1. Synthesis, in vitro antibacterial and antifungal activity of some n-acetylated and non-acetylated pyrazolines
Muhammad Baseer, Farzana Latif Ansari, Zaman Ashraf Pak J Pharm Sci. 2013 Jan;26(1):67-73.
Fourteen new N-acetylated and non-acetylated pyrazoline derivatives were synthesized by reacting chalcones with hydrazine in the presence of absolute ethanol however reaction was carried out in the presence of glacial acetic acid to afford N-acetylated pyrazolines. The chemical structures of the synthesized pyrazolines were confirmed by FTIR, (1)HNMR, (13)CNMR and mass spectroscopic data. The pyrazolines (1-14) were screened for antibacterial activity against ten bacterial strains using seven Gram-positive and three Gram-negative bacteria and antifungal activity against Aspergillus flavus, Aspergillus niger and Aspergillus pterus. Pyrazolines (1-14) found to exhibit good to excellent antimicrobial activities compared to the levofloxacin and fluconazole used as standard drugs.
2. Synthesis and antimicrobial activity of some 1-(2,4-dinitrophenyl)-3-(3-nitrophenyl)-5-(4-substituted phenyl)-4-bromo-2-pyrazolines and 1-(2,4-dinitrophenyl)-3-(3-nitrophenyl)-5-(4-substituted phenyl)-2-pyrazolin-4-ones
Sagar K Mishra, Sabuj Sahoo, Prasana K Panda, Satya R Mishra, Raj K Mohanta, Poluri Ellaiah, Chandra S Panda Acta Pol Pharm. 2007 Jul-Aug;64(4):359-64.
A series of 1-(2,4-dinitrophenyl)-3-(3-nitrophenyl)-5-(4-substituted phenyl)-2-pyrazolin-4-ones (4a-e) have been synthesized by the oxidation of 1-(2,4-dinitrophenyl)-3-(3-nitrophenyl)-5-(4-substituted phenyl)-4-bromo-2-pyrazolines (3a-e) with dimethylsulfoxide. The structure has been established on the basis of spectral data (IR,1H NMR). The synthesized compounds have been screened in vitro for their possible antimicrobial activity.
3. Synthesis, antibacterial and antifungal activity of some new pyrazoline and pyrazole derivatives
Seham Y Hassan Molecules. 2013 Feb 28;18(3):2683-711. doi: 10.3390/molecules18032683.
A series of 2-pyrazolines 5-9 have been synthesized from α,β-unsaturated ketones 2-4. New 2-pyrazoline derivatives 13-15 bearing benzenesulfonamide moieties were then synthesized by condensing the appropriate chalcones 2-4 with 4-hydrazinyl benzenesulfonamide hydrochloride. Ethyl [1,2,4] triazolo[3,4-c][1,2,4]triazino[5,6-b]-5H-indole-5-ethanoate (26) and 1-(5H-[1,2,4]triazino[5,6-b] indol-3-yl)-3-methyl-1H-pyrazol-5(4H)-one (32) were synthesized from 3-hydrazinyl-5H-[1,2,4]triazino[5,6-b]indole (24). On the other hand ethyl[1,2,4]triazolo[3,4-c][1,2,4]triazino[5,6-b]-5,10-dihydroquinoxaline- 5-ethanoate (27) and 1-(5,10-dihydro-[1,2,4]triazino[5,6-b]quinoxalin-3-yl)-3-methyl-1H-pyrazol-5(4H)-one (33) were synthesized from 3-hydrazinyl-5,10-dihydro-[1,2,4]triazino[5,6-b]quinoxaline (25) by reaction with diethyl malonate or ethyl acetoacetate, respectively. Condensation of 6,6-dimethyl-4-oxo-4,5,6,7-tetrahydro-1H-indole-2-carbaldehyde (1') with compound 24 or 25 afforded the corresponding Schiff's bases 36 and 37, respectively. Reaction of the Schiff's base 37 with benzoyl hydrazine or acetic anhydride afforded benzohydrazide derivative 39 and the cyclized compound 40, respectively. Furthermore, the pyrazole derivatives 42-44 were synthesized by cyclization of hydrazine derivative 25 with the prepared chalcones 2-4. All the newly synthesized compounds have been characterized on the basis of IR and 1H-NMR spectral data as well as physical data. Antimicrobial activity against the organisms E. coli ATCC8739 and P. aeruginosa ATCC 9027 as examples of Gram-negative bacteria, S. aureus ATCC 6583P as an example of Gram-positive bacteria and C. albicans ATCC 2091 as an example of a yeast-like fungus have been studied using the Nutrient Agar (NA) and Sabouraud Dextrose Agar (SDA) diffusion methods. The best performance was found for the compounds 16, 17, 19 and 20.
