Preparation and study of the inhibitory activity against bacteria of some substitutes --methyl nicotina mido] 1-3-4-oxada-pazole-2-new thiol

Abstract

In 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.