Poster presentation
224
NEUROTROPIC ACTIVITY OF 5-(P-AMINOPHENYL)-4-AMINO-
1,2,4-TRIAZOLE-3(2H) - THIONE POTASSIUM SALT
S.D. Rakhimboev, Z.I. Sanoev, S.Z. Rashidov, 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: zafarsano19@mail.ru
1,2,4-Triazole is one of the most significant nitrogen-containing scaffolds in the field
of medicinal chemistry due to its diverse biological properties. Among the azoles,
triazoles are the most stable compounds and are difficult to cleave. 1,2,4-Triazoles act
as important pharmacophores by interacting with biological receptors with high affinity
due to their dipole character, hydrogen bonding capacity, rigidity, and solubility. The
1,2,4-triazole nucleus is stable to metabolism and acts as an important pharmacophore
by interacting at the active site of a receptor as a hydrogen bond acceptor and as a
donor. Due to its polar nature, the triazole nucleus can increase the solubility of the
ligand and significantly improve the pharmacological profile of the drug.
Diverse
substitution at the C5 position has been associated with the promising activity of
synthesized oxindole derivatives such as progesterone antagonist, vasopressin
antagonist, anti-Alzheimer, phosphate inhibitor, kinase inhibitor, neuroprotection,
NMDA blocking, and anticancer, antioxidant, antibacterial, and anti-HIV activity.
Taking into account the above, the neurotropic activity of the 5 - (
p
-aminophenyl)- 4
- amino-1,2,4-triazole-3(2H)-thione of potassium salt was studied using several
preclinical research methods under experimental conditions. Neurotropic activity
was
carried out on white mongrel laboratory mice with a body weight of 20-24 g and rates
with a body weight of 180-220 g. stored in quarantine for 14 days in a vivarium. In
experiments, the studied compound was administered orally at doses of 10; 30 and 60
mg/ kg, in these doses increasing motor activity in rats by 2.0; 2.2 and 1.75 and research
activity by 1.2; 1.2 and 1.7, respectively, in relation to the control group by the "open
field" method. However, tremors were caused in white mice and the opposite M-
cholinolytic activity was caused in relation to tremor and salivation when subcutaneous
arecoline was administered at a dose of 10 mg/kg, as well as a weakening at doses of 10
and 30 mg/ kg of motor activity caused by the action of phenamine at a dose of 7 mg/kg
under the skin, while at a dose of 60 mg/kg, the motor activity increased.
Thus, the results obtained in the conducted preliminary screening studies suggest that
in the future a wide range of scientific studies maybe conducted to study the
neurodepressive, sedative and other biological properties of the substance under study.
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