L-755,807, a new non-peptide bradykinin binding inhibitor from an endophytic Microsphaeropsis sp.

被引:37
作者
Lam, YKT [1 ]
Hensens, OD [1 ]
Ransom, R [1 ]
Giacobbe, RA [1 ]
Polishook, J [1 ]
Zink, D [1 ]
机构
[1] MERCK SHARP & DOHME LTD,RES LABS,W POINT,PA 19486
关键词
D O I
10.1016/0040-4020(95)00985-X
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A new metabolite, L-755,807, 1, was isolated from an endophytic Microsphaeropsis sp. in the course of searching for a bradykinin binding inhibitor. The structure of 1, including relative stereochemistry, was determined 1 showed an IC50 of 71 mu M in H-3-bradykinin binding to a cloned human B-2 receptor.
引用
收藏
页码:1481 / 1486
页数:6
相关论文
共 13 条
[1]   H-1 AND C-13 ASSIGNMENTS FROM SENSITIVITY-ENHANCED DETECTION OF HETERONUCLEAR MULTIPLE-BOND CONNECTIVITY BY 2D MULTIPLE QUANTUM NMR [J].
BAX, A ;
SUMMERS, MF .
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 1986, 108 (08) :2093-2094
[2]   CORRELATION OF PROTON CHEMICAL-SHIFTS BY TWO-DIMENSIONAL FOURIER-TRANSFORM NMR [J].
BAX, A ;
FREEMAN, R ;
MORRIS, G .
JOURNAL OF MAGNETIC RESONANCE, 1981, 42 (01) :164-168
[3]  
BAX A, 1986, J MAGN RESON, V67, P375
[4]  
BOTHNERBY AA, 1984, J AM CHEM SOC, V106, P81
[5]   TAN-1496-A, TAN-1496-C AND TAN-1496-E, DIKETOPIPERAZINE ANTIBIOTICS WITH INHIBITORY ACTIVITY AGAINST MAMMALIAN DNA TOPOISOMERASE-I [J].
FUNABASHI, Y ;
HORIGUCHI, T ;
IINUMA, S ;
TANIDA, S ;
HARADA, S .
JOURNAL OF ANTIBIOTICS, 1994, 47 (11) :1202-1218
[6]   BRADYKININ RECEPTORS - PHARMACOLOGICAL PROPERTIES AND BIOLOGICAL ROLES [J].
HALL, JM .
PHARMACOLOGY & THERAPEUTICS, 1992, 56 (02) :131-190
[7]   CLONING AND PHARMACOLOGICAL CHARACTERIZATION OF A HUMAN BRADYKININ (BK-2) RECEPTOR [J].
HESS, JF ;
BORKOWSKI, JA ;
YOUNG, GS ;
STRADER, CD ;
RANSOM, RW .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1992, 184 (01) :260-268
[8]  
KYLE D J, 1992, Drugs of the Future, V17, P305
[9]   THE NONPEPTIDE WIN-64338 IS A BRADYKININ B-2 RECEPTOR ANTAGONIST [J].
SAWUTZ, DG ;
SALVINO, JM ;
DOLLE, RE ;
CASIANO, F ;
WARD, SJ ;
HOUCK, WT ;
FAUNCE, DM ;
DOUTY, BD ;
BAIZMAN, E ;
AWAD, MMA ;
MARCEAU, F ;
SEOANE, PR .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (11) :4693-4697
[10]   L-671,329, A NEW ANTIFUNGAL AGENT .1. FERMENTATION AND ISOLATION [J].
SCHWARTZ, RE ;
GIACOBBE, RA ;
BLAND, JA ;
MONAGHAN, RL .
JOURNAL OF ANTIBIOTICS, 1989, 42 (02) :163-167