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Chiral NG-acylated hetarylpropylguanidine-type histamine H2 receptor agonists do not show significant stereoselectivity.
Bioorg Med Chem Lett
May 2010
Institute of Pharmacy, Pharmaceutical/Medicinal Chemistry, University of Regensburg, D-93040 Regensburg, Germany.
A set of chiral imidazolylpropylguanidines and 2-aminothiazolylpropylguanidines bearing N(G)-3-phenyl- or N(G)-3-cyclohexylbutanoyl residues was synthesized and investigated for histamine H(2) receptor (H(2)R) agonism (guinea pig (gp) right atrium, GTPase assay on recombinant gp and human (h)H(2)R) and for hH(2)R selectivity compared to hH(1)R, hH(3)R and hH(4)R. In contrast to previous studies on arpromidine derivatives, the present investigation of acylguanidine-type compounds revealed only very low eudismic ratios (1.1-3.
View Article and Find Full Text PDFStereoselectivity in the pharmacodynamics and pharmacokinetics of the chiral antimalarial drugs.
Clin Pharmacokinet
May 2004
Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Alberta, Canada.
Several of the antimalarial drugs are chiral and administered as the racemate. These drugs include chloroquine, hydroxychloroquine, quinacrine, primaquine, mefloquine, halofantrine, lumefantrine and tafenoquine. Quinine and quinidine are also stereoisomers, although they are given separately rather than in combination.
View Article and Find Full Text PDF[Characterization of drug, narcotic and psychotropic drug chirality by statistical methods].
Acta Pharm Hung
April 1999
SOTE Gyógyszerészi Kémiai Intézet H-1092 Budapest.
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.
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