Several chiral drugs are produced and administered as pure enantiomers, whereas many others, especially of synthetic origin, are used mainly in the form of racemates. The biological and pharmacological activity of chiral compounds depends on their configuration. The racemic drugs may exhibit quite different activity from the optically pure drugs. Often only one of the enantiomers is pharmacologically active and/or even can be toxic. Since numerous enantiomers have been shown to behave differently from at least one point of view, whether pharmacokinetic, pharmacodynamic, toxicological or interaction, there seems to be hardly any exception to the general rule that a racemate cannot be considered as a single drug entity. A variety of chromatographic methods have been developed for optical resolution recently. Usually direct separation of the enantiomers is carried out on HPTLC chiral precoated plates or on plates impregnated with chiral substances. TLC techniques are a developing branch of separation and quantitation of drugs, both in pharmaceutical dosage forms and in biological material. This review presents an overview of the current successful enantioseparations of drugs by TLC and their potential in the analysis of the drug racemates.
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http://dx.doi.org/10.1002/(SICI)1099-0801(199912)13:8<531::AID-BMC921>3.0.CO;2-Q | DOI Listing |
Pharmaceutics
December 2024
Vinča Institute of Nuclear Sciences, National Institute of the Republic of Serbia, University of Belgrade, Mike Petrovića Alasa 12-14, 11001 Belgrade, Serbia.
Pathogen bacteria appear and survive on various surfaces made of steel or glass. The existence of these bacteria in different forms causes significant problems in healthcare facilities and society. Therefore, the surface engineering of highly potent antimicrobial coatings is highly important in the 21st century, a period that began with a series of epidemics.
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December 2024
Industrial Chemistry Laboratory, Department of Chemistry, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece.
Well-defined amorphous/semi-crystalline statistical copolymers of n-dodecyl isocyanate, DDIC, and allyl isocyanate, ALIC, were synthesized via coordination polymerization using the chiral half-titanocene complex CpTiCl(O-(S)-2-Bu) as an initiator. In the frame of the terminal model, the monomer reactivity ratios of the statistical copolymers were calculated using both well-known linear graphical methods and the computer program COPOINT. The molecular and structural characteristics of the copolymers were also calculated.
View Article and Find Full Text PDFPlants (Basel)
December 2024
Departamento de Química, Universidad Técnica Particular de Loja (UTPL), Calle Paris s/n y Praga, Loja 110107, Ecuador.
This study presents the first chemical and enantioselective analyses of essential oils (EOs) derived from the leaves of two endemic species, Cuatrec. and (Kunth) Cass., from Loja, Ecuador.
View Article and Find Full Text PDFPharmaceuticals (Basel)
November 2024
Herbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.
Small-molecule probes are powerful tools for studying biological systems and can serve as lead compounds for developing new therapeutics. Especially, nitrogen heterocycles are of considerable importance in the pharmaceutical field. These compounds are found in numerous bioactive structures.
View Article and Find Full Text PDFMolecules
December 2024
Chengdu Shibeikang Biomedical Technlogy Co., Ltd., 26-1-2, No.2 Tianyu Road, Chendu Gaoxin West District, Chengdu 611700, China.
A new process route suitable for the industrial production of BAY2433334 has been developed in this paper, which avoids the patent limitations of the originator company of BAY2433334 to the preparation of BAY2433334. BAY2433334 is obtained from (2)-2-aminobutyric acid by esterification, diazotization, condensation reactions, deacetyl deprotection, activation reactions, and Mitsunobu reactions. This method is simple to operate, and the raw materials are inexpensive and readily available.
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