Search

In this study, a new series of 1,3-dimethyl-6-(amino aceto hydrazine) pyrimidine-2,4- dione-6-yl with 4-substituted benzyldehyde, The compound (1-5) was synthesized in a single pot that cyclization by the addition of sodium azide, 2-mercapto acid & 2-amino acetic acid to produce five-membered heterocyclic rings includes: tetrazoline-1yl (6-10), thiazolidin-4-one (11-15) and imidazolidin-4-one (16-20) derivatives respectively. These compounds were characterized using spectral methods [FTIR and 1HNMR, 13C-NMR for some of them] evaluations, measurements, and analyses of their physical qualities. Each molecule was evaluated for antioxidant activity in vitro to use the DPPH and phosphomolybdenum methods. When compared to the standard drug Ascorbic acid, (1-20) demonstrated promising antioxidant activity among the bioactive molecules synthesized. Furthermore, molecular docking against, substances showed superiority over the standard medication Exemestane in tests of the Aromatase enzyme.

Novel derivatives of benzopyran-2-ones are synthesized by catalytic condensation reaction. 4-(3-Hydroxy-2-pyridinylamino)- 3-nitro-2H-[1]-benzopyran-2-one 4a, 4-(4-methyl-3-nitro-2-pyridinylamino)-3-nitro-2H-[1]-benzopyran-2-one, 4b and 4-(pyrimidinylamono)-3-nitro-2H-[1]-benzopyran-2-ones 4(c, d) are synthesized by condensation of 4-Chlor-3-nitro-2H-[1]-benzopyran-2-one 2 and corresponding heteroarylamines 3(a-d ) under reflux reaction conditions. Alkali hydrolysis of 4(a-d ) afforded the 2-hydroxy-? -nitroacetophenone 5. Structural characterization of the synthesized products is done on the basis of spectrometric data. Antibacterial activity of the compounds 4(a-d) against S. aureus, E. coli and Klebsiella was examined by measuring the inhibition zones around the disks marked with the corresponding product solutions in N,N-DMF concentration 2 mg/mL , 4 mg/mL and 6 mg/mL. Compounds 4a and 4c have shown significant antibacterial activity against S. aureus, compounds 4b and 4d exhibited significant activity against E. coli whereas compound 4d was more active against Klebsiella.

Novel derivatives of benzopyran-2-ones are synthesized by catalytic condensation reaction. 4-(3-Hydroxy-2-pyridinylamino)- 3-nitro-2H-[1]-benzopyran-2-one 4a, 4-(4-methyl-3-nitro-2-pyridinylamino)-3-nitro-2H-[1]-benzopyran-2-one, 4b and 4-(pyrimidinylamono)-3-nitro-2H-[1]-benzopyran-2-ones 4(c, d) are synthesized by condensation of 4-Chlor-3-nitro-2H-[1]-benzopyran-2-one 2 and corresponding heteroarylamines 3(a-d ) under reflux reaction conditions. Alkali hydrolysis of 4(a-d ) afforded the 2-hydroxy-? -nitroacetophenone 5. Structural characterization of the synthesized products is done on the basis of spectrometric data. Antibacterial activity of the compounds 4(a-d) against S. aureus, E. coli and Klebsiella was examined by measuring the inhibition zones around the disks marked with the corresponding product solutions in N,N-DMF concentration 2 mg/mL , 4 mg/mL and 6 mg/mL. Compounds 4a and 4c have shown significant antibacterial activity against S. aureus, compounds 4b and 4d exhibited significant activity against E. coli whereas compound 4d was more active against Klebsiella.

Novel derivatives of benzopyran-2-ones are synthesized by catalytic condensation reaction. 4-(3-Hydroxy-2-pyridinylamino)- 3-nitro-2H-[1]-benzopyran-2-one 4a, 4-(4-methyl-3-nitro-2-pyridinylamino)-3-nitro-2H-[1]-benzopyran-2-one, 4b and 4-(pyrimidinylamono)-3-nitro-2H-[1]-benzopyran-2-ones 4(c, d) are synthesized by condensation of 4-Chlor-3-nitro-2H-[1]-benzopyran-2-one 2 and corresponding heteroarylamines 3(a-d ) under reflux reaction conditions. Alkali hydrolysis of 4(a-d ) afforded the 2-hydroxy-? -nitroacetophenone 5. Structural characterization of the synthesized products is done on the basis of spectrometric data. Antibacterial activity of the compounds 4(a-d) against S. aureus, E. coli and Klebsiella was examined by measuring the inhibition zones around the disks marked with the corresponding product solutions in N,N-DMF concentration 2 mg/mL , 4 mg/mL and 6 mg/mL. Compounds 4a and 4c have shown significant antibacterial activity against S. aureus, compounds 4b and 4d exhibited significant activity against E. coli whereas compound 4d was more active against Klebsiella.

Novel derivatives of benzopyran-2-ones are synthesized by catalytic condensation reaction. 4-(3-Hydroxy-2-pyridinylamino)- 3-nitro-2H-[1]-benzopyran-2-one 4a, 4-(4-methyl-3-nitro-2-pyridinylamino)-3-nitro-2H-[1]-benzopyran-2-one, 4b and 4-(pyrimidinylamono)-3-nitro-2H-[1]-benzopyran-2-ones 4(c, d) are synthesized by condensation of 4-Chlor-3-nitro-2H-[1]-benzopyran-2-one 2 and corresponding heteroarylamines 3(a-d ) under reflux reaction conditions. Alkali hydrolysis of 4(a-d ) afforded the 2-hydroxy-? -nitroacetophenone 5. Structural characterization of the synthesized products is done on the basis of spectrometric data. Antibacterial activity of the compounds 4(a-d) against S. aureus, E. coli and Klebsiella was examined by measuring the inhibition zones around the disks marked with the corresponding product solutions in N,N-DMF concentration 2 mg/mL , 4 mg/mL and 6 mg/mL. Compounds 4a and 4c have shown significant antibacterial activity against S. aureus, compounds 4b and 4d exhibited significant activity against E. coli whereas compound 4d was more active against Klebsiella.