Microbiological Evaluation of 4-substituted-imidazolidine Derivatives
In the present studies, two series of 4-substituted-imidazolidines (IIIa-i and IIIj,k) were synthesized by reacting different tetrahydro-di-Schiff bases (IIa-i and IIj,k) with p-diethylaminobenzaldehyde/ dimethylaminobenzaldehyde. The title compounds were evaluated for their antibacterial and antifungal actions against some selected microbes. The results of microbiological evaluation revealed that two compounds, 4-(1,3-bis(benzo[d][1,3]dioxol-5-ylmethyl)-4-methylimidazolidin-2-yl)-N,N-diethyl aniline (IIIj), 4-(1,3-bis(benzo[d][1,3]dioxol-5-ylmethyl)-4-methylimidazolidin-2-yl)-N,N-dimethyl aniline (IIIk) were good in their antibacterial as well as antifungal actions. Minimum inhibitory concentration values (MIC) of the compounds are reported.
Synthesis of novel tetrahydroimidazole derivatives and studies for their biological properties.
Ethylenediamine was reacted with suitable aromatic aldehydes in order to prepare their respective diSchiff bases. These compounds were then reduced to give the corresponding tetrahydrodiSchiff bases, which were low melting in nature. Finally, these derivatives were condensed with different aromatic aldehydes to give the desired tetrahydroimidazoles. The structures of all these compounds were established on the basis of spectral data. These novel tetrahydroimidazoles showed promising anti-inflammatory and analgesic activity. The compounds were also screened for their anti-bacterial property against Staphylococcus aureus and Escherichia coli.
Synthesis and anti-filarial activity of 6-(3-aminophenyl)-2,3,5,6-tetrahydroimidazol[2,1-b]thiazole derivatives
Abstract Structure activity studies against filariae are described for a series of derivatives of 6-(3-aminophenyl)-2,3,5,6-tetrahydroimidazo[2,1- b ]thiazole ( 15 derivatives. In an in vivo assay using gerbils implanted with both Acanthocheilonema viteae and Brugia pahangi , the former parasite was shown to be the more sensitive to a range of amides of 15 . None of these compounds, however, had any activity at 5 × 10 −5 mol against the worms in vitro suggesting that they required in vivo activation. This was confirmed when the benzamido derivative ( 6 ) was shown to be rapidly metabolised in gerbils to the parent amine ( 15 ). The latter had potent effects on filariae both in vivo and in vitro but was also found to be toxic to mammals and unsuitable for further development. Unsuccessful attempts to improve upon the therapeutic index of 15 through the synthesis of various novel analogues are described.