Derivatives of 4-aminoquinoline have, as is well known, considerable antimalarial activity. The first representative of this series, 4-(8-diethylammo-a-methylbutylamino)-6-methoxyquinoline, obtained by one of us in collaboration with O. Y. Magidson in 19371 possessed antimalarial activity very similar to that of quinine.2Later, 4-(8-diethylamino-a-methylbutylamino)-7-chloroquinoline (chloroquine)3 was synthesized, which is even more active and can be used not only in malaria but also in the treatment of lupus erythematosus and of amcebal liver abscesses.In contrast to the derivatives of 4-amino quinoline, the corresponding derivatives of 4-aminoquinaldine have no antimalarial properties.1 Thus, the introduction of a methyl group into the 2-position of the quinoline nucleus abolishes chemotherapeutic activity in these compounds. However, as it was shown by our studies, conversion of 4-aminoquinaldines to the corresponding 2-styrylquinolines re-established and even increased antimalarial properties. Furthermore, we observed that such 2-styrylquinoline derivatives have pronounced activity not only against protozoa but also against bacteria, actinomycetes and fungi. This latter observation prompted us to extend the investigation of compounds of this class and to synthesize series of derivatives of 6-methoxy-and 7-chloro-2-styrylquinolines, with different substituents in the styryl group and in position 4 of the quinoline nucleus. The compounds obtained are listed in Tables I, II, and III.The styrylquinolines were prepared by condensation of the 8 113
Application examples are described for eucalimin -a medicinal plant preparation possessing antimicrobial and antiinflammatory properties, which is used in combined therapy of acute and chronic pyoinflammatory processes of the respiratory tract, for the treatment of staphylococcal and streptococcal pyodermia, acne simplex, stomatitis, periodontitis, as well as in gynecology, proctology, and surgery.
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