[Characterization of drug, narcotic and psychotropic drug chirality by statistical methods].
The percentage of chiral entities among drug, narcotic drug and psychotropic compounds is steadily increasing. Receptors of the human body recognize the enantiomeric forms of constitutionally identical compounds as entirely different chemical agents. Based upon these facts, this paper reports the percentage of chiral compounds in the various pharmacological classes, and related data. Pertinent terms, such as eutomer, distomer, eudismic index, eudismic affinity quotient are defined. Differences in biological activity between eutomers and distomers are exemplified. The pharmacological classes and subclasses of highest chirality, and the "most chiral" active principles are shown. Some puzzling observations on pharmacological behaviour of stereoisomers are highlighted. The necessity of "racemate switch" in the pharmaceutical industry, and the significance of stereo-specific interactions between the drug, narcotic drug and psychotropic ligands, and complementary, "pocket" moieties of the human body are emphasized. Some features of enantiopharmacology, a fledgling science in the interface of stereochemistry and traditional pharmacology are introduced. The statistical treatment of asymmetric compounds in pharmacological classes and subclasses shows that presently, the percentage of chirality in drug categories is more characteristic of the origin of the compound than its target molecule.
Noszál
B
B
SOTE Gyógyszerészi Kémiai Intézet H-1092 Budapest.
Schiller
Z
Z
D006801:Humans; D015394:Molecular Structure; D009294:Narcotics / Q000737:chemistry*; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011619:Psychotropic Drugs / Q000737:chemistry*; D011955:Receptors, Drug / Q000378:metabolism; D011957:Receptors, Opioid / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D009294:Narcotics; D004364:Pharmaceutical Preparations; D011619:Psychotropic Drugs; D011955:Receptors, Drug; D011957:Receptors, Opioid
Gyógyszer- és kábítószervegyületek kiralitásának statisztikai jellemzése.