Synthesis and evaluation of the anxiolytic activity of some phthalimide derivatives in mice model of anxiety

The aim of the present study was to synthesis a series of phthalimides based on our previous works and examine their anxiolytic properties. Using a three steps process, phthalimides were prepared from the corresponding di-methyl phthalate derivatives. Phthalic anhydride was nitrated to produce 3-nitrophthalic acid. Ring closer of either 3-nitrophthalic acid or di-methyl phthalate with urea were carried out in reflux condition. Final compounds were prepared by base catalyzed condensation of 4-methylbenzoyl chloride, benzoyl chloride and benzyl chloride with the resulting imides. From the tested compounds, only N-benzoyl 3-nitro-phthalimide was shown to produce anxiolytic activity by increasing the number of entries and time spent in open arms at 10 mg/kg

Synthesis and primary cytotoxic screening of some 3-sulfonamide substituted benzamido-benzimidazolones

Several cycline dependent kinase 2 [CDK2] inhibitors with different chemical structures have been introduced. The hinge region of CDK2 [residues 81_84] contains a set of hydrogen bond donor and acceptor sites some of which must be satisfied for potent inhibitor binding. The benzimidazolone skeleton may provide such interactions. Accordingly, 3-sulfonamide substituted benzamido-benzimidazolones 24-31 were prepared starting from benzoic acid to give the acyl chloride 1 which was reacted with different amines to afford the acids 2-9. The acids were changed to their corresponding acyl chlorides 10-17. Reaction of 10-17 with o-nitropheyl hydrazine gave the nitro derivatives 18-25 followed by reduction of the nitro groups to give 26-33 which were then reacted with ethyl chloroformate to give the target compounds 34-41. The 3-pyridyl derivative 47 was prepared starting with chlorosulfonyl benzoyl chloride to give the acid 43 which was changed to the corresponding acyl, nitro and amino derivatives 44, 45 and 46, respectively, followed by the final ring closure reaction to give 47. The dibenzimidazolinoe derivative 49 was also obtained from the reaction of isopropenyl-benzimidazolone 48 and 3-chloro sulfonyl benzoyl chloride. The target compounds were then tested against the cancer cell lines, Hepa G2, HT-29, CL1-5 and AGS. Results indicated that the target compounds did not show reasonable cell growth inhibition comparing to the positive and negative controls