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Chiral drugs that are equimolar (1:1) mixture of enantiomers are called racemic drugs and these are obviously devoid of optical rotation. The most commonly encountered stereogenic unit, [ 2 ] that confers chirality to drug molecules are stereogenic center.
There are examples of common drugs, like ibuprofen, where the use of chiral switching has caused controversy. Ibuprofen is a racemic mixture where the S-enantiomer is known to play a major role in reducing inflammation as it inhibits COX-2 (cooxygenase 2) compared to the R-enantiomer; the fact that the S-enantiomer is stronger is what led to ...
Levofloxacin as an example of a chiral switch. A chiral switch is a chiral drug that has already approved as racemate but has been re-developed as a single enantiomer. [1] [2] The term chiral switching was introduced by Agranat and Caner in 1999 [3] to describe the development of single enantiomers from racemate drugs.
Moving from a racemic drug to a chiral specific drug may be done for a better safety profile or an improved therapeutic index. This process is called chiral switching and the resulting enantiopure drug is called a chiral switch. [10] As examples, esomeprazole is a chiral switch of (±)-omeprazole and levocetirizine is a chiral switch of (± ...
There are a few examples of chiral drugs where both the enantiomers contribute, in different ways, to the overall desired effect. An interesting situation is that in which the distomer antagonizes a side-effect of the eutomer for the desired action, mutually beneficial action form therapeutic standpoint.
Chiral inversion is the process of conversion of one enantiomer of a chiral molecule to its mirror-image version with no other change in the molecule. [1] [2] [3] [4]Chiral inversion happens depending on various factors (viz. biological-, solvent-, light-, temperature- induced, etc.) and the energy barrier energy barrier associated with the stereogenic element present in the chiral molecule. 2 ...
Chiral resolution, or enantiomeric resolution, [1] is a process in stereochemistry for the separation of racemic mixture into their enantiomers. [2] It is an important tool in the production of optically active compounds, including drugs . [ 3 ]
The use of atropisomeric drugs provides an additional way for drugs to have stereochemical variations and specificity in design. [22] One example is (–)-N-acetylallocolchinol, a drug that was discovered to aid in chemotherapy cancer treatment. [22] [23] Telenzepine is atropisomeric in the conformation of its central thienobenzodiazepine ring.