Antimicrobial therapy is a significant element of modern medical and pharmaceutical practice. To create more effective medicines the researches are carried out among different classes of organic substances. One of the key strategies in this field is combination of several pharmacophores in a single molecule. In this aspect, the authors´ attention was attracted derivatives xantina, with a wide range of paid activity, and the large variability of the possibility of chemical modification. Objects of the study were derivatives of 3-benzyl-8-methylxanthinyl-7-acetic acid, synthesized by authors´ group previously. Antibacterial properties of these compounds were studied on Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and antifungal activity on Candida albicans. It was found that the most active against Staphylococcus aureus compound was substance A-18, which according to this indicator significantly exceeded the Ampicillin. Compounds A-4, A-9, A-ll, A-13, A-19 by antistaphylococcal activity are not inferior to the Am-picillin. Ylidenhydrazide A-16 and S-substituted triazolylmethylxanthines A-22 and A-23 - surpassed it. It was also found that hydra-zide A-3, ylidenhydrazides A-6, A-ll - A-14 and A-17 showed fungistatic properties comparable to the Nystatin.
derivatives of 3-benzylxanthine, bacteriostatic activity, antifungal action
Антимикробная терапия является весомым звеном современной медицинской практики. Большое количество разнообразных схем лечения используют широкий арсенал антибактериальных лекарственных стредств [3]. При лечении инфекционных заболеваний используются природные и полусинтетические антибиотики, а отдельные антибактериальные препараты получают путем целенаправленного химического синтеза [2]. Несмотря на высокую избирательность действия, антибиотики вызывают ряд побочных эффектов: аллергические реакции, суперинфекции (дисбактериоз, ослабление иммунитета) и токсические явления (диспепсию, флебиты, нарушения функции печени, почек и др.) [6].
В связи с этим, а также с возникновением новых резистентных форм возбудителей инфекционного процесса, существенной проблемой современной медицины является дальнейшее усовершенствование терапии инфекционных
1. Kireev IV. Issledovanie antibakterial´noy i fungistati-cheskoy aktivnosti zameshchennykh i annelirovannykh proizvod-nykh ksantina. Visnik SumDU, Seriya Meditsina. 2009;1:22-9. Russian.
2. Mashkovskiy MD. Lekarstvennye sredstva. 5 izda-nie. Moscow: Novaya Volna; 2005. Russian.
3. Sleptsov VP. Antimikrobnye preparáty v prakticheskoy meditsine: prakticheskoe rukovodstvo. 3 izdanie. Simferopol; 2009. Russian.
4. Volyans´kiy YuL, Gritsenko IS, Shirobokov VP. Metodichni rekomendatsi´i «Vivchennya spetsifichno´i aktivnosti protimikrobnikh likars´kikh zasobiv». Kiev: DFTs MOZ Ukra´ini; 2004. Russian.
5. Levich SV, Shkoda OS, Aleksandrova KV. Sintez ta fiziko-khimichni vlastivosti S-zamishchenikh pokhidnikh 3-benzil-8-metil-7-[(4-fenil-5-tio-4H-l,2,4-triazol-3-il)metil] ksan-tinu. Aktual´ni pitaniya farmatsevtichnoï ta medichnoï nauki i praktiki. 2013;ll(l):54-8. Russian.
6. Posokhova KA, Viktorov OP. Antibiotiki (vlastivosti, zastosuvannya, vzaemodiya): Navch. posibnik. Ternopil´: TDMU; 2005. Russian.
7. Shkoda OS, Levich SV, Aleksandrova KV. 8-Zamishcheni 3-benzilksantinu yak perspektivní spoluki dlya poshuku biologichno aktivnikh rechovin. Farmatsevtichniy chasopis. 2013;25(l):23-8. Russian.
8. Anandarajagopal K, Anbu Jeba Sunilson J, Illavarasu A, Thangavelpandian N, Kalirajan R. Antiepileptic and antimicrobial activities of novel l-(unsubstituted \substituted)-3,5-dimethyl-lH-pyrazole derivatives. Internation Journal of ChemTech Research. 2010;2:45-9.
9. Bremner JB, Ambrus JI, Samosorn S. Dual action-based aproaches to antibacterial agentse. Curent Medical Chemistry. 2007;14(13):1459-77.
10. Elgaher WA, Hayallah AM, Sálem OIA. Synthesis, Anti-bronchoconstrictive, and antibacterial activities of some new 8-substituted-l,3-dimethylxanthine derivatives. Bull. Pharm. Sci., Assiut University. 2009;32(l):153-87.
11. Hubschwerlen C, Specklin J-L, Sigwalt C. Design, synthesis and biological evaluation of oxazilidinone-quinolone hybrids. Biooraganic and Medicinal Chemistry. 2003;11(10): 2313-19.
12. Kumari Shalini, Nitin Kumar, Sushma Drabu. Advances in synthetic aproach to and antifungal activity of tri-azoles. Beilstein J. Org. Chem. 2011;7:668-77.
13. Prasad DJ, Ashok M, Karegoudar P, Poojary B, Holla BS, Kumari NS. Synthesis and antimicrobial activities of some new triazolothiadiazoles bearing 4-methylthiobenzyl moiety. European J. of Med. Chem. 2009;44(2):551-7.
14. Priadarsini P, Ujwala B, Venkata Rao C, Madhava Rao V. Synthesis and antimicrobial activity of some novel pyra-zoles. Der Pharmacia Lettre. 2012;4(4):1123-8.
