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Synthesis and biological activity of some new benzimidazolyl-azetidin-2-ones and -thiazolidin-4-ones.

Arylidene-2-aminobenzimidazoles (1) were prepared by condensation of 2-aminobenzimidazole with aromatic aldehydes. Cyclocondensation of mercaptoacetic acid, chloracetylchloride and phthaloyl glycyl chloride on 1 giving the corresponding 4-thiazolidinones (2) and azetidinones (3 and 4) respectively, in good yields. The biological activities of the prepared compounds were screened against several strains of bacteria.

Anti-Bacterial Agents↗

Synthesis and anticonvulsant activity of new 1-substituted 1'-methyl-3-chloro-2-oxospiro (azetidin-3',4-indol-2' ones).

The aim of the present research work is to discover new compounds with potential anticonvulsant activity. Several indolinone derivatives and also azetidinones are reported to have significantly anticonvulsant activity. So, it was thought considerable to synthesise compounds having both these moieties and study their anticonvulsant activity. The new spiroazetinones synthesized from the reaction of 3-(N-substituted) imino-1-methyl-indol-2-ones with chloroacetyl chloride in presence of triethylamine have been characterised on the basis of triethylamine have been characterised on the basis of satisfactory analytical and spectral data. Of the eight compounds screened in the series two compounds (3c and 3h) exhibited significant activity against MES.

Animals↗

An assessment of the importance of error-prone repair and point mutations to forward mutation to L-azetidine-2-carboxylic acid resistance in Escherichia coli.

By comparison of E. coli WP2 with CM891 (uvrA- pKM101) we found that pKM101 plasmid and uvrA- mutation considerably enhanced both spontaneous and chemically-induced reversion at the trp locus. However, little or no increase was observed for forward mutation at the A2C locus. Furthermore, mutation frequency decline was considerably greater for trp reversion than for mutation to A2Cr. Thus neither error-prone repair nor point mutation seemed likely to be the major mechanism for forward mutation at the A2C locus. Results for spontaneous mutation of recA-, polA- and gyrA- strains showed that polA- and gyrA- gave good increases in forward mutation but not in reversion. It was inferred that deletion, transposition and/or larger chromosomal effects rather than point mutation were mainly responsible for most forward mutation.

Azetidinecarboxylic Acid↗