4-Aminoantipyrine was utilized as key intermediate for the synthesis of pyrazolone derivatives bearing biologically active moieties. The newly synthesized compounds were characterized by IR, 1H- and 13C-NMR spectral and microanalytical studies. The compounds were screened as anticancer agents against a human tumor breast cancer cell line MCF7, and the results showed that (Z)-4-((3-amino-5-imino...

Purpose: The article is aimed to synthesize,characterize and screening the biological activity of a series of Synthesis of 1-(2-(3-(3-chloro-1-(4-substituted phenyl)-4-tetrazole-2-yl)-1H-indol-1-yl)acetyl)-4-(2-(4substituted phenyl)hydrazono)-3-(trifluoromethyl)-1H-pyrazol-5(4H)-one 4(a-f). Indole-3-carbaldehyde and chloro ethyl acetate were dissolved in DMF. To this reaction mixture anhydrous ...

4-{[4-({(3R)-1-Butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenyl]oxy}benzoic acid hydrochloride (873140) is a potent noncompetitive allosteric antagonist of the CCR5 receptor (pK(B) = 8.6 +/- 0.07; 95% CI, 8.5 to 8.8) with concomitantly potent antiviral effects for HIV-1. In this article, the receptor-based mechanism of action of 873140 is compared ...

A promising imidazole compound was synthesized through the following route. The reaction of 5-methyl-2-phenyl-1H-imidazole-4-carbohydrazide (1) with carbon disulfide and potassium hydroxide in ethanol (80%) afforded salt (2). Refluxing (2) phenacyl bromide (3) ethanol/water (1:1) gave 2-((5-(5-methyl-2-phenyl-1H-imidazol-4-yl)-1,3,4-oxadiazol-2-yl)thio)-1-phenylethan-1-one (4) a 76% yield. stru...

The novel racemic secondary alcohol (±)-2-{[4-(4-bromophenyl)-5-phenyl-4H-1,2,4-triazol-3-yl]sulfanyl}-1-phenyl-1-ethanol (12) has been successfully synthesized through S-alkylation of 4-(4-bromophenyl)-5-phenyl-4H-1,2,4-triazole-3-thiol (10) in alkaline medium with 2-bromo-1-phenylethanone followed by reduction the corresponding ketone 11. All compounds were characterized IR, 1D (1H, 13C, DEPT...

Tertiary piperazine aminoalcohols were synthesized by reacting 1-(4-butoxyphenyl)-3-(4-substituted piperazin-1-yl)-2-phenylpropan-1-ones with alkyl(aryl)magnesium halides. Some of the final compounds converted into dihydrochlorides. The influence on C-180 mouse tumor DNA methylation was studied in vitro incubating drug solutions (3 × 10–6 M) homogenates at 37°C (thermostatted) for 24 h. Rather ...