Síntese de novos derivados de sulfonamidas com actividade anticolérica

Abstract

This work is part of a project launched by the Department of Chemistry at UEM for the synthesis of biologically active substances based on sulfonamides, in particular anticholera substances, from sulfanilamide (p-aminobenzenesulfonamide), and is basically aimed at the study of new methods applied to obtain medicines used in modern medical practice. The number of conditions in which sulfonamides are therapeutically useful and constitute the drugs of first choice has been markedly reduced with the development of more effective antimicrobial agents and with the gradual increase of resistance of several species of bacteria to this class of drugs. However, the use of sulfonamides has reappeared as a result of the introduction of their combination with other drugs. It is known that phthalylsulfonamides were the most effective agents in reducing stool volume, intravenous fluid replacement and duration of diarrhea and positive stool cultures. Within a systematic study of sulfonamides, Phthalylsulfacetamides, 3-Nitrophthalylsulphatamides, Diarylsulfonylphthalamides, N-arylsulfonylaminophthalic acids and derivatives of Phtalylaminobenzenesulfonylxaminic acid were synthesized, with potential gram-negative antibacilli properties, in particular Vibrio. The nitro group (-NO2 ) is introduced at the 3 position of the phthalic acid residue with the aim of increasing the anticholeric action in view of the presence of the same group in the Chloramphenicol (I) molecule which is one of the most potent anticholerics. Nowadays, in the treatment of cholera, the use of some Tetracycline (II) derivatives is recommended, especially Doxycycline (substitutes -OH and -H (in place of -CH3) in positions 5 and 6 respectively). There is already information that some strains of Vibrio Cholerae are resistant to Tetracyclines, hence the interest in synthesizing new phthalylsulfonamide derivatives that can be used in combination with other drugs.(TRADUÇÃO NOSSA)