SYNTHESIS AND EVALUATION OF NOVEL PHENACYL BASED CARBOXAMIDE DERIVATIVES OF PIPERIDINE AS ANTIHYPERTENSIVE AGENTS Shamim Akhtar, Z S Saify, M Arif, Nousheen Mushtaq, Ahsana Dar, Ashfaq Ahmed Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Karachi, Karachi-75270, Pakistan, *Department of Pharmacology, HEJ Research Institute of Chemical Sciences, University of Karachi, ...

Pyrrolo[2,1-a]isoquinoline derivatives were synthesized by one-pot three-component reactions starting from isoquinoline, 2-bromoacetophenones and different non-symmetrical acetylenic dipolarophiles using 1,2-epoxypropane as solvent. The structure of the compounds was assigned by IR and NMR spectroscopy.

The synthesis of 3-methyl-1,4-diphenyl-7-thioxo-4,6,8,9-tetrahydropyrazolo[5,4-b] pyrimidino[5,4-e]pyridine-5-one (6) was achieved by two different one-pot multi-component synthesis (one-pot three-component and one-pot four component synthesis). Mono and dialkylation of 6 under different conditions gave compounds 7-11. The hydrazine 12 produced from reaction of 9 with N₂H₄ was subjected to reac...

2-Amino-5-(2-aryl-2H-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles 2-4 have been synthesized by the reaction of 2-aryl-2H-1,2,3-triazole-4-carboxylic acids 1 with thiosemicarbazide. Their reaction with phenacyl (p-substituted phenacyl) bromides led to formation of the respective 6-aryl-2-(2-aryl-2H-1,2,3-triazol-4-yl)imidazo[2,1-b]-1,3,4-thiadiazoles 5. Reactivity of the latter fused ring towards reac...

We describe a novel isothermal gas-chromatographic procedure for measuring valproic acid. Plasma, with cyclohexanecarboxylic acid added as internal standard, is selectively extracted with pentane to minimize the extraction of other acidic drugs. To convert carboxylic acids to their phenacyl esters, alpha-bromoacetophenone is added to the organic extract before evaporating the solvent. These est...

Three azolo[b]1,3,4-thiadiazinium bromides were prepared from the respective N-amino-N'-methylazolethiones and phenacyl bromide, and their crystal structures were determined. 6-Phenyl-1-methylimidazo[2,1-b]1,3,4-thiadiazinium bromide (1) crystallized as methanol solvate (P21/n), 6-phenyl-1-methyl-1,2,4-triazolo[3,4-b]1,3,4-thiadiazinium bromide (2) as hemi-ethanol solvate (P21/n), and 6-phenyl-...

The isoquinoline alkaloids and their biosynthetic relatives include many compounds which show important physiological properties in animals: dopamine, mescaline, morphine, papaverine, and narcotine are pertinent examples. The biosynthetic routes to the members of this family start from the essential aminoacids tyiosine or phenflalanine. Decarboxylation gives a phenethylamine building block (C,-...

In the crystal structure of the title compound, [Cu(2)(CH(3)COO)(4)(C(9)H(7)N)(2)], the Cu(II) cation is coordinated by four acetate anions and one isoquinoline mol-ecule in a distorted square-pyramidal geometry; the Cu(II) cation is 0.1681 (6) Å from the basal coordination plane formed by the four O atoms. Each acetate anion bridges two Cu(II) cations to form the centrosymmetric dinuclear comp...

Nitration of isoquinoline and phthalazine has been successfully demonstrated using a novel process which does not require strong acids. In this study, nitration of isoquinoline was repeated and the method applied to 1-nitroisoquinoline and the azaaromatics quinoline, quinazoline, quinoxaline and pyridine. Nitration of only quinoline was observed, with a product yield lower than that reported fo...