BENZOMALVINS, NEW SUBSTANCE-P INHIBITORS FROM A PENICILLIUM SP

被引：77

作者：

SUN, HH

BARROW, CJ

SEDLOCK, DM

GILLUM, AM

COOPER, R

机构：

[1] Sterling Winthrop Pharmaceuticals Research Division, Pennsylvania 19355, 5 Great Valley Parkway, Malvern

来源：

JOURNAL OF ANTIBIOTICS | 1994年 / 47卷 / 05期

关键词：

D O I：

10.7164/antibiotics.47.515

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

In the course of screening microbial broths for neurokinin receptor antagonists, a series of new benzodiazepines, benzomalvins A (1), B (2) and C (3), has been isolated from the culture broth of a fungus identified as a Penicillium sp. Benzomalvin A (1) showed inhibitory activity against substance P with Ki values of 12, 42 and 43 mu M at the guinea pig, rat and human neurokinin NK1 receptors, respectively. Benzomalvins B (2) and C (3) were only weakly active. The structures of these compounds were determined by spectroscopic methods including MS measurements and NMR analysis.

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页码：515 / 522

页数：8

相关论文

共 24 条

[1]

APPELL KC, 1992, MOL PHARMACOL, V41, P772

[2] STRUCTURE DETERMINATION, PHARMACOLOGICAL EVALUATION, AND STRUCTURE-ACTIVITY STUDIES OF A NEW CYCLIC PEPTIDE SUBSTANCE-P ANTAGONIST CONTAINING THE NEW AMINO-ACID 3-PRENYL-BETA-HYDROXYTYROSINE, ISOLATED FROM ASPERGILLUS FLAVIPES [J].

BARROW, CJ ;

DOLEMAN, MS ;

BOBKO, MA ;

COOPER, R .

JOURNAL OF MEDICINAL CHEMISTRY, 1994, 37 (03) :356-363

[3] WIN 64821, A NEW COMPETITIVE ANTAGONIST TO SUBSTANCE-P, ISOLATED FROM AN ASPERGILLUS SPECIES - STRUCTURE DETERMINATION AND SOLUTION CONFORMATION [J].

BARROW, CJ ;

CAI, P ;

SNYDER, JK ;

SEDLOCK, DM ;

SUN, HH ;

COOPER, R .

JOURNAL OF ORGANIC CHEMISTRY, 1993, 58 (22) :6016-6021

[4] A POTENT NONPEPTIDE CHOLECYSTOKININ ANTAGONIST SELECTIVE FOR PERIPHERAL-TISSUES ISOLATED FROM ASPERGILLUS-ALLIACEUS [J].

CHANG, RSL ;

LOTTI, VJ ;

MONAGHAN, RL ;

BIRNBAUM, J ;

STAPLEY, EO ;

GOETZ, MA ;

ALBERSSCHONBERG, G ;

PATCHETT, AA ;

LIESCH, JM ;

HENSENS, OD ;

SPRINGER, JP .

SCIENCE, 1985, 230 (4722) :177-179

[5] PHARMACOLOGICAL PROPERTIES OF A POTENT AND SELECTIVE NONPEPTIDE SUBSTANCE-P ANTAGONIST [J].

GARRET, C ;

CARRUETTE, A ;

FARDIN, V ;

MOUSSAOUI, S ;

PEYRONEL, JF ;

BLANCHARD, JC ;

LADURON, PM .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1991, 88 (22) :10208-10212

[6] ASPERLICIN, A NOVEL NON-PEPTIDAL CHOLECYSTOKININ ANTAGONIST FROM ASPERGILLUS-ALLIACEUS - FERMENTATION, ISOLATION AND BIOLOGICAL PROPERTIES [J].

GOETZ, MA ;

LOPEZ, M ;

MONAGHAN, RL ;

CHANG, RSL ;

LOTTI, VJ ;

CHEN, TB .

JOURNAL OF ANTIBIOTICS, 1985, 38 (12) :1633-1637

[7]

HAGAN RM, 1991, BRIT J PHARMACOL, V102, P168

[8] WS9326A, A NOVEL TACHYKININ ANTAGONIST ISOLATED FROM STREPTOMYCES-VIOLACEUSNIGER NO-9326 .2. BIOLOGICAL AND PHARMACOLOGICAL PROPERTIES OF WS9326A AND TETRAHYDRO-WS9326A (FK224) [J].

HASHIMOTO, M ;

HAYASHI, K ;

MURAI, M ;

FUJII, T ;

NISHIKAWA, M ;

KIYOTO, S ;

OKUHARA, M ;

KOHSAKA, M ;

IMANAKA, H .

JOURNAL OF ANTIBIOTICS, 1992, 45 (07) :1064-1070

[9] WS9326A, A NOVEL TACHYKININ ANTAGONIST ISOLATED FROM STREPTOMYCES-VIOLACEUSNIGER NO-9326 [J].

HAYASHI, K ;

HASHIMOTO, M ;

SHIGEMATSU, N ;

NISHIKAWA, M ;

EZAKI, M ;

YAMASHITA, M ;

KIYOTO, S ;

OKUHARA, M ;

KOHSAKA, M ;

IMANAKA, H .

JOURNAL OF ANTIBIOTICS, 1992, 45 (07) :1055-1063

[10] NOVEL CHOLECYSTOKININ ANTAGONISTS FROM ASPERGILLUS-ALLIACEUS .2. STRUCTURE DETERMINATION OF ASPERLICIN-B, ASPERLICIN-C, ASPERLICIN-D, AND ASPERLICIN-E [J].

LIESCH, JM ;

HENSENS, OD ;

ZINK, DL ;

GOETZ, MA .

JOURNAL OF ANTIBIOTICS, 1988, 41 (07) :878-881