The stereoselective synthesis of (1S,2S,5R)-5-((4-methoxybenzyl)oxy)-2-methyl-8-methylene-1,2,4a,5,6,7,8,8a-octahy-dronaphthalene-1-carboxylic acid (2) is described, which comprises the bicyclic core structure natural product amycolamicin (1). ring-system was established via an intramolecular Diels-Alder reaction a triene carrying SuperQuat chiral auxiliary. latter could be readily removed by m...

Reaction of thionyl chloride with 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid 1 gave acid chloride 2. Compound 2 was reacted with glycine and D-glutamic acid to afford 2-(7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4- dihydroquinoline-3-carbonyl) aminopantandioicacid 3a and 2-(7-chloro-1-cyclopropyl-6- fluoro -4- oxo-1,4-dihydroquinoline-3-carbonyl)aminoacetica...

with urease. A third minor metabolite was present in urine collected after intraperitoneal administration but remains unidentified. The quantitative distribution of pterin-dcarboxylic acid and urea in the 0-24 h urine samples is shown in Table 1. Fukushima & Nixon (1980) reported the degradation of [2-14C]pterin-6-carboxylic acid to 14C02 by the gut microorganisms of the rat. It is possible tha...

A series of 3-monohydroxylated bile acids, in unlabeled and radioactive form, of varying side chain length and configuration at C-3 has been synthesized and rigorously characterized. They include: 3 alpha- and 3 beta-hydroxy-5 beta-androstane-17 beta-carboxylic acids (C20); 3 alpha- and 3 beta-hydroxy-5 beta-pregnan-21-oic acids (C21); 3 alpha- and 3 beta-hydroxy-23,24-bisnor-5 beta-cholan-22-o...

In an investigation of the mechanisms of the neuroprotective effects of theanine (gamma-glutamylethylamide) in brain ischemia, inhibition by theanine of the binding of [3H](RS)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), [3H]kainate, and [3H](E)-3-(2-phenyl-2-carboxyethenyl)-4,6-dichloro-1-H-indole-2-carboxylic acid (MDL 105,519) to glutamate receptors was studied in terms ...

The anorexigen (+)-fenfluramine was used for treatment of obesity until the association of use with valvular heart disease and primary pulmonary hypertension. (+)-Fenfluramine has been found in Chinese and Korean slimming pills. The hepatic metabolite of (+)-fenfluramine, (+)-norfenfluramine, has affinity for 5-hydroxytryptamine (5-HT)(2A) and 5-HT(2B) receptors. We tested the hypothesis that (...

Mukesh C. Sharma Dept. of Pharmaceutical Sciences, Dr.Hari Singh Gour University Sagar (M.P) 470003 India Department of Chemistry Yadhunath Mahavidyalya Bhind (M.P) 477001 India Email: [email protected] Abstract A new series of non peptide angiotensin (A-II) receptor antagonist has been prepared. This N-(biphenyl methyl) imidazoles e.g. Some new 4'-{5-amino2-[2-substituted-phenylamino)-ph...

Condensation and cyclization of 5-hydroxy- 1,2,4- thiadiazol-2-yl hydrazine 1 with pyruvic acid, phenacyl bromide, propargyl bromide and ally1 bromide afforded compounds 2,5,7 3, 4 ,6 and 8 respectively, Reaction of 1 with epichforohydrine afforded 4-hydroxy-N-[5-hydroxy- 1 ,3,4-thiadiazoly1] pyrazolidine 9

Phytohemagglutinin (PHA)-induced mitogenesis of mixed mouse spleen lymphocyte populations, measured by [3H]thymidine incorporation, was completely inhibited by micromolar concentrations of certain hydroxyeicosatetraenoic acids (HETE's). These are lipoxygenase metabolites of arachidonic acid which are synthesized in considerable concentrations by macrophages, lymphocytes, and other components of...

The growth-inhibiting activity of Tabebuia impetiginosa Martius ex DC dried inner bark-derived constituents against Helicobacter pylori ATCC 43504 was examined using paper disc diffusion and minimum inhibitory concentration (MIC) bioassays. The activity of the isolated compounds was compared to that of the commercially available anti-Helicobacter pylori agents, amoxicillin, metronidazole, and t...