In Vitro Activity of API-1252, a Novel FabI Inhibitor, against Clinical Isolates of
            <i>Staphylococcus aureus</i>
            and
            <i>Staphylococcus epidermidis</i>

Karlowsky, James A.; Laing, Nancy M.; Baudry, Trish J.; Kaplan, Nachum; Vaughan, David; Hoban, Daryl J.; Zhanel, George G.

doi:10.1128/aac.01254-06

Cited by 56 publications

(50 citation statements)

References 7 publications

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“…A recently developed inhibitor of FabI API-1252 (Fig. 2B iv), showed MIC 50 s of 4 -15 ng/ml against S. aureus and S. epidermidis drug resistant strains [23], none of which carries the FabK gene Ethionamide and prothionamide, which are structurally similar to isoniazid, have been used for some time in the treatment of M. tuberculosis, M. leprae and M.avium infections and are assuming increasing importance with the growing incidence of isoniazid resistance. Their mechanism of action has been assumed to be the same as isoniazid, which is a pro-drug that requires enzymatic activation by a catalase-peroxidase (KatG) to react with NAD + and form the adduct which is the proximal inhibitor of FabI.…”

Section: Fasii Inhibitors From Structure-based Design and Chemical LImentioning

confidence: 99%

Antibacterial targets in fatty acid biosynthesis

Wright

Reynolds

2007

Current Opinion in Microbiology

171

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SummaryThe fatty acid biosynthesis pathway is an attractive but still largely unexploited target for development of new anti-bacterial agents. The extended use of the anti-tuberculosis drug isoniazid and the antiseptic triclosan, which are inhibitors of fatty acid biosynthesis, validates this pathway as a target for anti-bacterial development. Differences in subcellular organization of the bacterial and eukaryotic multi-enzyme fatty acid synthase systems offer the prospect of inhibitors with host vs. target specificity. Platensimycin, platencin, and phomallenic acids, newly discovered natural product inhibitors of the condensation steps in fatty acid biosynthesis, represent new classes of compounds with antibiotic potential. An almost complete catalogue of crystal structures for the enzymes of the type II fatty acid biosynthesis pathway can now be exploited in the rational design of new inhibitors, as well as the recently published crystal structures of type I FAS complexes.

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Section: Fasii Inhibitors From Structure-based Design and Chemical LImentioning

confidence: 99%

Antibacterial targets in fatty acid biosynthesis

Wright

Reynolds

2007

Current Opinion in Microbiology

171

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“…Other compounds which have completed phase I clinical trials include the oral and injectable pleuromutilin BC-3205, 17 the FabI inhibitor AFN-1252 targeting staphylococcal infections 18 and the lipopeptide friulimicin (Table 1). 19 The scenario is even more disappointing for compounds targeting Gram-negative pathogens, in which old drugs have been revamped for new uses, and none of them has reached phase III yet (Table 1).…”

mentioning

confidence: 99%

Antibiotic discovery in the twenty-first century: current trends and future perspectives

Donadio¹,

Maffioli²,

Monciardini³

et al. 2010

J Antibiot

223

126

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New antibiotics are necessary to treat microbial pathogens that are becoming increasingly resistant to available treatment. Despite the medical need, the number of newly approved drugs continues to decline. We offer an overview of the pipeline for new antibiotics at different stages, from compounds in clinical development to newly discovered chemical classes. Consistent with historical data, the majority of antibiotics under clinical development are natural products or derivatives thereof. However, many of them also represent improved variants of marketed compounds, with the consequent risk of being only partially effective against the prevailing resistance mechanisms. In the discovery arena, instead, compounds with promising activities have been obtained from microbial sources and from chemical modification of antibiotic classes other than those in clinical use. Furthermore, new natural product scaffolds have also been discovered by ingenious screening programs. After providing selected examples, we offer our view on the future of antibiotic discovery.

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“…A limited number of antibiotics also possess antiprotozoal activity. Antibiotics are not effective against viruses such as the common cold or influenza, and may be harmful when taken inappropriately [2].…”

Section: Introductionmentioning

confidence: 99%

Molecular Evaluation of Antistaphylococcal Secondary Metabolites of Bacterial Isolates From Hospital Wastewater Environment

Rajan

Sudhakar

Bhaskar

et al. 2017

Asian J Pharm Clin Res

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Objective: Antibiotics revolutionized medicine in the 20 th century, and have together with vaccination led to the near eradication of diseases such as tuberculosis in the developed world. Their effectiveness and easy access led to overuse, especially in livestock raising, prompting bacteria to develop resistance. The lantibiotics form a particular group among the antimicrobial peptides and are characterized by unique structural features. They are produced by a group of bacteria against some gram-positive bacteria. The present study was designed to screen for the lantibiotic producing organisms from the hospital samples. Methods:The bacterial isolates were identified based on Bergey's manual of bacteriology and screened for the epidermin gene by polymerase chain reaction amplification. Results:Of the 21 isolates screened, only 10 of them showed positive amplification for the epigene. Based on the biochemical characteristics, the isolates obtained were identified and labeled. Conclusion:Further study on the purification of the compound need to be done. Some bacterial samples may not have the epidermin gene which does not show amplification, this confers that the epidermin gene is absent in certain organisms.

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In Vitro Activity of API-1252, a Novel FabI Inhibitor, against Clinical Isolates of Staphylococcus aureus and Staphylococcus epidermidis

Cited by 56 publications

References 7 publications

Antibacterial targets in fatty acid biosynthesis

Antibacterial targets in fatty acid biosynthesis

Antibiotic discovery in the twenty-first century: current trends and future perspectives

Molecular Evaluation of Antistaphylococcal Secondary Metabolites of Bacterial Isolates From Hospital Wastewater Environment

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