6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD-SPECTRUM INHIBITORS OF BACTERIAL BETA-LACTAMASE .5. CHIRAL 1,2,3-TRIAZOLYL DERIVATIVES

被引：71

作者：

BENNETT, IS ^{[1
]}

BROOKS, G ^{[1
]}

BROOM, NJP ^{[1
]}

CALVERT, SH ^{[1
]}

COLEMAN, K ^{[1
]}

FRANCOIS, I ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,CHEMOTHERAPEUT RES CTR,BROCKHAM PK,BETCHWORTH RH3 7AJ,SURREY,ENGLAND

来源：

JOURNAL OF ANTIBIOTICS | 1991年 / 44卷 / 09期

关键词：

D O I：

10.7164/antibiotics.44.969

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：

Structure-activity relationships in a series of (5R)-6-triazolylmethylene penems with potent beta-lactamase inhibitory activity are described, In most cases, their in vitro synergistic activity with amoxycillin is superior to that of clavulanic acid, sulbactam and tazobactam (YTR 830). Against an Escherichia coli TEM-1 infection in mice, the compounds showed a broad range of potencies; an optimum polarity was found, however, which gave maximum potency.

引用

页码：969 / 978

页数：10

共 18 条

[1] 6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD-SPECTRUM INHIBITORS OF BACTERIAL BETA-LACTAMASE .1. RACEMIC 6-ETHYLIDENEPENEMS [J].

BASKER, MJ ;

OSBORNE, NF .

JOURNAL OF ANTIBIOTICS, 1990, 43 (01) :70-75

[2] 6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD-SPECTRUM INHIBITORS OF BACTERIAL BETA-LACTAMASE .3. STRUCTURE-ACTIVITY-RELATIONSHIPS OF THE 5-MEMBERED HETEROCYCLIC-DERIVATIVES [J].

BENNETT, I ;

BROOM, NJP ;

BRUTON, G ;

CALVERT, S ;

CLARKE, BP ;

COLEMAN, K ;

EDMONDSON, R ;

EDWARDS, P ;

JONES, D ;

OSBORNE, NF ;

WALKER, G .

JOURNAL OF ANTIBIOTICS, 1991, 44 (03) :331-337

[3]

BENNETT IS, 1991, J ANTIBIOT, V44, P338, DOI 10.7164/antibiotics.44.338

[4]

BENNETT IS, 1988, 28TH INT C ANT AG CH, P130

[5] SYNTHESIS AND BETA-LACTAMASE INHIBITORY ACTIVITY OF 9-(2-AMIDOETHENYLTHIO)-9-DEOXY DERIVATIVES OF CLAVULANIC ACID [J].

BROOKS, G ;

COLEMAN, K ;

DAVIES, JS ;

HUNTER, PA .

JOURNAL OF ANTIBIOTICS, 1988, 41 (07) :892-898

[6] 6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD-SPECTRUM INHIBITORS OF BACTERIAL BETA-LACTAMASE .2. RACEMIC FURYL AND THIENYL DERIVATIVES [J].

BROOM, NJP ;

COLEMAN, K ;

HUNTER, PA ;

OSBORNE, NF .

JOURNAL OF ANTIBIOTICS, 1990, 43 (01) :76-82

[7]

BROOM NJP, 1989, SPECIAL PUBLICATION, V70, P247

[8] INVITRO EVALUATION OF BRL 42715, A NOVEL BETA-LACTAMASE INHIBITOR [J].

COLEMAN, K ;

GRIFFIN, DRJ ;

PAGE, JWJ ;

UPSHON, PA .

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1989, 33 (09) :1580-1587

[9]

COULTON S, 1987, Patent No. 232966

[10] SYNTHESIS OF 1,2,3-TRIAZOLO[1,5-A]-1,3,5-TRIAZINE - NEW HETEROCYCLIC SYSTEM [J].

KLEIN, RS ;

DELASHERAS, FG ;

TAM, SYK ;

WEMPEN, I ;

FOX, JJ .

JOURNAL OF HETEROCYCLIC CHEMISTRY, 1976, 13 (03) :589-592

← 1 2 →