- Antifungal properties of novel N- and α,β-substituted succinimides against dermatophytes
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The synthesis and antifungal properties of a series of new N-aryl α,β-substituted succinimides against a panel of dermatophytes of clinical relevance are reported. Among those compounds possessing a N-phenyl substituent, 7-thia-2-azabicyclo[2,2,1]hept-2-en-3-amine[5,6-c]succinimide was the better inhibitor of Trichophyton rubrum, the major ethiological agent of all infections produced by dermatophytes. In contrast, succinimides containing a N-(p-sulfonylphenyl) substituent, only inhibited Epidermophyton floccosum, all active compounds possessing an oxabicyclo group in positions α,β of the imide. Substituents on the oxabicyclo group were important for the activity. Regarding the mechanism of action, N-(p-N′-4-methoxyphenylsulfamoylphenyl) -8-oxabicyclo[2,2,1]hept-4-en-3-methyl[5,6-c]succinimide produced a mottled inhibition halo in the Neurospora crassa assay, showing that it would act by inhibiting the synthesis or assembly of the fungal cell wall.
- Lopez, Silvia N.,Sortino, Maximiliano,Escalante, Andrea,De Campos, Fatima,Correa, Rogerio,Cechinel Filho,Nunes, Ricardo J.,Zacchino, Susana A.
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p. 280 - 288
(2007/10/03)
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- Synthesis of new succinimides and sulphonated derivatives with analgesic action in mice
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Recently, we have investigated the chemistry and biology of cyclic imides and have used phyllanthimide to obtain several analogues such as maleimides, succinimides and related compounds, which have demonstrated analgesic activity, amongst other properties. The work presented here describes the synthesis of new succinimides and their sulphonated derivatives. These substances were confirmed as having analgesic activity through abdominal constriction tests in mice. The results showed that some of the compounds, given intraperitoneally at a dose of 10 mg kg-1, were more effective than aspirin and paracetamol.
- Correa,Cechinel Filho,Rosa,Isolani Pereira,Schlemper,Nunes
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- REACTIONS OF N-(p-CHLOROSULFONYLPHENYL)MALEIMIDE
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N-Phenylmaleimide reacted with chlorosulfonic acid to give an excellent yield of the sulfonyl chloride (1), which with dimethylamine or aniline (2 equivs.) afforded the corresponding sulfonamides (2,3).However, use of more dimethylamine (4 equivs.) caused
- Cremlyn, Richard,Nunes, Richardo
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p. 245 - 254
(2007/10/02)
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