WF11243 substance

Details WF11243 substance WF11243 substance

1993-11-04

1995-08-29

Lilling, Herbert J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

424118, 435 711, 4352541, 435911, 514 9, 514 10, 530317, 530321, 530323, C07K 1102, C12P 2102, C12N 114, A61K 3812

Patent

active

054460220

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to WF11243 substance and its salts as well as to a method of preparing them and use of them. The WF11243 substance is a novel substance which is isolated and purified from a culture broth of microorganisms, especially fungi. It has excellent fungicidal and protozoicidal activity and is, therefore, useful as various preventing and treating medicines for preventing, curing and reducing various diseases and disorders to be caused by fungi and protozoans. It is also useful for prevention and treatment of Pneumocystis carinii pneumonia.
Therefore, the present invention plays an important role in various technical fields of medicines, cosmetics, foods and drinks.


PRIOR ART

Hitherto, various fungicides have been obtained from cultures of microorganisms or by chemical syntheses. Some of them could be admitted to be good, but many of them have various problems, such as appearance of drug-tolerant microoganisms and safety of themselves. At present, no one has a satisfactory fungicidal agent which is completely free from the problems.
Recently, various diseases to be caused by protozoans, especially those to be caused by Pneumocystis carinii such as Pneumocystis carinii pneumonia, have been closed up, and development of methods of preventing and treating them has been strongly desired in this technical field.


PROBLEMS TO BE SOLVED BY THE INVENTION

The present invention has been made in view of the current technical situation as mentioned above, and the object of the present invention is to provide and develop a novel protozoicidal agent which is effective for preventing the growth of Pneumocystis carinii which causes Pneumocystis carinii pneumonia and other diseases, or protozoans. Another object of this invention is to develop and provide novel fungicides useful for preventing the growth of various fungi.


MEANS TO SOLVE THE PROBLEMS

In order to attain the above-mentioned object, the present inventors investigated from various aspects and noted natural substances, especially fermented products from microorganisms, in view of safety. They studied and investigated various microorganisms and, as a result, have found that fungal strain No. 11243 as isolated from fallen leaves samples collected in Ayabe-shi, Kyoto-fu, Japan, produces and accumulates the intended product in the culture broth. They have further studied in detail the product with respect to the physico-chemical properties thereof and have found that the product is a novel substance. They have named the substance WF11243 substance. Further, they have named the hydrochloride thereof FR901469 substance. After further study of the novel WF11243 substance, they have established an industrial method of producing them and have achieved the present invention.


EXPLANATION OF THE DRAWINGS

FIG. 1 shows a .sup.13 C nuclear magnetic resonance spectrum of FR901469 substance.
FIG. 2 is .sup.1 H nuclear magnetic resonance spectrum of FR901469 substance.
The WF11243 substance of the present invention is a novel substance having, as its hydrochloride, FR901469 substance, the physico-chemical properties as mentioned below.


Physico-chemical Properties of FR901469 Substance (1)

Calcd (%): for C.sub.71 H.sub.116 N.sub.14 O.sub.23.HCl.8H.sub.2 O C 49.74, H 7.82, N 11.44 Found (%): C 49.65, H 7.72, N 11.40


______________________________________ Stationary phase Developing solvent Rf value ______________________________________ Silica gel n-butanol/acetic acid/water 0.42 60 F.sub.254 (4/1/2) (made by E. Merck) RP-18 45% aqueous acetonitrile 0.18 WF.sub.254 S (containing 0.5% NH.sub.4 H.sub.2 PO.sub.4) (made by E. Merck) ______________________________________


______________________________________ .nu..sub.max.sup.KBr : 3400, 2920, 1730, 1660, 1650, 1635, 1540, 1520, 1460, 1250, 1090 cm.sup.-1 ______________________________________ Co., Ltd.) H.sub.2 PO.sub.4)
FIG. 1 shows the chart.
.delta.c: 176.1 (s), 174.6 (s), 174.0 (s), 173.8 (s), 173.4 (s), 172.8 (s), 172.6 (s), 1

REFERENCES:
patent: 4931352 (1990-06-01), Fromtling et al.
patent: 4968608 (1990-11-01), Giacobbe et al.
patent: 5021341 (1991-06-01), Giacobbe et al.
patent: 5021403 (1991-06-01), Sesin et al.
patent: 5137813 (1992-08-01), Fountoulakis et al.
patent: 5162211 (1992-11-01), Sesin et al.
patent: 5166135 (1992-11-01), Schmatz
patent: 5194377 (1993-03-01), Schwartz et al.
patent: 5229363 (1993-07-01), Hammond et al.
patent: 5306708 (1994-04-01), Schwartz et al.

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