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 Glycopetide antibiotic PA-45052-B

Details
Inventors: Kondo, Eiji; Kawamura, Yoshimi; Tsuji, Naoki; Matsumoto, Koichi; Kobayashi, Masaaki; Kamigauchi, Toshiyuki; Hayashi, Yoshiyuki; Konishi, Takao;
Assignee: Shionogi & Co., Ltd. (Osaka, JP)
Primary Examiner: Schwartz; Richard A.
Assistant Examiner: Mosher; Mary E.
Attorney, Agent or Firm: Wenderoth, Lind & Ponack

Glycopeptide antibiotics PA-45052 which are produced by Nocardia orientalis PA-45052, show potent activity against gram-positive bacteria, especially against methicillin-resistant bacteria, and stimulate growth of animals.

DETAILED DESCRIPTION OF THE INVENTION The present inventors found that the strain belonging to the genus Nocardia produces compounds which are represented by the following formula: ##STR2## or H and R.
sub.
1 is CH.
sub.
3 or H.
sub.
1) and which have a strong antibacterial activity, and named a compound of which R in the above formula is ##STR3## and R.
sub.
1 is H as PA-45052-A, named another compound of which R in the formula is ##STR4## and R.
sub.
1 is H as PA-45052-B, named a further different compound of which R is H and R.
sub.
1 is H as PA-45052-C, named a further different compound of which R is ##STR5## and R.
sub.
1 is CH.
sub.
3 as PA-45052-D, named a further different compound of which R is ##STR6## and R.
sub.
1 is CH.
sub.
3 as PA-45052-E, and named a further different compound of which R is H and R.
sub.
1 is CH.
sub.
3 as PA-45052-F.
The present invention includes not only these compounds but also their pharmaceutically acceptable salts.
PA-45052 described in this specification means mainly any one of the above six compounds but in some cases specifies all of these compounds.
The physicochemical properties of the compounds of this invention are shown below.
The appellations PA-45052-A (HCl), PA-45052-B (HCl), PA-45052-C (HCl), PA-45052-D (HCl), and PA-45052-E (HCl) denote that all of them are hydrochlorides.
PHYSICOCHEMICAL PROPERTIES Ultraviolet Absorption Spectrum PA-45052-A (HCl): .
lambda.
.
sub.
max.
sup.
0.
01NHCl nm (E.
sub.
1cm.
sup.
1%): 281.
0 (36.
4).
.
lambda.
.
sub.
max.
sup.
0.
01NNaOH .
aq nm (E.
sub.
1cm.
sup.
1%): 301.
8 (40.
4).
PA-45052-B (HCl): .
lambda.
.
sub.
max.
sup.
0.
01NHCl nm (E.
sub.
1cm.
sup.
1%): 281.
2 (41.
1).
.
lambda.
.
sub.
max.
sup.
0.
01NNaOH .
aq nm (E.
sub.
1cm.
sup.
1%): 302.
0 (46.
8).
PA-45052-C (HCl): .
lambda.
.
sub.
max.
sup.
0.
01NHCl nm (E.
sub.
1cm.
sup.
1%): 279.
6 (46.
7).
.
lambda.
.
sub.
max.
sup.
0.
01NNaOH.
aq nm (E.
sub.
1cm.
sup.
1%): 296.
4 (87.
0).
PA-45052-D (HCl): .
lambda.
.
sub.
max.
sup.
0.
01NHCl nm (E.
sub.
1cm.
sup.
1%): 280.
7 (34.
5).
.
lambda.
.
sub.
max.
sup.
0.
01NNaOH .
aq nm (E.
sub.
1cm.
sup.
1%): 301.
8 (39.
4).
PA-45052-E (HCl):



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