Yoshio Igarashi

Antimicrobial activities of some N-alkylmaleimides.

SummaryA variety ofN-alkylmaleimides have been prepared and screened for antimicrobial activity using various fungi, yeasts and bacteria.N-Methyl,N-octyl andN-decylmaleimide showed antifungal activities. All test compounds showed antibacterial activity.

Antimicrobial activities of 2-arylthio-N-alkylmaleimides

SummaryA variety of 2-arylthio-N-alkylmaleimides were prepared, and their antimicrobial activities were examined. Almost all of these compounds exhibited antibacterial activity against Gram-positive bacteria such asBacillus subtilis andStaphylococcus aureus. Some compounds such as 2-(halogeno-phenyl)-thio-N-methylmaleimides (4, 5, 6, 8 and 10) and 2-(2-carbamoylphenyl)thio-N-methylmaleimide(35) exhibited antibacterial activity againstEscherichia coli. All compounds tested were inactive againstPseudomonas aeruginosa except 2-(2-carbamoylphenyl)thio-N-methylmaleimide(35) which was marginally active. Activities against Gram-positive bacteria were not due to the effect of the substituent on the benzene ring, except in the instances 2-carboxy, 2-carbomethoxy, 2-amino groups and alkyl chains, however, activities against Gram-negative bacteria were due to phenylthio and the alkyl substituents. Some of 2-arylthio-N-alkylmaleimides were examined for their antifungal activities using eight strains of fungi, and they showed activity against these.

Lipase-mediated kinetic resolution of cis-1,2-indandiol and the Ritter reaction of its mono-acetate

Abstract Lipase-mediated kinetic resolution of cis -1,2-indandiol 5 in the presence of lipase PS was examined. Enantiomerically enriched (1 S ,2 R )-2-acetoxy-1-indanol 6a was obtained when cis -1,2-indandiol 5 was treated with one equivalent of vinyl acetate. Treatment of 5 with two equivalents of vinyl acetate furnished a mixture of (1 R ,2 S )-2-acetoxy-1-indanol 6a and (1 R ,2 S )-1-acetoxy-2-indanol 6b . A route to both enantiomers of 1 was also developed by using the enantiomerically enriched mono-acetate thus obtained.