Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1984-07-18
1986-06-17
Daus, Donald G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544311, 548239, 549479, 560 17, 560106, 562557, 564440, A61K 31505, C07D23910
Patent
active
045956871
ABSTRACT:
Sparsomycin derivatives of the formula ##STR1## wherein X and Y are each independently an oxo or an imino group; n is 0 or the integer 1 or 2; R.sub.1 is a hydrogen or 1 to 4 carbon alkyl group; R.sub.2 is a hydrogen, a 1 to 4 carbon alkyl, a 2 to 5 carbon acyl or a benzoyl group; and R is a 1 to 6 carbon alkyl, 3 to 8 carbon alkenyl, cyanomethyl carboxymethyl, carbalkoxymethyl wherein the alkoxy moiety is a 1 to 4 carbon alkoxy group, nitromethyl, alkylcarbonylmethyl wherein the alkyl moiety is a 1 to 4 carbon alkyl group, pyridyl, furanyl, or furfuryl group or a phenyl or benzyl group optionally substituted by a methylenedioxy or one to two halogen, 1 to 4 carbon alkyl, 1 to 4 carbon alkoxy, 1 to 4 carbon alkylthio, hydroxy, nitro or cyano groups or a pharmaceutically acceptable acid addition salt thereof. Also described are their use as antiprotozoals and antibacterials.
REFERENCES:
Goldberg and Mitsugi, Biochemical and Biophysical Research Communications, vol. 23, No. 4, 1966, pp. 453-459.
Lin and Dubois, J. Med. Chem., vol. 20, No. 3, pp. 337-341, (1977).
Burger, A., Medicinal Chemistry, 2nd ed. .COPYRGT.1960, p. 42.
Ottenheijm and Liskamp, Tetrahedron Letters, No. 27, pp. 2437-2438, 1978 (I).
Ottenheijm, Liskamp and Tijhvis, Tetrahedron Letters, No. 4, pp. 387-390, 1979 (II).
Duke, Dissertation Abstracts International, vol. 43, No. 10, p. 3249B, Apr. 1983.
Upjohn Co. Chemical Abstracts, vol. 62:5855d (1965).
Flynn and Ash Biochemical and Biophysical Research Communications, vol. 114, No. 1, 1983, Jul. 18, 1983, pp. 1-7, Necessity of the Sulfoxide Moiety for the Biochemical and Biological Properties of an Analog of Sparsomycin.
Ash et al., Antimicrobial Agents and Chemotherapy, Apr., 1984, pp.-443-445, vol. 25, No. 4, Importance of the Hydrophobic Sulfoxide Substituent on Nontoxic Analogs of Sparsomycin.
Beight Douglas W.
Flynn Gary A.
Daus Donald G.
Kapner Stephen M.
Merrell Dow Pharmaceuticals Inc.
Nesbitt Stephen L.
LandOfFree
Sparsomycin derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Sparsomycin derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Sparsomycin derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2273401