Meltem CEYLAN ÜNLÜSOY, Nurten ALTANLAR, Rahmiye ERTAN

Synthesis and Antimicrobial Activities of Some New Flavonyl Pro-drug Esters of Ampicillin

A new series of flavonyl pro-drug esters of ampicillin (Va-b) was prepared by condensing the appropriate bromomethyl flavone with ampicillin trihydrate potassium salt. Flavone derivatives and ampicillin both have good antibacterial activity. The synthesized compounds were tested for their antifungal and antibacterial activities in vitro. Both of the compounds were active against Candida krusei and Staphylococcus aureus.

Anahtar Kelimeler:

Flavone derivatives, Ampicillin, Pro-drug ester, Antimicrobial activities

Synthesis and Antimicrobial Activities of Some New Flavonyl Pro-drug Esters of Ampicillin

Keywords:

Flavone derivatives, Ampicillin, Pro-drug ester, Antimicrobial activities,

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T.J. Mabry, K.R. Markham and M.B. Thomas,. “The Systematic Identification of Flavonoids”, Springer Verlag, NY 83, Berlin-Heidelberg, 1970.
A. Mori, C. Nishino, N. Enoki and S. Tawata, Phytochemistry 26, 2231-34 (1987).
N.B. Perry and L.M. Foster, Planta Medica 60, 491-2 (1994).
C. Conti, D. Genovese, R. Santoro, M.L. Stein, N. Orsi and L. Fiore, Antimic. Agents Chemother. 34, 6 (1990).
D.S. Zaharko, C.K. Grieshaber, J. Plowman and J.C. Cradock, Cancer Treatment Reports 70, 1415-21 (1986).
M. Das and P. K. Ray, Biochemistry International 17, 203-9 (1988).
M. Gabor, Arzneim.-Forsch./Drug Res. 31, 442-5 (1981).
D. Nardi, A. Leonardi, R. Pennini, A. Tajana and R. Cazzulani, Arzneim.-Forsch./Drug Res. 43, 28-34 (1993).
J. Sj¨ovall, B. Huitfeldt, L. Magni and C.E. Nord, Scand. J. Infect. Dis. Suppl. 49, 73-84 (1986).
F. Sakamoto, S. Ikeda and G. Tsukamoto, Chem. Pharm. Bull. 32, 2241-48 (1984).
W.V. Daehne, E. Frederiksen, E. Gundersen, F. Lund, P. Morch, H.J. Petersen, K. Roholt, L. Tybring and W.O. Godtfredsen, J. Med. Chem. 13, 607-612 (1970).
H. Ferres and J.P. Clayton, U.S. Patent No. 3860579 (1972).
B. Ekstr¨om and B. Sj¨oberg, U.S. Patent No. 3939270 (1973).
F. Cramer and G.H. Elsching, Chem. Ber. 89, 1-12 (1956).
M. Tun¸cbilek and R. Ertan, Pharmazie 54, 255-259 (1999).
A.W. Bauer, W.M.M. Kirby, J.C. Sherris and M. Turck, Am. Clin. Pathol. 45, 493-6 (1966).