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Pharmaceutical Chemistry Journal, Vol. 54, No. 2, May, 2020 (Russian Original Vol. 54, No. 2, February, 2020)

SYNTHESIS AND ANTIMYCOBACTERIAL ACTIVITY OF 5-(HETARYLMETHYLIDENE)-2,4,6-PYRIMIDINE2,4,6(1H,3H,5H )-TRIONES AND 5-(2-CHLOROPROPYLIDENE)2,4,6-PYRIMIDINE-2,4,6(1H,3H,5H )-TRIONES M. Yu. Yushin,1 A. G. Tyrkov,2,* L. V. Saroyants,1 N. M. Gabitova,1,3 A. V. Khrapova,1,4 G. N. Genatullina,1,3 and A. K. Ayupova1,2 Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 54, No. 2, pp. 32 – 35, February, 2020.

Original article submitted November 25, 2019. Series of 5-(hetarylmethylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones and 5-(2-chloropropylidene)2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones were synthesized and tested for antimycobacterial activity against M. lufu and acute toxicity. The 5-(hetarylmethylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones and 5-(2-chloropropylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones were shown to possess low toxicity and antimycobacterial activity of various strengths as compared to dapsone and could be considered promising compounds for further discovery of antimycobacterial drugs. Keywords: synthesis, 5-(hetarylmethylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones, 5-(2-chloropropylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones, antimycobacterial activity, minimum inhibitory and bactericidal concentrations, acute toxicity.

Improvement of etiotropic therapy remains a very important issue of modern leprology because the arsenal of antileprotic drugs is limited practically to dapsone, rifampicin, and Lamprene® (clofazimine) [1, 2]. Moreover, all antileprotic drugs have side effects and relatively high toxicity [3 – 5]. Therefore, the search for new compounds with antimycobacterial activity and low toxicity remains critical. Currently, the search for such compounds is aimed at pyrimidine derivatives. Series of experiments established that compounds of this class possess anabolic activity, exhibit anti-inflammatory action, accelerate reparative regeneration, stimulate cellular and humoral immune factors, activate leuko- and erythropoiesis, and are effective as antiviral, antitumor, and other agents [6]. Recently, our research has taken this direction, in particular, the antimycobacterial activity of substituted 2-nitro-1-(4-toluenesulfonyl)-2-[3-methyl(phenyl)-1, 2, 4-oxadia 1 2 3 4 *

zol-5-yl]ethanes and 5-(arylmethylene)hexahydropyrimidine-2,4,6-triones was demonstrated and their acute toxicities for M. lufu were determined [7, 8]. In continuation of research in this direction, new 5-(hetarylmethylidene)-2,4,6pyrimidine-2,4,6(1H,3H,5H)-triones (VII-XI) and 5-(2-chloropropylidene)-2,4,6-pyrimidine-2,4,6(1H,3H,5H)-triones (XIII and XIV) were synthesized by us and tested for antimycobacterial activity and acute toxicity.

II – VI VII – XI

XII I

Leprosy Research Institute, Ministry of Health of the RF, Astrakhan, 414057 Russia. Astrakhan State University, Astrakhan, 414056 Russia. Astrakhan State Medical University, Astrakhan, 414024 Russia. Astrakhan State Technical Univer

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