Some pharmacologically active sulpha/substituted Indoles were synthesised by refluxing the mixture of sulpha/substituted phenyl amine and α-haloacyl benzene in glacial acetic acid. The newly synthesised compounds were characterised by IR, 1H NMR, and UV spectral studies. They were also evaluated for their promising pharmacological activity such as anti-tuberculosis and anti-inflammatory activit...

New chiral mexiletine analogs were synthesized in their optically active forms and evaluated in vitro as use-dependent blockers of skeletal muscle sodium channels. Tests carried out on sodium currents of single muscle fibers of Rana esculenta demonstrated that all of them exerted a higher use-dependent block than mexiletine. The most potent analog, (S)-3-(2,6-dimethylphenoxy)-1-phenylpropan-1-a...

The olefin moiety presents in styrylsulfonylmethyl-1,2,4-triazolylamine (1) was exploited to build up five-member heterocycle-pyrazoles. series of novel pyrazolyl-1,2,4-triazole amine derivatives (2-3) have been synthesized. All the entitles compounds were characterized by 1H and 13C NMR spectra.

The synthesis of a small library of dihydrouracils spiro-fused to pyrrolidines is described. These compounds are synthesized from beta-aryl pyrrolidines, providing products with the 2-arylethyl amine moiety, a structural feature often encountered in compounds active in the central nervous system. The b-aryl pyrrolidines are synthesized through a three-step methodology that includes a Knoevenage...

In terms of molecular symmetry and bioactivity, new C3- and CS-symmetrical derivatives based on the tris(2-aminoethyl)amine scaffold were designed and synthesized. The synthesized compounds were evaluated for antiviral activity with herpes simplex virus type 1 (HSV-1) by a plaque reduction assay and for cytotoxic activity with Vero cells. Most of the compounds showed no significant anti-HSV-1 a...

Imatinib and its analogues were successfully synthesized by an improved method in 19.5– 46.2% total yield of six main steps. Pyrimidinyl amine was prepared by the reaction of enaminone and guanidine nitrate without the use of a toxic cyanamide. N-(2Methyl-5-nitrophenyl)-4-(pyridin-3-yl) pyrimidin-2-amine as a key intermediate for the synthesis of imatinib was prepared by coppercatalyzed N-aryla...

In this study we report the synthesis of a series 2-Azetidinones from N-(4-(5-bromothiophen-2-yl)-6-(4-chlorophenyl)pyrimidin-2- yl)-1-(aryl) methanimine. A mixture methanimine and triethyl amine was reacted with chloroacetyl chloride in 1,4-dioxane. The N-(4-(5-bromothiophen-2-yl)-6-(4 -chlorophenyl) pyrimidin-2- prepared reaction 4-(5-bromothiophene-2-yl)-6-(4-chloropheneyl)pyrimidin-2-amine ...

The amine-borane adducts of cyclohexylamine and toluidine were observed to be potent hypolipidemic agents in mice, I.P. and rats orally at 8 mg/kg/day lowering both serum cholesterol and triglyceride levels after 14-16 days. These compounds were able to lower tissue lipids including the cholesterol content of the aorta wall. The agents successfully lower VLDL- and LDL-cholesterol content while ...