Current Issue : October-December Volume : 2016 Issue Number : 4 Articles : 5 Articles
Some novel compounds of 3-[3-chloro-2-(4-sustituted)-4-oxoazetidin-1-yl] 2-phenyl disubstituted quinazolin-4(3H)-one, 3-{[2-(3-chloro-4-substituted 2-oxoazetidin-1-yl)-1,3-thiazol-4-yl] amino}-2-phenyl disubstituted quinazolin-4(3H)-one were screened for their antifungal activity against fungi Candida albicans. These compounds have showed moderate and very good antifungal activity. The quantitative structure activity-relationships (QSAR) study on the quinazolin-4(3H)-one series was made using lipophilic, electronic and steric parameters. Several statistical expressions were developed and best models were validated. The studies confirm that the antifungal activity is dependent on selected lipophilic and electronic parameters. The study suggests that substitution on R1 group with increasing lipophilic nature and decreasing electronic factor favorable for antifungal activity. The QSAR study provides important structural insights in designing of potent antifungal agents....
Copper complexes of a few amino acid Schiff bases have been prepared in moderate to good yield. The structures of final compounds were characterized by IR and physicochemical properties. The synthesized compounds have been checked for antiepileptic activity using MES electroshock procedure. Among all the evaluated complexes, compound C3C8 came out to be most active with 74% protection from seizures. Complexes of aromatic amino acid were more efficacious than that of aliphatic ones....
A series of new N-substituted 5-arylidenerhodanine derivatives (D1-D10) were synthesized starting from 5-arylidenerhodanines. The 5-arylidinerhodanines were reacted with 2-bromo-1,1-dimethoxyethane in presence of potassium hydroxide and dimethyl formamide under microwave conditions to give N-substituted 5-arylidenerhodanine derivatives. The synthesized compounds were confirmed on the basis of spectral data and elemental analyses. The newly synthesized compounds were tested for cytotoxicity by brine shrimp lethality bioassay. The N-substituted 5-arylidenerhodanine derivatives (D7, D5 and D6) were proven to be the best potent cytotoxic agents....
A new class of ethyl 5-oxo-4-aryl-5,6-dihydro-4H-1,3,4-oxadiazine-2-carboxylate 3(a-e) derivatives were obtained from various phenyl hydrazine 1(a-e), diethyl oxalates and chloro acetyl chloride. The newly synthesized compounds were confirmed by spectral analysis....
Various substituted 2-phenyl-1H-Benzimidazole derivatives and substituted N-[(1H-benzimidazol-2-yl) methyl]-Benzenamine derivatives were synthesized and characterized by IR, H NMR, Mass spectrometry and were evaluated for their in-vitro antimicrobial activities against Staphylococcus aureus (S. aureus ATCC 25923), Escherichia coli (E. Coli ATCC No. 8739) and antifungal activities against Aspergillus niger and Candida albicans by the means of minimum inhibitory concentration 500 µg/ml to 1 µg/ml using ciprofloxacin HCl and ketocanazole as reference standard....
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