Organizing co mmittee

 
 

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Poster presentation 
225 
COMPARATIVE ACUTE TOXICITY OF DERIVATIVES WITH 
1,3,4-OXADIAZOLE-2-THIONE NUCLEUS 
S.Z. Rashidov, Z.I. Sanoev, S.D. Raximboev, I.T. Abdinazarov, T.T. Khamroev,
D.S. Ismailova, B.J. Elmuradov. 
S.Yu. Yunusov Institute of the Chemistry of Plant Substances Academy of sciences of the 
Republic of Uzbekistan st. Mirzo-Ulugbek, 77, 100170 Tashkent 
e-mail: [e-mail]  
There were four different known isomers of oxadiazole, such as of 1,2,4-oxadiazole, 
1,2,3-oxadiazole, 1,2,5-oxadiazole and 1,3,4-oxadiazole. Among them, 1,3,4-
oxadiazoles and 1,2,4-oxadiazoles are well known and more widely studied by 
researchers because of their wide range of chemical and biological properties. The 
presence of toxophoric –N = C–O– linkage in 1,3,4-oxadiazole ring might be 
responsible for their potent pharmacological activities. Among these, substituted 1,3,4-
oxadiazoles are of considerable pharmaceutical interest. 1,3,4-Oxadiazoles have become 
important symptoms in the development of new drugs. Derivatives of the oxadiazole 
nucleus (1,3,4-oxadiazoles) show various biological activities, such as antibacterial, 
antimycobacterial, antitumor, antidepressant, antiviral and antioxidant activity, etc., as 
reported in the literature. 
The acute toxicity of the studied substances was determined on white mongrel 
laboratory mice with a body weight of 22-24 g. In the conducted studies, the acute 
toxicity of the studied substances (LD
50
) was as follows; 5-(
o
-aminophenyl)-1,3,4 - 
oxadiazole-2-tione - 4558 mg/kg, 5-(
m
-aminophenyl)-1,3,4-oxadiazole-2-thione - 1535 
mg/kg, 5-(
p
-aminophenyl)-1,3,4- oxadiazole-2-thione - 3490 mg/kg, potassium salt 5-
(
o
-aminophenyl)-1,3,4-oxadiazole-2-thione - 2725 mg/kg, potassium salt 5-(
p
-
aminophenyl)-1,3,4 - oxadiazole-2-tione - 1975 mg/kg. A noteworthy aspect of these 
indicators was that when the amino group (NH
2
) in the ring was in the ortho, meta and 
para positions showed less toxicity in relation to cases, up to 2,97 and 1,31 times, 
respectively. It was also noted that the derivatives in the ortho- and para positions were 
noted to be less toxic than their potassium salt by 1,67 and 1,77 times, respectively.