Biotransformation reactions of five-membered aromatic heterocyclic rings

…, AS Kalgutkar, SC Khojasteh-Bakht… - Chemical research in …, 2002 - ACS Publications
Organic compounds containing five-membered aromatic heterocyclic rings are widely
distributed in nature and often play an important role in various biochemical processes. …

Pennyroyal toxicity: measurement of toxic metabolite levels in two cases and review of the literature

…, JE Meeker, SC Khojasteh-Bakht… - Annals of internal …, 1996 - acpjournals.org
Background: Pennyroyal is a widely available herb that has long been used as an
abortifacient despite its potentially lethal hepatotoxic effects. However, quantitative data for …

Metabolism of (R)-(+)-pulegone and (R)-(+)-menthofuran by human liver cytochrome P-450s: evidence for formation of a furan epoxide

SC Khojasteh-Bakht, W Chen, LL Koenigs… - Drug Metabolism and …, 1999 - ASPET
(R)-(+)-Pulegone, a monoterpene constituent of pennyroyal oil, is a hepatotoxin that has been
used in folklore medicine as an abortifacient despite its potential lethal effects. Pulegone …

(R)-(+)-Menthofuran is a potent, mechanism-based inactivator of human liver cytochrome P450 2A6

SC Khojasteh-Bakht, LL Koenigs, RM Peter… - Drug metabolism and …, 1998 - ASPET
… Immunization was performed by injecting modified metallothionein sc into rabbits. The rabbits
received two booster shots. The antisera were found to recognize protein adducts formed …

Glutathione S-transferase catalyzes the isomerization of (R)-2-hydroxymenthofuran to mintlactones

SC Khojasteh-Bakht, SD Nelson, WM Atkins - Archives of biochemistry and …, 1999 - Elsevier
(R)-(+)-Menthofuran is the proximate toxic metabolite of pulegone, the major constituent of the
pennyroyal oil, that contributes significantly to the hepatotoxicity resulting from ingestion of …

Formation of a Quinoneimine Intermediate of 4-Fluoro-N-methylaniline by FMO1: Carbon Oxidation Plus Defluorination

…, N Segraves, SC Khojasteh-Bakht - Chemical research in …, 2010 - ACS Publications
Here, we report on the mechanism by which flavin-containing monooxygenase 1 (FMO1)
mediates the formation of a reactive intermediate of 4-fluoro-N-methylaniline. FMO1 catalyzed …

Metabolism, pharmacokinetics, tissue distribution, and excretion of [14C] CP-424391 in rats

SC Khojasteh-Bakht, JP O'donnell, HG Fouda… - Drug metabolism and …, 2005 - ASPET
CP-424391, 2-amino-N-[3aR-benzyl-2-methyl-3-oxo-2,3,3a,4,6,7-hexahydro-pyrazolo[4,3-c]pyridin-5-yl)-1R-benzyloxymethyl-2-oxoethyl]-isobutyramide,
is an orally active growth …

Inhibitory properties of trapping agents: glutathione, potassium cyanide, and methoxylamine, against major human cytochrome p450 isoforms

…, CE Hop, SC Khojasteh-Bakht - Drug metabolism …, 2009 - ingentaconnect.com
In the early stages of drug discovery, the formation of reactive metabolites is often assessed
by co-incubating the drug in liver microsomes with a trapping agent in the presence of …

Automated online liquid chromatographic/mass spectrometric metabolic study for prodrug stability

F Lai, SC Khojasteh-Bakht - Journal of Chromatography B, 2005 - Elsevier
In vitro metabolic stability studies are performed routinely in drug discovery to determine the
rate of metabolism as well as the metabolic fate of compounds. These studies are labor …

Metabolism, pharmacokinetics, and excretion of a nonpeptidic substance P receptor antagonist, ezlopitant, in normal healthy male volunteers: characterization of polar …

C Prakash, J O'Donnell, SC Khojasteh-Bakht - Drug metabolism and …, 2007 - ASPET
The excretion, biotransformation, and pharmacokinetics of ezlopitant [(2-benzhydryl-1-aza-bicyclo[2.2.2]oct-3-yl)-(5-isopropyl-2-methoxy-benzyl)-amine],
a substance P receptor …