Nitroimidazoles, Part XXIII--activity of satranidazole series against anaerobic infections.
Indian J Exp Biol
; 1992 Mar; 30(3): 193-200
Article
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| ID: sea-63124
ABSTRACT
A large number of nitroimidazoles have been examined for in vitro activity against three anaerobes - Bacteroides fragilis (Bf), a strain of Bf resistant to metronidazole (16a) and Clostridium perfringens and many found to be active. Among these may be mentioned 1-methyl-5-nitroimidazoles carrying N - bound hetetocycles at position 2, such as satranidazole 1a, 1b, 1c, 1k, 1n and 1v which are at least twice as active as metronidazole (16a), ornidazole (16b) and tinidazole (16c). Even more active are 5-nitroimidazolyl benzimidazole 5d, -thiazolidinone 6b and thiadiazolidine dioxide 8a. Many other types of compounds derived from 1-methyl-2-amino-5-nitroimidazole are feebly active. Among 5-nitroimidazoles with a carbon substituent at position 2, 16a, 16b and 16c are equiactive while dimetridazole 14f is more active than 16a against Bf. Some 2-vinyl derivatives are very potent, with 18f and 18i being outstanding. Activity better than that of metronidazole is seen for nitroimidazooxazepines, e.g. 29d. 5-Nitroimidazoles are more active against anaerobes than 4-nitro isomers. Antianaerobic and antiamoebic activities generally run parallel in these classes of compounds. The study has led to the elaboration of the antianaerobic profile of satranidazole 1a.
Полный текст:
1
База данных:
IMSEAR
Основная тема:
Structure-Activity Relationship
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Bacteria, Anaerobic
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Bacterial Infections
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Bacteroides fragilis
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Microbial Sensitivity Tests
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Clostridium perfringens
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Amebicides
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Nitroimidazoles
Язык:
En
Журнал:
Indian J Exp Biol
Год:
1992
Тип:
Article