Reaction of tryptamine 1 with dimethyl -3-methoxyallylidenemalonate 2 afforded N?-[4,4-bis (methoxycarbonyl)-1,3-butadienyl] tryptamine 3 which in combination with acetylchloride and pyridine in dichloromethane gave N?, N?-[acetyl]-[(4,4-dinethoxycarbonyl) 1,3butadienyl] tryptamine 4. Treatment of 3 with sodium hydroxide afforded 2H[N-(3-indolyl) ethyl] 2-oxo-3-methoxycarbonyl-1-pyridine 5. Cy...

The molecular mechanisms of three intramolecular rearrangements (I, the rearrangement allyloxycycloheptatriene to yield tricyclic ketones; II, cycloaddition a nitrone-alkene render two isoxazolidines; and III, decomposition N-carbamoyl-L-proline in tetrahydro-1H-pyrrolo[1,2-c]imidazole-1,3(2H)-dione plus water, or tetrahydro-1H,3H-pyrrolo[1,2-c]oxazole-1,3-dione ammonia) have been studied by me...

2 The present work deals with the synthesis of some novel heterocyclic compounds such as benzoxazoles , 7, 13 and 19, imidazoles 3, 8, 14 and 20, benzimidazoles 4, 9, 15 and 21, and tetrazoles 10, 16, and 22. The synthesized compounds were characterized by IR, 1H NMR, mass spectrometry and elemental analysis. The compounds were evaluated for cytotoxicity against human cancer cell lines such as ...

Extracellular signal-regulated kinase (ERK) 1/2, a well known regulator of gene expression, is likely to contribute to signaling events underlying enduring neural adaptations. Phosphorylated (phospho)-ERK was examined immunohistochemically after both single and repeated (i.e., sensitizing) doses of the partial D1-dopamine (DA) receptor agonist SKF-38393 (2,3,4,5-tetrahydro-7,8-dihydroxy-1-pheny...

synthesis and characterization of 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6h-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7h)-oneabstractnew 6-(hydroxymethyl)-14, 16-dimethyl-13, 14, 16, 17-tetrahydro-6h-13, 17-epiminodibenzo [e, l] [1, 4] dioxacyclotridecin-15 (7h)-one (2a) was synthesized in good yield by the petrenko–kritchenko reaction of 2, 2'-((3-hydroxyp...

Dopamine D4 receptors (D4R) are localized in the globus pallidus (GP), but their function remains unknown. In contrast, dopamine D2 receptor activation hyperpolarizes medium spiny neurons projecting from the striatum to the GP and inhibits GABA release. However, using slice preparations from D2R-deficient [D2 knock-out (D2KO)] mice, we found that dopamine inhibited GABA(A)-receptor-mediated cur...

(2R*,4S*)-Methyl 2,3,4,5-tetrahydro-1,4-epoxy-1H-benz[b]azepine-2-carboxylate, C12H13NO3, (I), and its reduction product (2R*,4S*)-methyl 4-hydroxy-2,3,4,5-tetrahydro-1H-benz[b]azepine-2-carboxylate, C12H15NO3, (II), both crystallize as single enantiomers in the space group P212121, while the hydrolysis product (2RS,4SR)-4-hydroxy-2,3,4,5-tetrahydro-1H-benz[b]azepine-2-carboxylic acid, C11H13NO...

The anticancer drug paclitaxel (Taxol) has been converted to a large number of 2-debenzoyl-2-aroyl derivatives by three different methods. The bioactivities of the resulting analogues were determined in both tubulin polymerization and cytotoxicity assays, and several analogues with enhanced activity as compared with paclitaxel were discovered. Correlation of cytotoxicity in three cell lines wit...

Conscious squirrel monkeys were treated i.v. with cocaine and various dopamine agonist drugs. Cocaine produced a dose-dependent increase in blood pressure, heart rate, and the rate-pressure product (RPP). The dopamine D1 receptor agonist (+/-)-6-chloro-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide (SKF 82958) produced effects comparable to cocaine. The D1 agonist (+/-)-6-chl...