Synthesis and Biological Activity of Some New ?- Lactame Derivatives
Journal: International Journal of Science and Research (IJSR) (Vol.6, No. 3)Publication Date: 2017-03-05
Authors : F. A. Yassin; Amal F. Seliem; B. E. Bayomy; H. M. Hawsawi;
Page : 914-919
Keywords : Pyrazole; thiazolidine; semicarbazone; -lactam; thiadiazole; selenadiazole; Schiff- bases; antibacterial and antifungal activities;
Abstract
Methyl 5-amino- 3- methylthio-1- phenyl-pyrazole -4- carboxylate 1 was reacted with different aldehydes namely, benzaldehyde, anisaldehyde, p- nitrobenzaldehyde, p-chlorobenzaldehyde and p-bromobenzaldehyde in the presence of glacial acetic acid at refluxed temperature afforded the corresponding Schiff- bases 2 (a-e), which on reaction with each of chloroacetyl chloride and thioglycolic acid gave the corresponding -lactam derivatives 3 (a-e) and thiazolidines 4 (a-e) respectively. N-alkylation of pyrazole derivative 6 was achieved by reaction with chloroacetyl amino acetophenone 5 in refluxing toluene, while the reaction of purified semicarbazone 7 with each of thionyl chloride and selenium dioxide gave the corresponding1, 2, 3- thiadiazole 8 and 1, 2, 3-selenadiazole 9 derivatives. The antibacterial and antifungal activities of some synthesized compounds have been discussed.
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