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Full-Text Articles in Social and Behavioral Sciences

Central Administrations Of Palmitic Acid And Arachidonic Acid Decrease Central Leptin Sensitivity In Mice, L Cheng, Xu-Feng Huang, Y Yu Jun 2016

Central Administrations Of Palmitic Acid And Arachidonic Acid Decrease Central Leptin Sensitivity In Mice, L Cheng, Xu-Feng Huang, Y Yu

Xu-Feng Huang

Purpose: Leptin inhibits feeding and increases energy expenditure through the central nervous system. High-fat diet with saturated fatty acids (SFA) or n-6 polyunsaturated fatty acids (n-6 PUFA) has been reported to induce central leptin resistance and obesity. However, little is known if central administration of SFA or n-6 PUFA can reduce central leptin sensitivity. This study examined the central leptin sensitivity in response to intracerebroventricular (i.c.v.) injection of SFA, palmitic acid (PA) and n-6 PUFA, arachidonic acid (ARA) in mice. Methods: After overnight fasting, C57BL/6J male mice (n=24/group) were i.c.v. injected with either PA (50pmol/2ul), ARA (50pmol/2ul) or vehicle (saline, …


A Neuregulin 1 Transmembrane Domain Mutation Causes Imbalanced Glutamatergic And Dopaminergic Receptor Expression In Mice, K A. Newell, T Karl, Xu-Feng Huang Jun 2016

A Neuregulin 1 Transmembrane Domain Mutation Causes Imbalanced Glutamatergic And Dopaminergic Receptor Expression In Mice, K A. Newell, T Karl, Xu-Feng Huang

Xu-Feng Huang

The neuregulin 1 gene has repeatedly been identified as a susceptibility gene for schizophrenia, thus mice with genetic mutations in this gene offer a valuable tool for studying the role of neuregulin 1 in schizophrenia-related neurotransmission. In this study, slide-based receptor autoradiography was used to quantify glutamatergic N-methyl-d-aspartate (NMDA), dopaminergic D2, cannabinoid CB1 and acetylcholine M1/4 receptor levels in the brains of male heterozygous transmembrane domain neuregulin 1 mutant (Nrg1+/−) mice at two ages. Mutant mice expressed small but significant increases in NMDA receptor levels in the cingulate cortex (7%, p = 0.044), sensory cortex (8%, p = 0.024), and …


An Analysis Of Metabotropic Glutamate Receptors 2/3 And 5 In Schizophrenia, Major Depression And Bipolar Disorder From The Stanley Neuropathology Consortium, N Matosin, E Frank, F Fernandez, C Deng, J Wong, Xu-Feng Huang, K A. Newell Jun 2016

An Analysis Of Metabotropic Glutamate Receptors 2/3 And 5 In Schizophrenia, Major Depression And Bipolar Disorder From The Stanley Neuropathology Consortium, N Matosin, E Frank, F Fernandez, C Deng, J Wong, Xu-Feng Huang, K A. Newell

Xu-Feng Huang

Purpose: Metabotropic glutamate receptors (mGluRs) are proposed novel therapeutic targets for a variety of brain disorders such as schizophrenia (SZ), bipolar disorder (BP) and major depression (MD). Despite their potential, the involvement of these receptors in these pathological processes is uncertain. This information is crucial to understand the efficiency of drugs that target these receptors. Methods: Using post-mortem human brains, mGluR2/3 and mGluR5 binding densities were measured in the anterior cingulate cortex of SZ, BP, MD and matched controls (CT) (n=15/group) by receptor autoradiography. Results: Whilst preliminary analyses indicated no diagnostic effect in mGluR2/3 or mGluR5 binding densities, mGluR2/3 binding …


A Neuregulin 1 Transmembrane Domain Mutation Causes Imbalanced Glutamatergic And Dopaminergic Receptor Expression In Mice, K A. Newell, T Karl, Xu-Feng Huang Jun 2016

A Neuregulin 1 Transmembrane Domain Mutation Causes Imbalanced Glutamatergic And Dopaminergic Receptor Expression In Mice, K A. Newell, T Karl, Xu-Feng Huang

Xu-Feng Huang

The neuregulin 1 gene has repeatedly been identified as a susceptibility gene for schizophrenia, thus mice with genetic mutations in this gene offer a valuable tool for studying the role of neuregulin 1 in schizophrenia-related neurotransmission. In this study, slide-based receptor autoradiography was used to quantify glutamatergic N-methyl-d-aspartate (NMDA), dopaminergic D2, cannabinoid CB1 and acetylcholine M1/4 receptor levels in the brains of male heterozygous transmembrane domain neuregulin 1 mutant (Nrg1+/−) mice at two ages. Mutant mice expressed small but significant increases in NMDA receptor levels in the cingulate cortex (7%, p = 0.044), sensory cortex (8%, p = 0.024), and …


Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine Nov 2013

Anti-Cancer Activity Of An Acid-Labile N-Alkylisatin Conjugate Targeting The Transferrin Receptor, Vineesh Indira Chandran, Lidia Matesic, Julie Locke, Danielle Skropeta, Marie Ranson, Kara Vine

Danielle Skropeta

We have previously reported a series of pH-sensitive imine-linked N-alkylisatin prodrugs that are stable at pH 7.4, but readily cleaved at pH 4.5. Herein, one of the most potent prodrugs, 5,7-dibromo-N-(pmethoxybenzyl) isatin (NAI), was functionalized with a para-phenylpropionic acid linker, and the resulting NAI–imine prodrug conjugated to transferrin (Tf) to form a NAI–imine–Tf conjugate. Cytotoxicity assays revealed the conjugate was equipotent to the free drug against MCF-7 breast cancer cells, with clear selectivity patterns based on TfR levels. These results suggest that this novel isatin-based cytotoxin conjugated to a tumor targeting protein via an acid-labile linker warrants further preclinical testing.


The Effect Of Individual N-Glycans On Enzyme Activity, Danielle Skropeta Nov 2013

The Effect Of Individual N-Glycans On Enzyme Activity, Danielle Skropeta

Danielle Skropeta

No abstract provided.


Domino Pericyclic Reactions Of Acyclic Conjugated (E,Z,E,E)-Tetraenes, Danielle Skropeta, Rodney Rickards Nov 2013

Domino Pericyclic Reactions Of Acyclic Conjugated (E,Z,E,E)-Tetraenes, Danielle Skropeta, Rodney Rickards

Danielle Skropeta

No abstract provided.


N-Phenethyl And N-Naphthylmethyl Isatins And Analogues As In Vitro Cytotoxic Agents, John Bremner, Stephen Pyne, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow Nov 2013

N-Phenethyl And N-Naphthylmethyl Isatins And Analogues As In Vitro Cytotoxic Agents, John Bremner, Stephen Pyne, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow

Danielle Skropeta

Arange of N-phenethyl,N-phenacyl, and N-(1- and 2-naphthylmethyl) derivatives of 5,7-dibromoisatin 2 were prepared byN-alkylation reactions. Their activity against human monocyte-like histiocytic lymphoma (U937), leukemia (Jurkat), and breast carcinoma (MDA-MB-231) cell lines was assessed. The results allowed further development of structureactivity relationships. The compound 5,7-dibromo-N-(1-naphthylmethyl)-1H-indole-2,3-dione 5a was the most potent against U937 cells with an IC50 value of 0.19 microM.


Complete Assignment Of The 1h And 13c Nmr Spectra Of Antimicrobial 4-Arylamino- 3-Nitrocoumarin Derivatives, Vidoslav Dekic, Niko Radulovic, Rastko Vukicevic, Biljana Dekic, Danielle Skropeta, Radosav Palic Nov 2013

Complete Assignment Of The 1h And 13c Nmr Spectra Of Antimicrobial 4-Arylamino- 3-Nitrocoumarin Derivatives, Vidoslav Dekic, Niko Radulovic, Rastko Vukicevic, Biljana Dekic, Danielle Skropeta, Radosav Palic

Danielle Skropeta

No abstract provided.


Synthesis And Hydrolytic Evaluation Of Acid-Labile Imine-Linked Cytoxic Isatin Model Systems, Lidia Matesic, Julie Locke, Kara Perrow, Marie Ranson, John Bremner, Danielle Skropeta Nov 2013

Synthesis And Hydrolytic Evaluation Of Acid-Labile Imine-Linked Cytoxic Isatin Model Systems, Lidia Matesic, Julie Locke, Kara Perrow, Marie Ranson, John Bremner, Danielle Skropeta

Danielle Skropeta

In this study a series of isatin-based, pH-sensitive aryl imine derivatives with differing aromatic substituents and substitution patterns were synthesised and their acid-catalysed hydrolysis evaluated. These derivatives were functionalised at the C3 carbonyl group of a potent N-substituted isatin cytotoxin and were stable at physiological pH but readily cleaved at pH 4.5. Observed rates of hydrolysis for the embedded imine-acid moiety were in the order para-phenylpropionic acid>phenylacetic acid (para>meta)>benzoic acid (meta>para). The ability to fine-tune hydrolysis rates in this way has potential implications for optimising imine linked, tumour targeting cytotoxin-protein conjugates


N-Glycolisation Regulates Endothelial Lipase-Mediated Phospholipid Hydrolysis In Apoe- And Apoa-I-Containing High Density Lipoproteins, Danielle Skropeta, Daniel Rader, Weijun Jin, Monica Mcmahon, Kate Shearston, Philip Barter, Kristine Mcgrath, Kerry-Anne Rye, Chatri Settasatian, Daniela Caiazza Nov 2013

N-Glycolisation Regulates Endothelial Lipase-Mediated Phospholipid Hydrolysis In Apoe- And Apoa-I-Containing High Density Lipoproteins, Danielle Skropeta, Daniel Rader, Weijun Jin, Monica Mcmahon, Kate Shearston, Philip Barter, Kristine Mcgrath, Kerry-Anne Rye, Chatri Settasatian, Daniela Caiazza

Danielle Skropeta

No abstract provided.


Cytotoxic And Anticancer Activities Of Isatin And Its Derivatives: A Comprehensive Review From 2000-2008, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow Nov 2013

Cytotoxic And Anticancer Activities Of Isatin And Its Derivatives: A Comprehensive Review From 2000-2008, Marie Ranson, Danielle Skropeta, Julie Locke, Lidia Matesic, Kara Perrow

Danielle Skropeta

No abstract provided.


Chemotaxonomy Of The Peppergrass Lepidium Coronopus (L.) Al-Shehbaz (Syn. Coronopus Squamatus) Based On Its Volatile Glucosinolate Autolysis Products, Niko Radulovic, Bojan Zlatkovic, Danielle Skropeta, Radosav Palic´ Nov 2013

Chemotaxonomy Of The Peppergrass Lepidium Coronopus (L.) Al-Shehbaz (Syn. Coronopus Squamatus) Based On Its Volatile Glucosinolate Autolysis Products, Niko Radulovic, Bojan Zlatkovic, Danielle Skropeta, Radosav Palic´

Danielle Skropeta

The genus Lepidium comprises approximately 175 different plant species commonly referred to as peppergrasses or pepperworts ( Al-Shehbaz, 1997 and Mummenhoff et al., 2001), which occur worldwide apart from the polar regions where they are considered rare in the Arctic and are absent from Antarctica. Lepidium is a comparatively large genus belonging to the mustard family Brassicaceae. Lepidium coronopus (L.) Al-Shehbaz, a representative of the genus, is a herbaceous annual to biennial plant that belongs to the tribe Lepidieae and has previously been described by the following synonymous species: Coronopus squamatus (Forsskal) Ascherson; C. squamatus subsp. conradi (Muschler) Maire; C. …


Teasaponin Improves Central Leptin Sensitivity In High-Fat Diet-Induced Obese Mice, Y Wu, Xu-Feng Huang, Y Yu Sep 2013

Teasaponin Improves Central Leptin Sensitivity In High-Fat Diet-Induced Obese Mice, Y Wu, Xu-Feng Huang, Y Yu

Yizhen Wu

Purpose: Leptin promotes negative energy balance by suppressing energy intake (EI) and elevating energy expenditure through its central action. Central leptin resistance is a hallmark of diet-induced obesity (DIO). Oral administration of teasaponin (TS) can reduce body weight and fat mass. However, little is known if TS has benefit effect in improving central leptin sensitivity. This study investigated the effects of TS on central leptin sensitivity and leptin signalling in the hypothalamic arcuate nucleus (Arc) of DIO mice. Methods: After 15 weeks of high-fat diet, DIO mice (n=40) were divided into two groups received either intraperitoneal (ip) injection of TS …


Time-Dependent Ghrelinergic Signaling And Hyperphagia Induced By Olanzapine, Q Zhang, M He, J Lian, C Deng, Xu-Feng Huang Aug 2013

Time-Dependent Ghrelinergic Signaling And Hyperphagia Induced By Olanzapine, Q Zhang, M He, J Lian, C Deng, Xu-Feng Huang

Qingsheng Zhang

Olanzapine is widely used to treat schizophrenia and other mental diseases. Interestingly, although increased body weight is evident throughout the course of olanzapine treatment, elevated food intake only appears in relatively shorter term. Olanzapine can modulate ghrelin levels, which may upregulate neuropeptide Y (NPY) secretion at hypothalamus. Brain-specific homeobox transcription factor (BSX) may also be involved in ghrelin-induced hyperphagia. PURPOSE: To investigate the effect of olanzapine on central NPY, BSX and plasma ghrelin levels, and their relationship to food intake. METHODS: Rats were treated with olanzapine (1mg/kg, orally, 3x/day, n=12/group) or vehicle for 1 week, 2 weeks, or 5 weeks. …


Time-Dependant Alterations Of Hypothalamic Energy Regulatory Network By Olanzapine In Rats, Q Zhang, M He, Hongqin Wang, J Lian, C Deng, Xu-Feng Huang Aug 2013

Time-Dependant Alterations Of Hypothalamic Energy Regulatory Network By Olanzapine In Rats, Q Zhang, M He, Hongqin Wang, J Lian, C Deng, Xu-Feng Huang

Qingsheng Zhang

Abstract of a paper that presented at the Australian Neuroscience Society 32nd Annual meeting.


Apolipoprotein J And Leptin Levels In Patients With Coronary Heart Disease, Mark Wilson, Dimitri Mikhailidis, Maria Poulakou, Christos Tsigris, Despina Perrea, Kosmas Paraskevas, Dimitrios Iliopoulos May 2013

Apolipoprotein J And Leptin Levels In Patients With Coronary Heart Disease, Mark Wilson, Dimitri Mikhailidis, Maria Poulakou, Christos Tsigris, Despina Perrea, Kosmas Paraskevas, Dimitrios Iliopoulos

Mark R Wilson

No abstract provided.


Ozone-Induced Dissociation On A Modified Tandem Linear Ion-Trap: Observations Of Different Reactivity For Isomeric Lipids, Berwyck Poad, Huong Pham, Michael Thomas, Jessica Hughes, J Campbell, Todd Mitchell, Stephen Blanksby May 2013

Ozone-Induced Dissociation On A Modified Tandem Linear Ion-Trap: Observations Of Different Reactivity For Isomeric Lipids, Berwyck Poad, Huong Pham, Michael Thomas, Jessica Hughes, J Campbell, Todd Mitchell, Stephen Blanksby

Berwyck L. J. Poad

Ozone-induced dissociation (OzID) exploits the gas-phase reaction between mass-selected lipid ions and ozone vapor to determine the position(s) of unsaturation. In this contribution, we describe the modification of a tandem linear ion-trap mass spectrometer specifically for OzID analyses wherein ozone vapor is supplied to the collision cell. This instrumental configuration provides spatial separation between mass-selection, the ozonolysis reaction, and mass-analysis steps in the OzID process and thus delivers significant enhancements in speed and sensitivity (ca. 30-fold). These improvements allow spectra revealing the double-bond position(s) within unsaturated lipids to be acquired within 1 s: significantly enhancing the utility of OzID in …


The Effects Of Phencyclidine Treatment On The Nmdar-Nrg1 Signalling Pathway In Rats, T Morosin, T Du Bois, K Newell, Xu-Feng Huang Apr 2013

The Effects Of Phencyclidine Treatment On The Nmdar-Nrg1 Signalling Pathway In Rats, T Morosin, T Du Bois, K Newell, Xu-Feng Huang

Xu-Feng Huang

No abstract provided.


Diagnostic-Specific Reductions In Nmda And Mglu5 Glutamatergic Receptors In Schizophrenia, K Newell, N Jimenez, A Geddes, E Frank, T Du Bois, M Safadi, Xu-Feng Huang Apr 2013

Diagnostic-Specific Reductions In Nmda And Mglu5 Glutamatergic Receptors In Schizophrenia, K Newell, N Jimenez, A Geddes, E Frank, T Du Bois, M Safadi, Xu-Feng Huang

Xu-Feng Huang

Abstract of a paper that presented at the Australian Neuroscience Society 32nd Annual meeting


Effects Of Dopamine D2 Receptor Partial Agonist Bifeprunox On Body Weight Gain, Food And Water Intake In Male Rats, M De Santis, Xu-Feng Huang, C Deng Apr 2013

Effects Of Dopamine D2 Receptor Partial Agonist Bifeprunox On Body Weight Gain, Food And Water Intake In Male Rats, M De Santis, Xu-Feng Huang, C Deng

Xu-Feng Huang

An abstract of a poster presentation that presented at Australian Neuroscience Society 32nd Annual meeting.


Metabotropic Glutamate Receptor Subtype 5 Is Reduced In Schizophrenia Subjects With Comorbid Major Depression And Unchanged Following Antipsychotic Drug Treatment, N Jimenez, Xu-Feng Huang, C Deng, K Newell Apr 2013

Metabotropic Glutamate Receptor Subtype 5 Is Reduced In Schizophrenia Subjects With Comorbid Major Depression And Unchanged Following Antipsychotic Drug Treatment, N Jimenez, Xu-Feng Huang, C Deng, K Newell

Xu-Feng Huang

Abstract of a paper that presented at the Australian Neuroscience Society 32nd Annual meeting.


Time-Dependant Alterations Of Hypothalamic Energy Regulatory Network By Olanzapine In Rats, Q Zhang, M He, Hongqin Wang, J Lian, C Deng, Xu-Feng Huang Apr 2013

Time-Dependant Alterations Of Hypothalamic Energy Regulatory Network By Olanzapine In Rats, Q Zhang, M He, Hongqin Wang, J Lian, C Deng, Xu-Feng Huang

Xu-Feng Huang

Abstract of a paper that presented at the Australian Neuroscience Society 32nd Annual meeting.


Mglur5 And Nmda Receptor Density Are Reduced In The Dorsolateral Prefrontal Cortex Of Schizoaffective But Not Schizophrenia Patients, Kelly Newell, Natalie Matosin, Elisabeth Frank, Chao Deng, Xu-Feng Huang Apr 2013

Mglur5 And Nmda Receptor Density Are Reduced In The Dorsolateral Prefrontal Cortex Of Schizoaffective But Not Schizophrenia Patients, Kelly Newell, Natalie Matosin, Elisabeth Frank, Chao Deng, Xu-Feng Huang

Xu-Feng Huang

Abstract of a poster that presented at the Society of Biological Psychiatry 67th Annual Meeting.


Gender Differences In Cognitive Function Of Patients With Chronic Schizophrenia, Mei Han, Xu-Feng Huang, Da Chen, Mei Xiu, Li Hui, Haibo Liu, Thomas Kosten, Xiang Zhang Feb 2013

Gender Differences In Cognitive Function Of Patients With Chronic Schizophrenia, Mei Han, Xu-Feng Huang, Da Chen, Mei Xiu, Li Hui, Haibo Liu, Thomas Kosten, Xiang Zhang

Xu-Feng Huang

Schizophrenic patients have cognitive impairments, but gender differences in these cognitive deficits have had limited study. This study assessed cognitive functioning in 471 subjects including 122 male and 78 female schizophrenic patients and 141 male and 130 female healthy controls. We found that immediate memory, language, delayed memory and total RBANS scores were significantly decreased in schizophrenia compared with healthy controls for both genders. Male patients had significant lower immediate memory, delayed memory and total RBANS scores than female patients, and healthy controls showed a similar gender difference. The RBANS showed modest correlations with PANSS scores, duration of illness and …


Oat Β-Glucan Increases Postprandial Cholecystokinin Levels, Decreases Insulin Response And Extends Subjective Satiety In Overweight Subjects, Eleanor Beck, Susan Tosh, Marijka Batterham, Linda Tapsell, Xu-Feng Huang Feb 2013

Oat Β-Glucan Increases Postprandial Cholecystokinin Levels, Decreases Insulin Response And Extends Subjective Satiety In Overweight Subjects, Eleanor Beck, Susan Tosh, Marijka Batterham, Linda Tapsell, Xu-Feng Huang

Xu-Feng Huang

This study recorded acute biochemical and subjective measures of satiety, followed by energy intake from a subsequent meal, after varying doses of β-glucan in extruded breakfast cereals. Molecular weight, solubility and viscosity of β-glucan products were determined. Seven male and seven female subjects (BMI 25–36 kg/m) consumed five breakfasts (different doses of β-glucan sourced from two different technological processes) and dietary intake was measured after four hours. Blood was collected to measure glucose, insulin, ghrelin and cholecystokinin, and visual analogue scales measured subjective satiety. Molecular weight, solubility and viscosity indicated products were likely to increase luminal viscosity. β-Glucan was found …


Diet High In Oat Β-Glucan Activates The Gut-Hypothalamic (Pyy3-36-Npy) Axis And Increases Satiety In Diet-Induced Obesity In Mice, Xu-Feng Huang, Yinghua Yu, Eleanor Beck, Timothy South, Yulin Li, Marijka Batterham, Linda Tapsell, Jiezhong Chen Feb 2013

Diet High In Oat Β-Glucan Activates The Gut-Hypothalamic (Pyy3-36-Npy) Axis And Increases Satiety In Diet-Induced Obesity In Mice, Xu-Feng Huang, Yinghua Yu, Eleanor Beck, Timothy South, Yulin Li, Marijka Batterham, Linda Tapsell, Jiezhong Chen

Xu-Feng Huang

This study tested the effects of (1-3),(1-4) b-D-glucan from oats, on activation of the guthypothalamic (PYY3–36-NPY) axis, satiety, and weight loss in diet-induced obesity (DIO) mice. DIO mice were fed standard lab chow diets or varied doses of b-glucan for 6 weeks. Energy intake, satiety, body weight changes and peptide Y-Y3-36 (PYY3-36) were measured together with a satiety test and measurement of neuropeptide Y (NPY) mRNA expression in the hypothalamic arcuate nucleus (Arc). The average energy intake (-13%, po0.05) and body weight gain was lower with increasing b-glucan over 6 wk with acute suppression of energy intake over 4 h. …


Synthesis Of Functionalised 2-Aryl-5-Nitro-1h-Indoles And Their Activity As Bacterial Nora Efflux Pump Inhibitors, John Bremner, Siritron Samosorn, Anthony Ball, Kim Lewis Jan 2013

Synthesis Of Functionalised 2-Aryl-5-Nitro-1h-Indoles And Their Activity As Bacterial Nora Efflux Pump Inhibitors, John Bremner, Siritron Samosorn, Anthony Ball, Kim Lewis

Kim Lewis

No abstract provided.


Conjugating Berberine To A Multidrug Resistance Pump Inhibitor Creates An Effective Antimicrobial, John Bremner, Siritron Samosorn, Anthony Ball, Gabriele Casadei, Terence Moy, Frederik Ausubel, Kim Lewis Jan 2013

Conjugating Berberine To A Multidrug Resistance Pump Inhibitor Creates An Effective Antimicrobial, John Bremner, Siritron Samosorn, Anthony Ball, Gabriele Casadei, Terence Moy, Frederik Ausubel, Kim Lewis

Kim Lewis

No abstract provided.


Structure-Activity Relationships Of 2-Aryl-1h-Indole Inhibitors Of The Nora Efflux Pump In Staphylococcus Aureus, John Bremner, Michael Kelso, Joseph Ambrus, Kim Lewis, Anthony Ball, Gabriele Casadei Jan 2013

Structure-Activity Relationships Of 2-Aryl-1h-Indole Inhibitors Of The Nora Efflux Pump In Staphylococcus Aureus, John Bremner, Michael Kelso, Joseph Ambrus, Kim Lewis, Anthony Ball, Gabriele Casadei

Kim Lewis

The synthesis of 22 2-aryl-1H-indoles, including 12 new compounds, has been achieved via Pd- or Rh-mediated methodologies, or selective electrophilic substitution. All three methods were based on elaborations from simple indole precursors. SAR studies on these indoles and 2-phenyl-1H-indole in Staphylococcus aureus as NorA efflux pump inhibitors indicated 5-nitro-2-(3-methoxycarbonyl)phenyl-1H-indole was a slightly more potent inhibitor than the lead INF55. A promising new antibacterial lead compound against S. aureus (2-phenyl-1H-indol-5-yl)-methanol, was also found.