hydrogen ion concentration (pH) at which 50% of the drug exists in its ionized hydrophilic form (i.e., in equilibrium with its un-ionized lipophilic form). All local anesthetic agents are weak bases. At physiologic pH, the lower the pKa the greater the lipophilicity.
What is the role of bioisosteres in Medicinal Chemistry?
As an established and powerful concept in medicinal chemistry, the application of bioisosteres will continue to play an important role in drug discovery. Isosterism can also contribute to the productive application in the design and optimization of catalysts on organic chemistry.
Why do we use bioisosterism to design new drugs?
There may be innumerous reasons for the use of bioisosterism to design new drugs, including the necessity to improve pharmacological activity, gain selectivity for a determined receptor or enzymatic isoform subtype – with simultaneous reduction of certain adverse effects -, or even optimize the pharmacokinetics the LC might present.
What is an example of isosteric substitution in biology?
7. APPLICATION OF CLASSICAL BIOISOSTERISM IN DRUG DESIGN. Replacement of monovalent atom. Example The substitution of hydrogen atom by fluorine is the one of the most commonly employed monovalent isosteric replacement.
What is the difference between classical and nonclassical bioisostere?
Unlike their classical counterparts, nonclassical bioisosteres do not conform to Langmuir’s broad definition of “isostere.” Nonclassical bioisosteres are groups capable of emulating the steric or electronic profile of the original functional group Introduction to Nonclassical Bioisosteres