Fumiko Fujisaki

A new route for the synthesis of linezolid mimetic 3,4-disubstituted oxazolidin-2-one derivatives

- New oxazolidin-2-ones (3), which mimic the clinically useful antibacterial agent (1) (Linezolid) were prepared by using a cyclization procedure with diethyl carbonate from aminoalcohol (7) starting with DL-serine methyl ester hydrochloride (4) and aromatic carboxylic acid derivatives (5).

Synthesis and Antibacterial Evaluation of Some New 5-Substituted Hydantoins and Novel Twin-Drug Type Derivatives

Abstract – We report the preparation of new oxygen analogues 2 of twin-drug type bivalent mid-size lead molecule 1 and related single-drug type hydantoin derivatives 3. The new twin-drug type oxygen analogues (2a and 2b) also showed significant antibacterial activity against a Gram-positive strain (S. aureus). A comparison of the two types of twin-drug type mid-size compounds 1 and 2 showed that the original lead 1 had a higher level of antibacterial activity against a Gram-positive strain (S. aureus) than those of the compounds (2a and 2b). We also report the results of antibacterial evaluation of prepared compounds and the investigated structure-activity relationships of these molecules.

Studies on pyrrolizidines and related compounds. Part 9. Rearrangement of 7a-trichloromethyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine and related compounds: an alternative route to 5-substituted 1-azabicyclo[3.3.1]nonanes

Rearrangement of 7a-trichloromethyl-2,3,5,6,7,7a-hexahydro-1H-pyrrolizine and related compounds provides a new synthesis of 1-azabicyclo [3.3.1] nonanes.