A series of D-erythro ceramide analogues, N-(2S, 3R, 4E)-1, 3-dihydroxy-5-phenyl pent-4-en-2-yl alkyl sulfonamides, were synthesized and evaluated for their in vitro cytotoxic activities against five human tumor cell lines. The aromatic sulfon amido ceramide analogue (10f) showed more potent cytotoxic activity than that of the B13, indicating that a sulfonamide group appears to serve as a bioisostere of an amide in drug design. Variations in the alkyl sulfonyl chain length significantly influenced the cytotoxic activity of the sulfonamido ceramide analogues, but the introduction of a para halogen on the phenyl ring of aromatic ceramide analogues had no affect on the activity.

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The antibacterial activity of novel beta-lactamase inhibitors, 6-exomethylene penamsulfones (CH1240, CH2140), has been compared in vivo with that of sulbactam and clavulanic acid against beta-lactamase producing strains. In vivo microbiological assessment was used as experimental mouse infection model by gram negative strains. Against Pseudomonas aeruginosa F0013, cefoperazone/CH1240 was slightly less active than sulbactam. Ampicillin/CH1240 was more active than sulbactam against Citrobacter diversus species. That of ampicillin/CH2140 was less effective than sulbactam against Escheriachia coli 3457. Especially against Citrobacter diversus 2046E, amoxicillin/CH2140 was the most potent and amoxicillin/CH1240 was slightly more active than clavulanic acid. Consequently the difference in efficacy between the drug combinations appears to be related to the degree of protection afforded the animals by the beta-lactamase inhibitors. CH1240 and CH2140 are promising new agents and should undergo further investigations.