تحضير ودراسة الفعالية التثبيطية ضد البكتريا لبعض معوضات 5-[N-مثيل نيكوتيناميدو]-4،3،1-اوكسادايازول-2-ثايول الجديدة

Abstract

AbstractIn this paper the synthesis of some 5-substituted-1,3,4-oxadiazole-2-thiol is reported. The reaction of nicotinic acid with thionyl chloride gave nicotinyl chloride, which then treated with amino acid esters (obtained from alanine, valine and phenyl alanine) to give amino acid esters of nicotinic acid.The resultant esters were treated with hydrazine hydrate in ethanol to give the corresponding hydrazides. The synthesized hydrazides were converted to disubstituted 1,3,4-oxadiazoles by their reaction with carbon disulfide in ethanolic potassium hydroxide.The influence of the synthesized esters, hydrazides and 1,3,4-oxadiazoles on growth of nine types of bacteria and the comparison of the result of the biological test with known drugs (Oxacilline, Ampicillin and Cephalaxine) was shown that these compounds have a bactericide properties.The activity of the synthesized compounds on dental plaque, Lactobacillus SPP, Streptococcus SPP and Neisseria lattarhalis) was studied. Whereas these compounds did not show any poisonous effects on rats of type BALB/c.The structures of the synthesized compounds were confirmed by H1NMR, IR, UV spectrum and CHN microanalysis as well as physical means.