Synthesis and In Vitro Antimicrobial SAR of Benzyl and Phenyl Guanidine and Aminoguanidine Hydrazone Derivatives

A series of benzyl, phenyl guanidine, and aminoguandine hydrazone derivatives was designed and in vitro antibacterial activities against two different bacterial strains (Staphylococcus aureus and Escherichia coli) were determined. Several compounds showed potent inhibitory activity against the bacterial strains evaluated, with minimal inhibitory concentration (MIC) values in the low µg/mL range. Of all guanidine derivatives, 3-[2-chloro-3-(trifluoromethyl)]-benzyloxy derivative 9m showed the best potency with MICs of 0.5 µg/mL (S. aureus) and 1 µg/mL (E. coli), respectively. Several aminoguanidine hydrazone derivatives also showed good overall activity. Compounds 10a, 10j, and 10r–s displayed MICs of 4 µg/mL against both S. aureus and E. coli. In the aminoguanidine hydrazone series, 3-(4-trifluoromethyl)-benzyloxy derivative 10d showed the best potency against S. aureus (MIC 1 µg/mL) but was far less active against E. coli (MIC 16 µg/mL). Compound 9m and the para-substituted derivative 9v also showed promising results against two strains of methicillin-resistant Staphylococcus aureus (MRSA). These results provide new and potent structural leads for further antibiotic optimisation strategies.     

Eine neue Reaction auf Galluss?ure

Ohne Zusammenfassung     

Analysis of stop consonant production errors in developmentally dysphasic children

The speech production skills of 12 dysphasic children and of 12 normal children were compared. The dysphasic children were found to have significantly greater difficulty than the normal children in producing stop consonants. In addition, it was found that seven of the dysphasic children, who had difficulty in perceiving initial stop consonants, had greater difficulty in producing stop consonants than the remaining five dysphasic children who showed no such perceptual difficulty. A detailed phonetic analysis indicated that the dysphasic children seldom omitted stops or substituted nonstop for stop consonants. Instead, their errors were predominantly of voicing or place of articulation. Acoustic analyses suggested that the voicing errors were related to lack of precise control over the timing of speech events, specifically, voice onset time for initial stops and vowel duration preceding final stops. The number of voicing errors on final stops, however, was greater than expected on the basis of lack of differentiation of vowel duration alone. They appeared also to be related to a tendency in the dysphasic children to produce final stops with exaggerated aspiration. The possible relationship of poor timing control in speech production in these children and auditory temporal processing deficits in speech perception is discussed.     

Epoxidation of olefins by hydrogen peroxide in the presence of tetrachloroacetone

1,1,3,3-Tetrachloroacetone, an inexpensive, commercially available material, has been shown to be effective in mediating the hydrogen peroxide oxidation of a variety of olefins to epoxides. The chloroacetone is readily recovered for re-use.