Anti-leishmanial lepidine derivatives

Details Anti-leishmanial lepidine derivatives Anti-leishmanial lepidine derivatives

1978-03-13

1980-06-24

Robinson, Allen J.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

546171, A61K 3147

Patent

active

042095190

ABSTRACT:
The subject 8-amino-6-methoxy lepidine derivatives have the formula: ##STR1## wherein, R represents an --alkylene (tertiary) amine, --alkylene-NH.sub.2, (N-alkylsubstituted piperadyl amino)-alkylene-, --alkylene-(tertiary) amine or --alkylene-N-heterocyclic; R.sub.1, represents an alkoxy, alkyl, halogenated alkyl, alkenyl, aryloxy, halogen or hydrogen radical; R.sub.2 represents an alkyl, halogenated alkyl or aryloxy; n represents integers 3, 4, 5, 6 or 7; and pharmaceutically acceptable salts thereof wherein the salt forming acid or acid-hydrate is organic or inorganic. These derivatives afford improvement in means for the chemotherapy of leishmaniasis. Presence of a basic sidechain attachment at position 8- provides means for enhancement of the effectiveness of such compounds, which may be administered parenterally or orally to infected animals.

REFERENCES:
patent: 2508937 (1950-05-01), Campbell
patent: 3142679 (1964-07-01), Barrett et al.
Shetty et al., J. of Med. Chem. (1977), vol. 20, #10, pp. 1349-1351.
Beveridge et al., "Nature", vol. 182 (1958), pp. 316-317.
Shetty et al., J. of Med. Chem. vol. 21, #9 (1978), pp. 995-998.
La Montagne et al., J. Med. Chem. vol. 20, #9 (1977), pp. 1122-1125.

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