Alastair L. Parkes

The state of the art in dual-acting hybrid antibiotics to combat bacterial resistance

Alastair L. Parkes, Oliver A. Bardell-Cox, Ricky Cain

INTRODUCTION: The efficacy of current treatments for bacterial infections is under threat due to the continuing rise in the prevalence of antimicrobial resistance (AMR). Resistance can arise due to a wide variety of changes in the bacterial cell that prevent the antibiotic …

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Lipid-Modulated, Graduated Inhibition of N-Glycosylation Pathway Priming Suggests Wide Tolerance of ER Proteostasis to Stress

Andrew M. Giltrap, Yin Yao Dong, Stephen A. Cochrane, Thomas M. Krülle et autres

Protein N-glycosylation is a cotranslational modification that takes place in the endoplasmic reticulum (ER). Disruption of this process can result in accumulation of misfolded proteins, known as ER stress. In response, the unfolded protein response (UPR) restores proteostasis or responds by controlling …

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Discovery of Novel UDP- N -Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa

Margret Ryan, Alastair L. Parkes, David F. Corbett, Anthony P. Dickie et autres

This study describes a novel series of UDP- N -acetylglucosamine acyltransferase (LpxA) inhibitors that was identified through affinity-mediated selection from a DNA-encoded compound library. The original hit was a selective inhibitor of Pseudomonas aeruginosa LpxA with no activity against Escherichia coli LpxA. …

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Crystal structure of Escherichia coli LpxA in complex with compound 1

Margret Ryan, Alastair L. Parkes, M. Southey, Ole A. Andersen et autres

Crystal structure of Pseudomonas aeruginosa LpxA in complex with compound 1

Margret Ryan, Alastair L. Parkes, M. Southey, Ole A. Andersen et autres

Antibacterial medicinal chemistry – what can we design for?

Alastair L. Parkes

INTRODUCTION: The need for new antibacterial agents continues to grow, but success in development of antibiotics in recent years has been limited. To improve the chances that new compounds will progress into clinical trials and beyond, it is vital that we consider …

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Hybrid antibiotics – clinical progress and novel designs

Alastair L. Parkes, Ian A. Yule

INTRODUCTION: There is a growing need for new antibacterial agents, but success in development of antibiotics in recent years has been limited. This has led researchers to investigate novel approaches to finding compounds that are effective against multi-drug resistant bacteria, and that …

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CCDC 260374: Experimental Crystal Structure Determination

S.G. Davies, Humberto Rodríguez‐Solla, Juan A. Tamayo, A.R. Cowley et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

CCDC 636363: Experimental Crystal Structure Determination

M.W. Powner, Carole Anastasi, Michael A. Crowe, Alastair L. Parkes et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

RNA: Prebiotic Product, or Biotic Invention

Carole Anastasi, Fabien F. Buchet, Michael A. Crowe, Alastair L. Parkes et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

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On the Prebiotic Synthesis of Ribonucleotides: Photoanomerisation of Cytosine Nucleosides and Nucleotides Revisited

Matthew W. Powner, Carole Anastasi, Michael A. Crowe, Alastair L. Parkes et autres

Recent work has emphasised the importance of D-ribose aminooxazoline 1 in the synthesis of cytidine ribonucleosides under potentially prebiotic conditions. Upon treatment with cyanoacetylene, 1 is transformed into alpha-D-cytidine (alpha-2), and if an efficient means of anomerising this nucleoside or a derivative …

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RNA: Prebiotic Product, or Biotic Invention?

Carole Anastasi, Fabien F. Buchet, Michael A. Crowe, Alastair L. Parkes et autres

Spectacular advances in structural and molecular biology have added support to the 'RNA world' hypothesis, and provide a mandate for chemistry to explain how RNA might have been generated prebiotically on the early earth. Difficulties in achieving a prebiotically plausible synthesis of …

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