TY - JOUR
T1 - Synthesis, characterization and biological activity of Schiff bases derived from metronidazole
AU - Saadeh, Haythem A.
AU - Shaireh, Eman A.Abu
AU - Mosleh, Ibrahim M.
AU - Al-Bakri, Amal G.
AU - Mubarak, Mohammad S.
N1 - Funding Information:
Acknowledgments I.M. Mosleh was supported by a joint grant from the Deanship of Scientific Research, The University of Jordan, and Hamdi Manko Center for Scientific Research (HMCSR), The University of Jordan. We also wish to thank Miss Lina Al-Natsheh for the technical assistance and the maintenance of cultures.
PY - 2012/10
Y1 - 2012/10
N2 - A series of novel Schiff bases; compounds 3a- j were prepared by reacting 1-(2-aminoethyl)-2-methyl-5-nitroimidazole dihydrochloride monohydrate (1) with different aldehydes. The structures of these compounds were confirmed through different spectroscopic methods such as 1H-NMR, 13C-NMR and mass spectrometry and also by elemental analyses. The prepared compounds were evaluated in vitro for their antigiardial, antibacterial and antifungal activities. Compounds 3h, 3b and 3d showed remarkable antigiardial activities and were found to be more active than metronidazole with IC 50 of 0.83, 1.36 and 1.83 μM, respectively. Other compounds also exhibited antigiardial activity and were as good as or even more potent than metronidazole. Some of the newly synthesized Schiff bases exhibited more antifungal activities than the parent drug. In addition, a few of the prepared compounds exhibited modest antibacterial activity but were not as active as metronidazole.
AB - A series of novel Schiff bases; compounds 3a- j were prepared by reacting 1-(2-aminoethyl)-2-methyl-5-nitroimidazole dihydrochloride monohydrate (1) with different aldehydes. The structures of these compounds were confirmed through different spectroscopic methods such as 1H-NMR, 13C-NMR and mass spectrometry and also by elemental analyses. The prepared compounds were evaluated in vitro for their antigiardial, antibacterial and antifungal activities. Compounds 3h, 3b and 3d showed remarkable antigiardial activities and were found to be more active than metronidazole with IC 50 of 0.83, 1.36 and 1.83 μM, respectively. Other compounds also exhibited antigiardial activity and were as good as or even more potent than metronidazole. Some of the newly synthesized Schiff bases exhibited more antifungal activities than the parent drug. In addition, a few of the prepared compounds exhibited modest antibacterial activity but were not as active as metronidazole.
KW - Antigiardial activity
KW - Metronidazole
KW - Schiff bases
UR - https://www.scopus.com/pages/publications/84866378217
UR - https://www.scopus.com/pages/publications/84866378217#tab=citedBy
U2 - 10.1007/s00044-011-9830-y
DO - 10.1007/s00044-011-9830-y
M3 - Article
AN - SCOPUS:84866378217
SN - 1054-2523
VL - 21
SP - 2969
EP - 2974
JO - Medicinal Chemistry Research
JF - Medicinal Chemistry Research
IS - 10
ER -