Synthesis and antifungal activity of N-(alkyl/aryl)-2-(3-oxo-1,4- benzothiazin-2-yl)acetamide
A series of N-(alkyl/aryl)-2-(3-oxo-1,4-benzothiazin-2-yl)acetamide have been synthesized by condensation of substituted amines with maleic anhydride (MA) followed by cyclization with o-aminothiophenol (o-ATP). All the compounds have been screened for their antifungal activity against Tricophyton rubrum, Epidermophyton floccosum and Malassazia furfur. In the primary screening, some of the compounds exhibited appreciable activity. The structures of the synthesized compounds 7a-z have been established on the basis of elemental analysis and spectral data.
Gupta,Wagh
p. 697 - 702
(2007/10/03)
Suppression of food intake in Triatoma infestans by N-substituted methyl maleamates
A series of methyl esters of N-substituted (Z)- and (E)-maleamic acids were synthesized and their effect on food intake measured on fifth-instar nymphs of Triatoma infestans. Suppression of food intake was found only for the (Z)isomers. The initial reaction rate of the synthesized compounds with glutathione (GSH) was calculated from the reaction in vitro of the (z)-isomers. No reaction was observed with the (E)-isomers. Good correlation between the suppression of food intake, measured by its ED50 (effective dose that inhibited feeding of 50% of the population) and the initial reaction rate with GSH and the hydrophobic parameter π, was found.
Audino,Masuh,De Licastro,Vassena,Picollo,Zerba
p. 339 - 343
(2007/10/03)
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