Recent Advances in Inhibitors of Bacterial Fatty Acid Synthesis Type II (FASII) System Enzymes as Potential Antibacterial Agents

Novel Schiff-Base-Derived FabH Inhibitors with Dioxygenated Rings as Antibiotic Agents

(2013) Yang Zhou et al.   ChemMedChem

Discovery of novel InhA reductase inhibitors: application of pharmacophore- and shape-based screening approach

(2013) Uday Chandra Kumar et al.   Future Medicinal Chemistry

In vitroactivity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics

(2013) Nachum Kaplan et al.   JOURNAL OF CHEMOTHERAPY

Pharmacokinetics, pharmacodynamics and efficacy of novel FabI inhibitor AFN-1252 against MSSA and MRSA in the murine thigh infection model

(2013) Mary A Banevicius et al.   JOURNAL OF CHEMOTHERAPY

Panosialins, Inhibitors of Enoyl-ACP Reductase from Streptomyces sp. AN1761

(2013) Yun Ju Kwon   JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY

Structure of FabH and factors affecting the distribution of branched fatty acids inMicrococcus luteus

(2012) Jose H. Pereira et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Purification, crystallization and preliminary X-ray diffraction analysis of enoyl-acyl carrier protein reductase (FabK) fromStreptococcus mutansstrain UA159

(2012) Tae-O Kim et al.   Acta Crystallographica Section F-Structural Biology and Crystallization Communications

Mode of Action,In VitroActivity, andIn VivoEfficacy of AFN-1252, a Selective Antistaphylococcal FabI Inhibitor

(2012) Nachum Kaplan et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Chalcomoracin and Moracin C, New Inhibitors of Staphylococcus aureus Enoyl-Acyl Carrier Protein Reductase from Morus alba

(2012) Yu Jin Kim et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Design, synthesis and antimicrobial activities of nitroimidazole derivatives containing 1,3,4-oxadiazole scaffold as FabH inhibitors

(2012) Yao Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery and modification of sulfur-containing heterocyclic pyrazoline derivatives as potential novel class of β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors

(2012) Yu-Shun Yang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Verrulactones A and B, new inhibitors of Staphylococcus aureus enoyl-ACP reductase produced by Penicillium verruculosum F375

(2012) Nyung Kim et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Advances in the Research of β-Ketoacyl-ACP Synthase III (FabH) Inhibitors

(2012) H. -J. Zhang et al.   CURRENT MEDICINAL CHEMISTRY

Targeting InhA, the FASII Enoyl-ACP Reductase: SAR Studies on Novel Inhibitor Scaffolds

(2012) Pan Pan et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Design, synthesis and antibacterial activities of vanillic acylhydrazone derivatives as potential β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors

(2012) Xiao-Liang Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structural and Enzymatic Analyses Reveal the Binding Mode of a Novel Series of Francisella tularensis Enoyl Reductase (FabI) Inhibitors

(2012) Shahila Mehboob et al.   JOURNAL OF MEDICINAL CHEMISTRY

From Triclosan toward the Clinic: Discovery of Nonbiocidal, Potent FabI Inhibitors for the Treatment of Resistant Bacteria

(2012) Vincent Gerusz et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Insights into the Mechanism and Inhibition of the β-Hydroxydecanoyl-Acyl Carrier Protein Dehydratase from Pseudomonas aeruginosa

(2012) Lucile Moynié et al.   JOURNAL OF MOLECULAR BIOLOGY

Environmental DNA-Encoded Antibiotics Fasamycins A and B Inhibit FabF in Type II Fatty Acid Biosynthesis

(2012) Zhiyang Feng et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Expression, purification and characterization of enoyl-ACP reductase II, FabK, from Porphyromonas gingivalis

(2012) Kirk E. Hevener et al.   PROTEIN EXPRESSION AND PURIFICATION

Crystal structure and fluorescence studies reveal the role of helical dimeric interface of staphylococcal fabg1 in positive cooperativity for NADPH

(2012) Debajyoti Dutta et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Structure of the Yersinia pestis FabV Enoyl-ACP Reductase and Its Interaction with Two 2-Pyridone Inhibitors

(2012) Maria W. Hirschbeck et al.   STRUCTURE

The MUT056399 Inhibitor of FabI Is a New Antistaphylococcal Compound

(2011) S. Escaich et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Discovery of vinylogous carbamates as a novel class of β-ketoacyl-acyl carrier protein synthase III (FabH) inhibitors

(2011) Huan-Qiu Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, molecular modeling and biological evaluation of β-ketoacyl-acyl carrier protein synthase III (FabH) as novel antibacterial agents

(2011) Hong-Jia Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, antibacterial activities and molecular docking studies of Schiff bases derived from N-(2/4-benzaldehyde-amino) phenyl-N′-phenyl-thiourea

(2011) Hong-Jia Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of urea derivatives from o-hydroxybenzylamines and phenylisocyanate as potential FabH inhibitors

(2011) Zi-Lin Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dialkylamino-2,4-dihydroxybenzoic Acids as Easily Synthesized Analogues of Platensimycin and Platencin with Comparable Antibacterial Properties

(2011) Jingxin Wang et al.   CHEMISTRY-A EUROPEAN JOURNAL

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

(2011) Joshua B Parsons et al.   CURRENT OPINION IN MICROBIOLOGY

Discovery of a Novel and Potent Class of F. tularensis Enoyl-Reductase (FabI) Inhibitors by Molecular Shape and Electrostatic Matching

(2011) Kirk E. Hevener et al.   JOURNAL OF MEDICINAL CHEMISTRY

Methyl-Branched Fatty Acids, Inhibitors of Enoyl-ACP Reductase with Antibacterial Activity from Streptomyces sp. A251

(2011) Chang Ji Zheng   JOURNAL OF MICROBIOLOGY AND BIOTECHNOLOGY

Metabolic basis for the differential susceptibility of Gram-positive pathogens to fatty acid synthesis inhibitors

(2011) J. B. Parsons et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Dimeric and tetrameric forms of enoyl-acyl carrier protein reductase from Bacillus cereus

(2010) Su Jin Kim et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Mechanism and Inhibition of the FabV Enoyl-ACP Reductase fromBurkholderia mallei

(2010) Hao Lu et al.   BIOCHEMISTRY

Synthesis, molecular modeling and biological evaluation of PSB as targeted antibiotics

(2010) Kui Cheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of novel deoxybenzoin derivatives as FabH inhibitors and anti-inflammatory agents

(2010) Huan-Qiu Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, and structure–activity relationships of pyrazole derivatives as potential FabH inhibitors

(2010) Peng-Cheng Lv et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Syntheses and Antibacterial Properties of iso-Platencin, Cl-iso-Platencin and Cl-Platencin: Identification of a New Lead Structure

(2010) Konrad Tiefenbacher et al.   CHEMISTRY-A EUROPEAN JOURNAL

Design and synthesis of potent inhibitors of β-ketoacyl-acyl carrier protein synthase III (FabH) as potential antibacterial agents

(2010) Lei Shi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Slow, Tight Binding Inhibitor of InhA, the Enoyl-Acyl Carrier Protein Reductase fromMycobacterium tuberculosis

(2010) Sylvia R. Luckner et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Crystal Structures of Enoyl-ACP Reductases I (FabI) and III (FabL) from B. subtilis

(2010) Kook-Han Kim et al.   JOURNAL OF MOLECULAR BIOLOGY

Essentiality of FASII pathway for Staphylococcus aureus

(2010) Wendy Balemans et al.   NATURE

Slow-Onset Inhibition of the FabI Enoyl Reductase fromFrancisella tularensis: Residence Time andin VivoActivity

(2009) Hao Lu et al.   ACS Chemical Biology

AFN-1252, a FabI Inhibitor, Demonstrates a Staphylococcus-Specific Spectrum of Activity

(2009) J. A. Karlowsky et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Triclosan Resistance of Pseudomonas aeruginosa PAO1 Is Due to FabV, a Triclosan-Resistant Enoyl-Acyl Carrier Protein Reductase

(2009) L. Zhu et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Campylobacter jejuni fatty acid synthase II: Structural and functional analysis of β-hydroxyacyl-ACP dehydratase (FabZ)

(2009) Andrew S. Kirkpatrick et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Aquastatin A, a New Inhibitor of Enoyl-Acyl Carrier Protein Reductase from Sporothrix sp. FN611

(2009) Yun-Ju Kwon et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Novel E. coli β-ketoacyl-acyl carrier protein synthase III inhibitors as targeted antibiotics

(2009) Jee-Young Lee et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, antibacterial activities and molecular docking studies of peptide and Schiff bases as targeted antibiotics

(2009) Kui Cheng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis of C(7) modified chrysin derivatives designing to inhibit β-ketoacyl-acyl carrier protein synthase III (FabH) as antibiotics

(2009) Huan-Qiu Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors

(2009) Peng-Cheng Lv et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and biological evaluation of platensimycin analogs

(2009) Hong C. Shen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Isolation, enzyme-bound structure and antibacterial activity of platencin A1 from Streptomyces platensis

(2009) Sheo B. Singh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

2,3,4,5-Tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines as inhibitors of the bacterial enoyl ACP reductase, FabI

(2009) Jailall Ramnauth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI)

(2009) Peter B. Sampson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers

(2009) Jingjing Yao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Diversity in enoyl-acyl carrier protein reductases

(2009) R. P. Massengo-Tiassé et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

Crystal structures of bacterial FabH suggest a molecular basis for the substrate specificity of the enzyme

(2009) Ketan S. Gajiwala et al.   FEBS LETTERS

Isolation, structure and biological activities of platensimycin B4 from Streptomyces platensis

(2009) Chaowei Zhang et al.   JOURNAL OF ANTIBIOTICS

Vinaxanthone, a new FabI inhibitor from Penicillium sp.

(2009) C. J. Zheng et al.   JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY

Heterologous Expression of Mycobacterial Proteins in Saccharomyces cerevisiae Reveals Two Physiologically Functional 3-Hydroxyacyl-Thioester Dehydratases, HtdX and HtdY, in Addition to HadABC and HtdZ

(2009) A. Gurvitz et al.   JOURNAL OF BACTERIOLOGY

Discovering Potent Inhibitors Against the β-Hydroxyacyl-Acyl Carrier Protein Dehydratase (FabZ) ofHelicobacter pylori: Structure-Based Design, Synthesis, Bioassay, and Crystal Structure Determination†

(2009) Lingyan He et al.   JOURNAL OF MEDICINAL CHEMISTRY

Type II fatty acid synthesis is not a suitable antibiotic target for Gram-positive pathogens

(2009) Sophie Brinster et al.   NATURE

Identification of 2-Aminothiazole-4-Carboxylate Derivatives Active against Mycobacterium tuberculosis H37Rv and the β-Ketoacyl-ACP Synthase mtFabH

(2009) Qosay Al-Balas et al.   PLoS One

Molecular basis for triclosan activity involves a flipping loop in the active site

(2009) Xiayang Qiu et al.   PROTEIN SCIENCE

Structural insights intoStaphylococcus aureusenoyl-ACP reductase (FabI), in complex with NADP and triclosan

(2009) Amit Priyadarshi et al.   PROTEINS-STRUCTURE FUNCTION AND BIOINFORMATICS

Natural product juglone targets three key enzymes fromHelicobacter pylori: inhibition assay with crystal structure characterization1

(2008) Yun-hua KONG et al.   ACTA PHARMACOLOGICA SINICA

Unsymmetric aryl–alkyl disulfide growth inhibitors of methicillin-resistant Staphylococcus aureus and Bacillus anthracis

(2008) Edward Turos et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase

(2008) Suresh K. Tipparaju et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and in vitro antimycobacterial activity of B-ring modified diaryl ether InhA inhibitors

(2008) Christopher W. am Ende et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Isolation, structure and fatty acid synthesis inhibitory activities of platensimycin B1–B3 from Streptomyces platensis

(2008) Chaowei Zhang et al.   CHEMICAL COMMUNICATIONS

Structure and Semisynthesis of Platensimide A, Produced byStreptomyces platensis

(2008) Kithsiri B. Herath et al.   ORGANIC LETTERS

Inhibiting enoyl-ACP reductase (FabI) across pathogenic microorganisms by linear sesquiterpene lactones from Anthemis auriculata

(2008) Anastasia Karioti et al.   PHYTOMEDICINE

Crystal structure of enoyl-acyl carrier protein reductase (FabK) fromStreptococcus pneumoniaereveals the binding mode of an inhibitor

(2008) Jun Saito et al.   PROTEIN SCIENCE

Structure of homoplatensimide A: a potential key biosynthetic intermediate of platensimycin isolated from Streptomyces platensis

(2008) Hiranthi Jayasuriya et al.   TETRAHEDRON LETTERS

The crystal structure of PfFabZ, the unique β-hydroxyacyl-ACP dehydratase involved in fatty acid biosynthesis of Plasmodium falciparum

(2005) Dirk Kostrewa et al.   PROTEIN SCIENCE

Antibiotics: Actions, origins, resistance, by C. Walsh. 2003. Washington, DC: ASM Press. 345 pp. $99.95 (hardcover).

(2004) Hans Von Döhren   PROTEIN SCIENCE