Micacocidin derivatives

Details Micacocidin derivatives Micacocidin derivatives

1998-08-05

1999-12-21

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514365, 548101, 548104, 548146, C07D27710, A01K 31425

Patent

active

060049529

DESCRIPTION:

BRIEF SUMMARY
DETAILED DESCRIPTION OF THE INVENTION



FIELD OF THE INVENTION

The present invention relates to a novel compound useful in the field of medicine and veterinary medicine, and to medical and animal drugs containing said compound.


BACKGROUND OF THE INVENTION

Pyochelin, which is produced by Pseudomonas aeruginosa, is known as a compound having a similar structure to that of the present invention (J. Bacteriology 137(1), 357, 1979). However, it is unknown whether it has also a biological activity similar to that of the compound of the present invention.


Subject of the Invention to be Solved

The object of the present invention is to provide a novel compound having various biological activities useful for medical and animal drugs.


Means for Solving the Subject

The present inventors have made extended studies to attain the object mentioned above and have found that a novel compound of the formula (I) shown below has anti-mycoplasma activity, anti-coccidium activity, antibacterial activity, antifungal activity and immunosuppressive activity.
Thus, the present invention provides a compound of the formula (I): ##STR2## wherein R.sup.1 is (1) COOR.sup.4 wherein R.sup.4 is hydrogen atom, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl; (2) CONR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen atom, hydroxyl, optionally substituted alkyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, provided that when one of R.sup.5 and R.sup.6 is hydroxyl or optionally substituted alkoxyl, the other is hydrogen atom, optionally substituted alkyl, optionally substituted aryl or optionally substituted aralkyl; (3) CO--R.sup.7 --OR wherein R.sup.7 is .alpha.-amino acid residue and R is hydrogen atom or alkyl ; or (4) CH.sub.2 OR.sup.8 wherein R.sup.8 is hydrogen atom, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, COR.sup.9 wherein R.sup.9 is hydrogen atom, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, COOR.sup.10 wherein R.sup.10 is optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, or CONR.sup.11 R.sup.12 wherein R.sup.11 and R.sup.12 are the same or different and represent hydrogen atom, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl; substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, COR.sup.13 wherein R.sup.13 is hydrogen atom, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, COOR.sup.14 wherein R.sup.14 is optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, or CONR.sup.15 R.sup.16 wherein R.sup.15 and R.sup.16 are the same or different and represent hydrogen atom, optionally substituted alkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl; provided that when it presents the presence of the double bond, R.sup.3 is oxygen atom, or when it represents the absence of the double bond, R.sup.3 is OR.sup.3' wherein R .sup.3' is hydrogen atom, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, COR .sup.17 wherein R.sup.17 is hydrogen atom, optionally substituted alkyl, optionally substitute

REFERENCES:
patent: 5707838 (1998-01-01), Takeda

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