The pharmacological activity of derivatives of 4-oxo-3,4-dihydroquinazoline and anthranilamides containing a fragment of glycine


  • Yu. O. Ovsjanykova National University of Pharmacy, Ukraine
  • D. V. Levashov National University of Pharmacy, Ukraine
  • V. M. Kravchenko National University of Pharmacy, Ukraine
  • V. P. Chernykh National University of Pharmacy, Ukraine
  • L. A. Shemchuk National University of Pharmacy, Ukraine



quinazolone, anthranilamide, antidepressant effect, anticonvulsant activity, hypnotic activity


Derivatives of 4-oxo-3,4-dihydroquinazoline are known as a promising class of compounds due to their wide spectrum of the pharmacological activity. Taking into account the PASS data for the substituted anthranilamides synthesized, as well as derivatives of 4-oxo-3,4-dihydroquinazoline containing an “in-built” fragment of amino acid glycine as a pharmacophore, the decision to study their central neurotropic effects was made. While studying the hypnotic, anticonvulsant and antidepressant activities the highest antidepressant properties of N-(1,1-diphenyl-1-hydroxyet-2-yl)-N'-diphenylhydroxyacetylanthranilamide (compound 4) have been determined, this compound is slightly inferior the reference drug Imipramine. N-(phenylhydrazidoacetyl)-N'-succinamidoanthranilamide (compound 1) reveals high anticonvulsant properties and is not inferior the classical anticonvulsant drug Depakine. When studying the hypnotic effect the antagonism with Barbamyl for 2-(4-oxo-3,4-dihydro-3-quinazolinyl)acetohydrazide (compound 5) has been found. Methyl-(2-methylcarbonyloxymethyl-4-oxo-3,4-dihydro-3-quinazolinyl)acetate (compound 8) decreased the latent period of “falling asleep” for animals in 1.6 and 1.7 times in the doses of 20 and 200 mg/kg, respectively (the same level with the reference drug), and therefore, it is a promising compound for further research of the hypnotic activity. The analysis of the “structure-activity” relationship gives the possibility to assume that such pronounced pharmacological activity is due to the presence of substituents in position 2 of the quinazoline nucleus. Therefore, the data obtained prove that the study of these derivatives is promising for further search of new biologically active substances with hypnotic, anticonvulsant and antidepressant properties.

Author Biographies

Yu. O. Ovsjanykova, National University of Pharmacy

Post-graduate student

D. V. Levashov, National University of Pharmacy

Assistant of the Organic Chemistry Department

V. M. Kravchenko, National University of Pharmacy

Professor of Human Physiology and Anatomy Department

V. P. Chernykh, National University of Pharmacy


L. A. Shemchuk, National University of Pharmacy

Head of the Organic Chemistry Department


Головенко М.Я., Громов Л.О. Доклінічне вивчення специфічної активності потенційних проти судомних препаратів: Метод. рекоменд. – К.: Авіценна, 2003. – 26 с.

Миронов А.Н., Кукес В.Г. Руководство по проведению доклинических исследований лекарственных средств. Ч. I. – М.: Гриф и К, 2012. – 244 с.

Manoj K., Srivastava S., Bharati M., Nizamuddin N. // Ind. J. Chem. – 2001. – Vol. 40. – P. 342-344.

Perumal P., Bilal A.R., Dontireddy R.S.R., Natesh R.K. // Eur. J. of Med. Chemistry. – 2009. – Vol. 44. – P. 2328-2333.

Porsolt R.D., Lenegre A., Elliot J.M. et al. // Experimental Approaches to Anxiety and Depression. – Chichester New York, 1992. – P. 73-85.

Sarvesh K.P., Abhishek S., Ashutosh S. // Eur. J. Med. Chem. – 2009. – Vol. 44. – P. 1188-1197.

Shemchuk L.A., Al-Asri Jamil M., Levashov D.V. et al. // Вісник Фармації. – 2011. – №3. – С. 30-32.

Shemchuk L.A., Levashov D.V., Al-Asri Jamil M. et al. // ЖОФХ. – 2011. – Т. 8, №9. – С. 36-39.

Shisokoo J., Shirsath S., Rathod J.S., Yande O. // Eur. J. Med. Chem. – 2000. – Vol. 35. – №3. – P. 351-358.

Usifoh C.O., Scriba K.E. // Med. Chem. – 2000. – Vol. 333. – P. 261-266.






Experimental and Clinical Pharmacology