Synthesis and pharmacological screening of some new phenothiazine derivatives

Some of phenothiazine derivatives; namely, 10H- phenothiazine-2-carboxylic acid 1- or 2-phenylcarbamoyl ethyl ester [3] and [4] as well as 2-[1,5-diphenyl-4,5-dihydro-1H-pyrazol-3-yl]-10H-phenothiazine and 2-[5-[4-chlorophenyl]-4,5-dihydroisoxazol-3-yl]-10H-phenothiazine derivatives 5 and 6, were synthesized. Compounds 4 showed interesting levels of analgesic and tranquilizing activities comparable with that of paracetamol and chlorpromazine, respectively

Synthesis and pharmacological activities of certain new pyrazole and chromone derivatives

In this investigation, some new chromone and pyrazole derivatives have been synthesized by the action of hydrazine hydrate on certain substituted chromones. Some of the synthesized compounds showed marked analgesic, anti-inflammatory and antipyretic activities

Synthesis of new derivatives of carnitine chloride

Five new carnitine chloride analogues were synthesized from lithio t- butyl acetate 2a and lithio t-butyl isopropionate 2b and the appropriate dimethylaminoketones 3a-c and 2-acetylpyridine. The condensation products 4a-d and 8 were converted to the required new acids 7a-d and 2 through few reaction steps. The selected molecular modifications don't affect markedly the main structural features of carnitine chloride. It is aimed that pharmacological testing of these new compounds may disclose the knowledge about the structure- activity relationship of carnitine chloride and its analogues

Synthesis of new analogues of 1- [3-Chlorophenyl] -1Methy1-2- Pheny1-2 [2-Pyridine] Ethanol and ethyl 2- [4-Chlorophenoxy] -2Methyl-propionate [Clofibrate]

This investigation deals with the synthesis of certain new benzylpyridine derivatives which are structurally related to the hypocholesteremic agents, benzylpyridines and the hypolipidemic agent, clofibrate. The new compounds, l-alkyl-1-[4-substained phenyl]-2- phenyl-2-[2-pyridyl] ethanols 6a-c, were synthesized by the interaction between 2-benzylpyridine and the appropriate ketone in presence of n-BuLi. Compound 6c was obtained in a poor yield which may be attributed to the steric effect of the relatively bulky starting material 4c. Phenyl-2-pyridyl-3,4,5-trimethoxybenzoyl methane 8 was obtained in a very low yield when 2-benzylpyridine was reacted with methyl 3,4,5-trimothoxybenzoate in presence of KNH2 in liquid NH3. The same procedure failed to yield ketones 12 and 13. Also, trials to synthesize these ketones by the direct interaction between the corresponding acid chloride and 2-benzylpyridine in presence of n-BuLi gave unexpected products of uncertain structures. It is of interest that n-BuLi affected the condensation very successfully, instead of KNH2 between ethyl 3-dimethylamino benzoate or phenoxyacetic acids-esters and 2-benzylpyridine to yield 3-dimethyl-aminobenzoylphenyl-[2-pyridyl] methane 12 and substituted phenoxyacetylphenyl-[2-pyridyl] methonal was obtained for the first time as a low melting point solid. Several other unsuccessful trails were reported and discussed