Literature DB >> 7096196

Thiolactomycin, a new antibiotic. IV. Biological properties and chemotherapeutic activity in mice.

S Miyakawa, K Suzuki, T Noto, Y Harada, H Okazaki.   

Abstract

The new thiolactone antibiotic, thiolactomycin, is rapidly absorbed in rats when administered either orally or by intramuscular injection. A peak in concentration of the drug is reached in the blood and in various visceral organs within 15 minutes after administration. The concentration decreases rather rapidly and about 51-69% of the drug is excreted in urine during the first 24 hours. Though the in vitro effect of thiolactomycin is moderate, it effectively protected mice challenged intraperitoneally with several strains of S. marcescens and K. pneumoniae and more effective than carbenicillin in treating experimental acute urinary tracts infected with S. marcescens. Also, in mice whom immunodefense was decreased by treatment with cyclophosphamide, thiolactomycin was more effective than carbenicillin against S. marcescens challenge.

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Year:  1982        PMID: 7096196     DOI: 10.7164/antibiotics.35.411

Source DB:  PubMed          Journal:  J Antibiot (Tokyo)        ISSN: 0021-8820            Impact factor:   2.649


  39 in total

1.  Structure-activity relationships at the 5-position of thiolactomycin: an intact (5R)-isoprene unit is required for activity against the condensing enzymes from Mycobacterium tuberculosis and Escherichia coli.

Authors:  Pilho Kim; Yong-Mei Zhang; Gautham Shenoy; Quynh-Anh Nguyen; Helena I Boshoff; Ujjini H Manjunatha; Michael B Goodwin; John Lonsdale; Allen C Price; Darcie J Miller; Ken Duncan; Stephen W White; Charles O Rock; Clifton E Barry; Cynthia S Dowd
Journal:  J Med Chem       Date:  2006-01-12       Impact factor: 7.446

Review 2.  Recent advances in the chemistry and biology of naturally occurring antibiotics.

Authors:  K C Nicolaou; Jason S Chen; David J Edmonds; Anthony A Estrada
Journal:  Angew Chem Int Ed Engl       Date:  2009       Impact factor: 15.336

3.  Overproduction of beta-ketoacyl-acyl carrier protein synthase I imparts thiolactomycin resistance to Escherichia coli K-12.

Authors:  J T Tsay; C O Rock; S Jackowski
Journal:  J Bacteriol       Date:  1992-01       Impact factor: 3.490

Review 4.  Challenges of antibacterial discovery.

Authors:  Lynn L Silver
Journal:  Clin Microbiol Rev       Date:  2011-01       Impact factor: 26.132

Review 5.  Is bacterial fatty acid synthesis a valid target for antibacterial drug discovery?

Authors:  Joshua B Parsons; Charles O Rock
Journal:  Curr Opin Microbiol       Date:  2011-08-20       Impact factor: 7.934

6.  Fatty acid biosynthesis in Pseudomonas aeruginosa: cloning and characterization of the fabAB operon encoding beta-hydroxyacyl-acyl carrier protein dehydratase (FabA) and beta-ketoacyl-acyl carrier protein synthase I (FabB).

Authors:  T T Hoang; H P Schweizer
Journal:  J Bacteriol       Date:  1997-09       Impact factor: 3.490

7.  Docking and molecular dynamics studies on triclosan derivatives binding to FabI.

Authors:  Xuyun Yang; Junrui Lu; Ming Ying; Jiangbei Mu; Peichun Li; Yue Liu
Journal:  J Mol Model       Date:  2017-01-07       Impact factor: 1.810

Review 8.  Bacterial fatty acid metabolism in modern antibiotic discovery.

Authors:  Jiangwei Yao; Charles O Rock
Journal:  Biochim Biophys Acta Mol Cell Biol Lipids       Date:  2016-09-23       Impact factor: 4.698

9.  Slow onset inhibition of bacterial beta-ketoacyl-acyl carrier protein synthases by thiolactomycin.

Authors:  Carl A Machutta; Gopal R Bommineni; Sylvia R Luckner; Kanishk Kapilashrami; Bela Ruzsicska; Carlos Simmerling; Caroline Kisker; Peter J Tonge
Journal:  J Biol Chem       Date:  2009-12-16       Impact factor: 5.157

10.  Selectivity of Pyridone- and Diphenyl Ether-Based Inhibitors for the Yersinia pestis FabV Enoyl-ACP Reductase.

Authors:  Carla Neckles; Annica Pschibul; Cheng-Tsung Lai; Maria Hirschbeck; Jochen Kuper; Shabnam Davoodi; Junjie Zou; Nina Liu; Pan Pan; Sonam Shah; Fereidoon Daryaee; Gopal R Bommineni; Cristina Lai; Carlos Simmerling; Caroline Kisker; Peter J Tonge
Journal:  Biochemistry       Date:  2016-05-17       Impact factor: 3.162

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