Investigation of actoprotective activity in a range of 6-N-R-tetrazolo[1,5-c]quinazolin-5(6H)-ones

Authors

  • O. M. Antypenko Zaporizhzhia State Medical University,
  • S. I. Kovalenko Zaporizhzhia State Medical University,
  • S. D. Trzhetsinsky Zaporizhzhia State Medical University,

DOI:

https://doi.org/10.14739/2310-1210.2016.1.64023

Keywords:

6-N-R-Tetrazolo[1, 5-c]quinazolin-5(6H)-ones, Actoprotective Activity, Normothermia, Hypothermia

Abstract

The pace of life in the XXI century often leads to mental and physical fatigue, which can be neutralized by drugs, namely actoprotectors.

Aim. To find compounds able to increase physical endurance among 6-N-R-tetrazolo[1,5-c]quinazolin-5(6H)-ones, which are promising in this regard.

Methods and results. Actoprotective activity was tested on Wistar white rats by swimming test with the extra weight. It was found, that compounds, intragastrically administrated in 50 mg/kg, increased the duration of swimming in conditions of normothermia and hypothermia.

Conclusion. Rats’ swimming duration compared with control has increased for compounds 1, 4 and 7 to 55.50%, 42.36% and 22.92% against 22.20% of «Mildronate». The leading compound was revealed, namely, 6-methyltetrazolo[1,5-c]quinazolin-5(6H)-one, which exceeded the activity of reference drug in the normothermia and hypothermia. And it has been established, that sulfur in the 5th position of tetrazolo[1,5-c]quinazoline is a key element in exhibiting the actoprotective activity.

References

Mashkovskij, M. D. (2006) Lekarstvennye sredstva [Drugs]. Moscow: Novaya volna. [in Russian].

Tozyuk, E. Yu., Stepanyuk, G. I., Chernoivan, N. H. (2013) Sravnitel′naya kharakteristika vliyaniya natriya 2-(tetrazolo[1,5-s]khinazolin-5-iltio)acetata i bemitila na fizicheskuyu vynoslivost′ krys v usloviyakh dlitel′noj gipokinezii [Comparative characteristics of influence of sodium 2-(tetrazolo[1,5-c]quinazoline-5-ylthio)acetate and bemithylum on rats physical endurance in conditions of chronic hypokinesia]. Chelovek i ego zdorov′e, 4, 46–49. [in Russian].

Stepaniuk, H. I., Toziuk, O. Yu., Voskoboinik, O. Yu., Kovalenko, S. I., & Chornoivan, N. H. (2012) Skryninh aktoprotektornoi aktyvnosti v riadu novykh pokhidnykh 5-R-tio-tetrazolo[1,5-s]khinazolinu [Screening of actoprotective activity in a series of new derivatives of 5-R-thio-tetrazolo[1,5-c]quinazoline]. Farmakolohiia ta likarska toksykolohiia, 5(30), 59–61. [in Ukrainian].

Shugalei, I., Ilyushin, M., Sokolova, V., Dubjago, N., Bachurina, I., & Garabadzhiu, A. (2013) Complex copper compounds with pentaaminotetrazole are the new challenge in treatment and prevention of free-radical conditions. Chem. J. Moldovа, 8(1), 6–13.

Kale, M. A., & Peharkar, M. R. (2013) Synthesis of some novel tetrazole substituted benzimidazoles and their evaluation as antioxidants. Int. J. Pharm. Bio. Sci., 4(4), 675–681.

Rasina, L. N., Charushin, V. N., Kotovskaya, S. K., & Orekhova, N. A. (2013) Vliyanie novykh proizvodnykh tiazola i tetrazola na antioksidantnyi status u prirodnykh populyacij myshej s povyshennym soderzhaniem 90Sr [Impact of new derivatives of triazole and tetrazole in the antioxidant status in natural populations of mice with a high content of 90Sr]. Radiacionnaya biologiya. Raduoe′kologiya, 53(5), 506–512. [in Russian].

Shamsuzzaman, M., Asif, A., Ali, A., Mashrai, H., Khanam, A., & Sherwani, M. (2014) Owais. Design, synthesis and biological evaluation of steroidal tetrazoles as antiproliferative and antioxidant agents. Eur. Chem. Bull., 3(11), 1075–1080.

Kaushik, N., Kumar, N., & Kumar, A. (2015) Synthesis of substituted 5-phenyl-1-(5-phenyl)-isoxazol-3-yl)-1H-tetrazole as antioxidant agents. J. Adv. Sci. Res., 6(1), 14–19.

Shneshil, M. K., Ibraheem, T. K., & Jamal, M. Y. (2014) Synthesis and antioxidant activity of 1-(1,2,3,4-tetrazol-2-yl-diazenyl)-4-(substituted benzylideneamino). J. Appl. Chem., 3(6), 2312–2317.

Kozhemiakin, Yu. M., Khromov, O. S., Filonenko, M. A.,. Saifetdinova, H. A. (2002) Naukovo-metodychni rekomendatsii z utrymannia laboratornykh tvaryn ta roboty z nymy [Scientific guidelines for keeping laboratory animals and working with them]. Kyiv: Avitsena. [in Ukrainian].

Zapadnyuk, I. P., Zapadniuk, V. I., Zakhariya, E. A., Zapadnyuk, B. V. (1983) Laboratornye zhivotnye. Razvedenie, soderzhanie, ispol′zovanie v e′ksperimente [Laboratory animals. Breeding, maintenance, use in the experiment]. Kyiv. [in Ukrainian].

Nakaz Ministerstva okhorony zdorov’ia Ukrainy «Poriadok provedennia doklinichnoho vyvchennia likarskykh zasobiv ta ekspertyzy materialiv doklinichnoho vyvchennia likarskykh zasobiv» vid 14.12.2009 r. №944. [Order of the Ministry of Health of Ukraine "Procedure for conducting the pre-clinical study of medicinal products and the expertise of pre-clinical study of medicinal products" December, 14, 2009, №944] [in Ukrainian].

(1986) European convention for the protection of vertebrate animal used for experimental and other scientific purposes. Strasbourg.

Bobkov, Yu. H., Vinogradov, V. I., Katkov, V. F., Losev, S. S., & Smirnov, A. V. (1984) Farmakologicheskaya korrekciya utomleniya [Pharmacological correction of fatigue]. Moscow: Medicina. [in Russian].

Stepaniuk, H. I., Toziuk, O. Yu., Chornoivan, N. H., Kovalenko, S. I., & Voskoboinikov, O. Yu. (2012) Vplyv pokhidnykh tetrazolo[1,5-s]khinazolinu na fizychnu vytryvalist shchuriv pry riznykh temperaturnykh rezhymakh [The influence of tetrazolo[1,5-c]quinazoline derivatives on the physical endurance at different temperatures]. Ukrainskyi zhurnal klinichnoi ta laboratornoi medytsyny, 7(4), 81–85. [in Ukrainian].

Mironov, A. N., Bunatyan, N. D., Vasil′ev, A. N., Verstakova, O. L., Zhuravleva, M. V., Lepakhin, V. K., et al. (2012) Rukovodstvo po provedeniyu doklinicheskikh issledovanij lekarstvennykh sredstv [Guidelines for drugs preclinical studies]. Moscow: Grif i K. [in Russian].

Kornienko, V. I., Shikova, V. V., Samura, B. A., Romanenko, N. I., & Rak, T. N. (2012) Vliyanie ammonievykh solej N-(3-metil-7-atsetilmetil-ksantinil)-8-N-zameshchennykh piperaziniya na vinoslivost′ kris k fizicheskim nagruzkam [Effect of ammonium salt of N-(3-methyl-7-acetylmethyl-xanthine)-8-N-substituted of piperazine at rats physical endurance]. Problemy ekolohichnoi ta medychnoi henetyky i klinichnoi imunolohii, 6, 385–391. [in Ukrainian].

Kornienko, V. I. (2013) Issledovanie vliyaniya ammonievykh solej N-(3-metil-7-β-metoksietilksantinil)-8-aminoacetata na fizicheskuyu rabotosposobnost' krys [Investigation of the effect of ammonium salts of N-(3-methyl-7-β-methoxyetylksantinil)-8-aminoacetate at rats physical endurance]. Ukrainskyi biofarmatsevtychnyi zhurnal, 1, 19–22. [in Ukrainian].

Dunaev, V. V., Belenichev, I. F., Kovalenko, S. I., Mazur, I. A., Sinyak, R. S., Bashkin, I. N., et al. (1993) Antioksidantnaya aktivnost′ novogo proizvodnogo 4-gidrazinokhinazolina pri e′ksperimental′noj gipoksii golovnogo mozga [The antioxidant activity of a novel 4-hydrazinoquinazoline derivative in experimental cerebral hypoxia]. Ukrainskyi biofarmatsevtychnyi zhurnal, 65(3), 118–120. [in Ukrainian].

Belenichev, I. F., Kovalenko, S. I., Dunaiev, V. V., Bukhtiiarova, N. V., & Yatsun, V. V. (2000) Doslidzhennia farmako-biokhimichnykh mekhanizmiv antyoksydantnoi dii N-(4-khinazolil)aminoarylkarbonovykh kyslot ta yikh solei v umovakh initsiiuvannia vilno radykalnykh protsesiv in vitro ta modeliuvannia ishemii holovnoho mozku [Research of pharmaco-biochemical mechanisms of antioxidant action of N-(4-quinazolil)aminoarylcarboxylic acids and their salts in terms of initiating free radical processes in vitro and simulation cerebral ischemia]. Liky, 3(4), 65–69. [in Ukrainian].

Kolalenko, S. I., Belenichev, I. F., & Bukhtiyarova, N. V. (2004) Proizvodnye khinazolina – perspektivnye nejroprotektivnye sredstva s antioksidantnym mekhanizmom dejstviya [Quinoline derivatives - promising neuroprotective agents with antioxidant mechanism of action]. Zaporozhskij medicinskij zhurnal, 2(1), 9–15. [in Ukrainian].

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How to Cite

1.
Antypenko OM, Kovalenko SI, Trzhetsinsky SD. Investigation of actoprotective activity in a range of 6-N-R-tetrazolo[1,5-c]quinazolin-5(6H)-ones. Zaporozhye Medical Journal [Internet]. 2016Mar.25 [cited 2024Nov.4];18(1). Available from: http://zmj.zsmu.edu.ua/article/view/64023

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Section

Problems of pharmacy