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At least 145 records · Page 8Linked to original sources
PubMed2006

Discovery of 4-{4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): a potent, selective, and orally active transforming growth factor-beta type I receptor inhibitor.

Inhibitors of transforming growth factor beta (TGF-beta) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary fibrosis. The optimization of a novel phenylpyridine pyrazole series (1a) led to the identification of potent, selective, and orally active ALK5 inhibitors. The cellular potency and pharmacokinetics profiles of these derivatives were improved and several compounds presented antifibrotic activity when orally administered to rats in an acute liver model of dimethylnitrosamine- (DMN-) induced expression of collagen IA1 mRNA, a major gene contributing to excessive extra cellular matrix deposit. One of the most potent ALK5 inhibitors identified in this chemical series, compound 13d (GW788388), reduced the expression of collagen IA1 by 80% at a dose of 1 mg/kg twice a day (b.i.d.). This compound significantly reduced the expression of collagen IA1 mRNA when administered orally at 10 mg/kg once a day (u.i.d.) in a model of puromycin aminonucleoside-induced renal fibrosis.

Activin Receptors, Type I↗
PubMed2002

Facile preparation of benzo[4,5]thieno[2,3-b]pyridines and naphtho[b-4,5]thieno[2,3-b]pyridines via the reaction of Barton esters and benzynes.

Titled compounds were prepared in a one-pot synthesis by generating symmetrically substituted benzyne intermediates by the diazotization of anthranilic acids in the presence of Barton esters. Unsymmetrically substituted aryne either gave mixtures of regioisomers or failed. However, nitro and methyl derivatives of titled compounds could be obtained as single products using appropriately substituted Barton esters.

Journal Article↗
PubMed1980

Pyridine nucleotide involvement in rat hepatic drug metabolism: pyridine nucleotide kinetics of aniline parahydroxylation.

Apparent kinetic constant (NADPH) have been calculated for NADPH-cytochrome P450 reductase and parahydroxylase in the presence of aniline with hepatic microsomes from both phenobarbital pre-treated and untreated rats. The addition of NADH gave similar stimulation of both aniline parahydroxylation and NADPH-cytochrome P450 reductase activity in the presence of aniline. It is proposed that the increase in aniline metabolism with NADH is due to an increase in the NADPH-cytochrome P450 reductase activity which is rate limiting in microsomes from both phenobarbital and untreated rats.

Aniline Compounds↗
PubMed2003

Di-micro-benzoato-bis[dicarbonyl(pyridine)ruthenium(I)] (new polymorph) and di-mu-trifluoroacetato-bis[dicarbonyl(pyridine)ruthenium(I)].

The syntheses and crystal structure determinations of a pair of 'sawhorse' dimers are reported, viz. [Ru(2)(C(6)H(5)CO(2))(2)(C(5)H(5)N)(2)(CO)(4)] [a new polymorph, cf. Kepert, Deacon, Spiccia, Fallon, Skelton & White (2000). J. Chem. Soc. Dalton Trans. pp. 2867-2874] and [Ru(2)(CF(3)CO(2))(2)(C(5)H(5)N)(2)(CO)(4)]. The Ru.Ru distances are 2.6724 (2) and 2.7122 (5) A, respectively.

Journal Article↗
PubMed2004

Diaquatetrakis(pyridine-2,6-dicarboxylato-kappa2O2,O6)tetrakis(micro-pyridine-3,5-dicarboxylic acid-kappa2N:O)tetracopper(II): a copper complex with tetrameric molecular units.

Crystals of the title tetramer, [Cu4(C7H3NO4)4-(C7H5NO4)4(H2O)2], were synthesized hydrothermally at 433 K. The triclinic structure consists of tetrameric molecular species, which interact via strong hydrogen bonds. The Cu(II) ions are distributed equally between one square-pyramidal site and one octahedral site distorted by the Jahn-Teller effect. This coordination complex exhibits the peculiarity of having Cu(II) ions linked to both the 2,6- and the 3,5-isomers of pyridinedicarboxylic acid.

Journal Article↗
PubMed1990

Effects of a new cardiotonic agent 1,2-dihydro-6-methyl-2-oxo-5-[imidazo (1,2-a) pyridin-6-yl]-3-pyridine carbonitrile hydrochloride monohydrate (E-1020) on contractile force and cyclic AMP metabolism in canine ventricular muscle.

E-1020, a newly synthesized imidazopyridinylpyridine or imidazopyridine derivative (structurally closely related to the bipyridine derivative milrinone) increased the force of contraction and cyclic AMP levels in a concentration-dependent manner in the isolated canine ventricular trabeculae electrically driven at 0.5 Hz at 37 degrees C. The concentration-response curve for the increase in force of contraction by E-1020 was biphasic. The maximal positive inotropic effect (PIE) of E-1020 is comparable to that of milrinone, and its potency is 3-fold less than that of milrinone, but 10-fold higher than that of amrinone. The time course of increases in force of contraction induced by E-1020 was coincident with that of cyclic AMP accumulation. The concentration-response curve for the PIE of E-1020 was superimposable to that of cyclic AMP accumulation. A beta-adrenoceptor antagonist, (+/-)-bupranolol (3 X 10(-7) mol/l), did not affect the PIE of E-1020. The increase in the force of contraction and accumulation of cyclic AMP produced by E-1020 were inhibited by a muscarinic receptor agonist, carbachol. The relationship between the force of contraction and cyclic AMP levels in the presence of E-1020 was not modified by addition of carbachol or isoproterenol. E-1020 shifted the concentration-response curve for isoproterenol to the left. E-1020 shortened the total duration of contraction and relaxation time of isometric contractions. These findings indicate that cyclic AMP is essentially involved in the PIE of E-1020 on the canine ventricular muscle, although the possible involvement of a cyclic AMP-independent mechanism can not be excluded.

Amrinone↗