Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1983-08-08
1986-10-28
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514394, 514636, A61K 31405, A61K 31415, A61K 31155
Patent
active
046199420
ABSTRACT:
A number of aromatic mono- and bis-amidines are capable of blocking cell fusion induced by Respiratory Syncytial (RS) virus. Suitable amidino compounds include those selected from the group consisting of 1-4-di(4-amidinophenoxy)-2-butanol; bis(5-amidino-2-benzimidazolyl)methane; 1,2-bis(5-amidino-2-benzimidazolyl )ethane; 5-amidino-indole; 5-amidinobenzimidazole, 5-amidino-1-methylindole and 5-amidino-1-(4-amidinobenzyl)indole. The most powerful of the compounds, bis(5-amidino-2-benzimidazolyl)methane (BABIM), is able to achieve complete suppression of syncytium formation at a concentration of 1 .mu.M. Inhibition occurs in RS virus-infected Hep-2 cells as well as CV-1 cells. BABIM also causes a significant retardation of RS virus penetration, but does not interfere with adsorption. Addition of the amidines after the penetration of RS virus does not affect single cycle yields. The compounds may be used in the prophylactic control of RS virus in man.
REFERENCES:
Chemical Abstracts, 95: 330u (1981).
Tidwell et al., J. Med. Chem., vol. 21, No. 7, 1978, pp. 613-623.
Dubovi Edward J.
Geratz Joachim D.
Tidwell Richard R.
Goldberg Jerome D.
University of North Carolina
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