Biomaterial Database

HPLC enantiomeric resolution of novel aromatase inhibitors on cellulose- and amylose-based chiral stationary phases under reversed phase mode. 2000

H Y Aboul-Enein, and I Ali, and G Gübitz, and C Simons, and P J Nicholls

Pharmaceutical Analysis Laboratory, Biological and Medical Research Department (MBC-03), King Faisal Specialist Hospital and Research Center, Riyadh, Saudi Arabia. enein@kfshrc.edu.sa

The chiral resolution of seven aromatase inhibitors (four triazole derivatives (Ia, Ib, Ic, and Id) and three tetrazole derivatives (IIa, IIb, and IIc)) was achieved on Chiralcel OJ-R [cellulose tris (4-methyl benzoate)], Chiralcel OD-RH [cellulose tris (3,5-dimethylphenyl carbamate)], and Chiralpak AD-RH [amylose tris (3,5-dimethylphenyl carbamate)] chiral stationary phases. The mobile phases used were A: 2-PrOH-MeCN (90:10, v/v); B: 2-PrOH-MeCN (50:50, v/v); C: MeCN-H(2)O (50:50, v/v); D: MeCN-H(2)O (80:20, v/v); and E: MeCN-H(2)O (95:05, v/v). The flow rate was 0.5 mL/min for all the mobile phases. The resolution capability of these chiral stationary phases were in the order Chiralpak AD-RH > Chiralcel OD-RH > Chiralcel OJ-R. The values of alpha and Rs of the resolved enantiomers of the aromatase inhibitors varied from 1.02-5.63 and 1. 12-6.72, respectively.

UI	MeSH Term	Description	Entries
D002482	Cellulose	A polysaccharide with glucose units linked as in CELLOBIOSE. It is the chief constituent of plant fibers, cotton being the purest natural form of the substance. As a raw material, it forms the basis for many derivatives used in chromatography, ion exchange materials, explosives manufacturing, and pharmaceutical preparations.	Alphacel,Avicel,Heweten,Polyanhydroglucuronic Acid,Rayophane,Sulfite Cellulose,alpha-Cellulose,Acid, Polyanhydroglucuronic,alpha Cellulose
D002851	Chromatography, High Pressure Liquid	Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.	Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D004791	Enzyme Inhibitors	Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.	Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D000688	Amylose	An unbranched glucan in starch.
D013237	Stereoisomerism	The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)	Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer
D013777	Tetrazoles
D014230	Triazoles	Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.	Triazole
D047072	Aromatase Inhibitors	Compounds that inhibit AROMATASE in order to reduce production of estrogenic steroid hormones.	Aromatase Inhibitor,Inhibitor, Aromatase,Inhibitors, Aromatase