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Optimization of a pipemidic acid autotaxin inhibitor.
J Med Chem
February 2010
Department of Chemistry, The University of Memphis, Memphis, Tennessee 38152, USA.
Autotaxin (ATX, NPP2) has recently been shown to be the lysophospholipase D responsible for synthesis of the bioactive lipid lysophosphatidic acid (LPA). LPA has a well-established role in cancer, and the production of LPA is consistent with the cancer-promoting actions of ATX. Increased ATX and LPA receptor expression have been found in numerous cancer cell types.
View Article and Find Full Text PDFKinetic model of drug distribution in the urinary bladder wall following intravesical instillation.
Int J Pharm
September 2006
Faculty of Pharmacy, University of Ljubljana, Askerceva 7, SI-1000 Ljubljana, Slovenia.
Intravesical administration of cytotoxic agents is commonly used in urological practice for treatment of superficial bladder cancer. The leading motive is optimisation of drug delivery near the site of action and reduction of systemic toxicity. Bladder pharmacokinetics is complicated by several mechanisms.
View Article and Find Full Text PDFMycobacterium tuberculosis DNA gyrase: interaction with quinolones and correlation with antimycobacterial drug activity.
Antimicrob Agents Chemother
April 2004
Laboratoire de Bactériologie, Faculté de Médecine Pitié-Salpêtrière, Université Pierre et Marie Curie, Paris, France.
Genome studies suggest that DNA gyrase is the sole type II topoisomerase and likely the unique target of quinolones in Mycobacterium tuberculosis. Despite the emerging importance of quinolones in the treatment of mycobacterial disease, the slow growth and high pathogenicity of M. tuberculosis have precluded direct purification of its gyrase and detailed analysis of quinolone action.
View Article and Find Full Text PDFSynthesis, characterization, and antibacterial activities of some rare Earth metal complexes of pipemidic acid.
Chem Pharm Bull (Tokyo)
May 2003
College of Chemistry and Environmental Science, Henan Normal University, Xinxiang, China.
Eight new solid complexes of pipemidic acid (PPA) with trichlorizated rare earth metals LaCl(3), CeCl(3), PrCl(3), NdCl(3), SmCl(3), TbCl(3), DyCl(3), and YCl(3) have been synthesized. The complexes were characterized by elemental analyses, IR, NMR, and molar conductance measurements. The general formulas of the complexes are [M(PPA)(4)]Cl(3) (M=Ce(III), Pr(III), Nd(III), Sm(III), Tb(III), Dy(III), Y(III)), and [La(PPA)(4)Cl]Cl(2).
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