Synthesis and analgesic activity of some 1-benzyl-2-substituted-4,5-diphenyl-1H-imidazole derivatives.

In this study, derivatives of 1-benzyl-2-substituted-4,5-diphenyl-1H-imidazole were synthesized and their analgesic activity assayed in two tests. 1,2,4,5-Tetrasubstituted imidazole compounds were obtained by the treatment of purified imidazole compounds with benzyl chloride in the presence of sodium hydride. The structure elucidation of the compounds was performed by IR, 1H-NMR and mass spectroscopic data and elemental analysis results. Generally the prepared compound exhibited only moderate analgesic activity in mice at the dose of 100 mg/kg i.p.; however, a few of them exhibited good activity, almost equivalent to that of morphine at 1 mg/kg i.p. was observed. At the above dosage, no toxicity was observed for all compounds.

Syntheses and analgesic activities of some 2-substituted-4,5-diphenyl and 1,2-disubstituted-4,5-diphenyl imidazole derivatives.

Some substituted imidazole compounds were synthesized and their analgesic activities were determined on the Swiss albino mice (25-35 g) of either sex. During the synthesis, 2-substituted-4,5-diphenyl imidazole compounds were obtained by the reaction of benzil with some substituted or nonsubstituted aldehyde derivatives, in the presence of ammonium acetate. 1-Ethyl-2-substituted-4,5-diphenyl imidazole compounds were obtained by the reaction of purified 2-substituted-4,5-diphenyl imidazole derivatives with alkyl halides in THF at the presence of NaH. All spectral and elemental analyses of the compounds were completed and their structures elucidated. Analgesic activities of the compounds were examined using the Tail-Clip method. 15a (2-p-chlorophenyl-4,5-diphenyl imidazole) and 6b (1-ethyl-2-p-hydroxyphenyl-4,5-diphenyl imidazole) derivatives were found to be more active than the others and their LD50 values were found to be greater than 100 mg/kg (i.p.).

The study on the synthesis and the effects on the intracellular calcium of some 9-substituted-phenanthrene derivatives.

Some 9-(substituted with heteroaryl)-phenanthrene compounds, polycyclic aromatic hydrocarbons (PAH), were obtained by two different methods. In the first method, 9-phenanthraldehyde was reacted with some dion compounds such as benzil, toluil, anisil, etc in the presence of ammonium acetate and glacial acetic acid. In the second method, 9-phenanthraldehyde was reacted with 5-substituted-1,2-phenylenediamine derivatives in the presence of NaHSO3 and ethanol. All of synthesized compounds by us were original and these compounds have not been studied in literature so far. The structures of compounds were confirmed by spectral data and elemental analyses results. The effects of compounds were studied on intracellular calcium level. All of the compounds were examined between the concentrations of 1 and 0.5 microg/mL.

Syntheses of some 2,3, 6-trisubstituted quinoxaline derivatives and investigation of their antispasmodic activities.

Some 2, 3, 6-trisubstituted quinoxaline derivatives were synthesized and their antispasmodic activities were determined on the isolated rat ileum. In the synthesis, some dicarbonyl compounds were reacted with substituted or non-substituted o-phenylenediamines in the presence of acetic acid and gained eighteen compounds. All spectral and elemental analyses of the compounds complete and their structures were elucidated. The pharmacological experiments indicate that the compounds 12,13,18 were most active derivatives and their LD50 values were found to be greater than 100 mg/kg (i.p.).

Synthesis and analgesic activities of 2-substituted-1H-phenantro [9,10-d] imidazoles.

Some 2-substituted-1H-phenantro [9, 10-d] imidazole compounds were synthesized and their analgesic activities were determined on the Swiss albino mice (25-35 g) of either sex. In the synthesis, phenantre-nequinone molecule was reacted with different aldehyde derivatives in acetic acid presence of ammonium acetate and finally 16 compounds were gained. All spectral and elemental analyses of the original compounds were completed and their structures were elucidated. Analgesic activity of the compounds were examined by using the Tail-Clip method. 2-Phenyl-1H-phenantro [9, 10-d] imidazole (comp.1) and 2-(4-chlorophenyl)-1H-phenantro [9, 10-d] imidazole (comp. 6) were found to be more active than the others and their LD50 values were found to be greater than 100 mg/kg (i.p.).