Synthesis and antimicrobial activity of some substituted 1, 3, 4-oxadiazole and other heterocycles derived from 4, 5-dimethoxy-2-nitrophenyl-thioacetic acid hydrazide

Anumber of substituted oxadiazoles, benzothiazinones and other heterocycles were synthesized from 4, 5-dimethoxy-2-nitrophenylthioacetic acid hydrazide. The structures of the prepared compounds were confirmed via their elemental analysis and the usual physical measurements. The prepared compounds have been screened for their antimicrobial activities against examples from gram positive, gram negative bacteria and fungi. Two of the tested compounds showed high activity comparable with the reference Levofloxacin while the others showed moderate to low activity

Synthesis of 7H-furo [32-g] -1-benzopyrene-7-ones and their angular analogues 2H-furo [2,3-h] -1-benzopyran-2-ones and 7H-furo [2,3-f] -1-benzopyran-7-ones as potential photodynamic agents

New linear and angular furobenzopyrone derivatives with various substituents [CH3, NO2, C6H5, p.ClC6H4, p.BrC6H4] were prepared by etherification of the key intermediates hydroxybenzopyrones with a proper a-haloketon, followed by cyclization with ethanolic sodium ethoxide. The structure of the new compounds was confirmed by elemental analysis and spectral data. The photobiological activity of the target compounds was investigated

New pyrano [3,2-f] quinolines of posible H1-antihistamine and mast cell stabilizing properties

The pyrano [3,2-f] quinoline-2-carboxylic acids 18-22 have been synthesized by a route that involves construction of the fused pyridine ring upon a performed substituted coumarin nucleus. The in vitro antihistaminic activity of the new acids was tested by measuring the inhibition of histamine-H1 induced contractions of guinea pig ileum

Novel 8-methyl-8-azabicyclo [321] oct-3-yl coumarinyloxy] acetates as potential anticholinergic agents

The synthesis of esters of 31-hydroxy-8-methyl-8-azabicyclo [3.2.1] octane with various [coumarinyloxy] acetic acids is described. Some quaternary salts were also prepared from the corresponding tertiary esters and dimethyl sulphate. Six of the new esters evaluated in terms of anticholinergic activity showed significant antispasmodic action without mydriatic effect

Synthesis of some new propanediols as potential centrally acting muscle relaxants

Two seriales of alpha-y-diethers of glycerol was synthesized as analogues to mephenesin. These compounds were synthesized for the pharmacodynamic study of the effect of substituting the O-methyl group of mephenesin by the more soluble basic substituted acylamino moieties. The skeletal muscle relaxant and tranquilizing activities of five of these compounds were tested in mice and results are included

Synthesis and anticholinergic activity of 8-methyl-8-azabicyclo [321] octanes analogs of atropine

Ten esters derived from 3-hydroxy-8-methyl-8-azabicycle [3.2.1] octane and the corresponding methiodin salts were synthesised. The novel compounds were evaluated for anti-cholinergic activity using rabbit duodenum assay. Among these compounds, 8-methyl-8-azabicycle [3.2.1.] loct-3-y1-3-carbisobutoxy-3- phenyl-propionate [12] was found to be the most effective antispasmodic, comparable in potency to atropine

Synthesis and antimicrobial activity of pyrano [2,3-e] benzoxazol-8- [H] -ones

Synthesis often pyrano [2,3 -e]benzoxazole -[H]-ones belonging to coumarinyl class of antimicrobial agents was described with use of 8- amino -7-hydroxy-4-methyl-coumarin as the starting material A study of antimicrobial activity of these compounds has revealed that N- methyl -1-,2-dihydri-2-oxo-6-methlpyrano [2,3-e] benzoxazole-8[H]-one was the most favorable compound

Novel oxazolocoumarins as antimicrobial agents

The synthesis of new coumarins containing an oxazole ring fused to the 6,7 or 7,8 positions is described. The linear and angular 2- substituted-mercapto-pyrano-benzoxazoles and 2 substituted- amino- pyrano-benzoxazoles were prepared from vic-amino-hydroxy- coumarins. The antimicrobial examination of these compounds revealed that the angular 2-n-butyl-amino-6-methylpyrano [2,3-e] benzoxazole-8 [H]-one is the most promising antibacterial agent

New derivatives of furocoumarins as potential photochemotherapeutic agents

New derivatives of linear and angular furocoumarins were synthesised for obtaining useful photosensitizing agents for treatment of psoriasis. The new compounds, 8-benzoyl-5,-5'-dimethylpsoralen [7b], 5-methyl-4'-phenylangelicin [10b] and their isomeric derivative 4,7 -dimethyl-4'-phenylallopsoralen [10c] were prepared starting from the coumarinic nucleus and condensing on it the furan ring. The photosensitizing activity of the prepared furocoumarins was tested on Bacillus subtilis