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ChemInform Abstract: Structure-Activity Relationships for the Antileishmanial and Antitrypanosomal Activities of 1′-Substituted 9-Anilinoacridines.

✍ Scribed by S. A. GAMAGE; D. P. FIGGITT; S. J. WOJCIK; R. K. RALPH; A. RANSIJN; J. MAUEL; V. YARDLEY; D. SNOWDON; S. L. CROFT; W. A. DENNY

Publisher
John Wiley and Sons
Year
2010
Weight
28 KB
Volume
28
Category
Article
ISSN
0931-7597

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✦ Synopsis

Structure-Activity Relationships for the Antileishmanial and Antitrypanosomal Activities of 1'-Substituted 9-Anilinoacridines.

-To further develop structure-activity relationships and to improve the effectiveness of this class of drugs a series (45 examples) of analogues of the known lead compound (Ia) is prepared and evaluated against the parasite Leishmania major. The results confirm earlier conclusions that lipophilic electron-donating groups at the 1'-position of 9-anilinoacridines provide high activity. It is indicated that the related 3,6-(NMe2)2 substitution pattern is favorable, leading to the three compounds (Ib) as the most potent derivatives. -(GAMAGE, S.

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