Philip G. E. Craven

Exploration of vanoxerine analogues as antibacterial agents

Alexander D. H. Kingdon, Holly V. Adcock, Eleni-Marina Kasimati, Philip G. E. Craven et autres

Mycobacterium tuberculosis is a bacterial pathogen, responsible for approximately 1.3 million deaths in 2022 through tuberculosis infections. The complex treatment regimen required to treat tuberculosis and growing rates of drug resistance, necessitates the development of new anti-mycobacterial agents. One approach is to …

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Azetidines Kill Multidrug-Resistant Mycobacterium tuberculosis without Detectable Resistance by Blocking Mycolate Assembly

Yixin Cui, Alice Lanne, Xudan Peng, Edward P. Browne et autres

High Resolution Image Download MS PowerPoint Slide Tuberculosis (TB) is the leading cause of global morbidity and mortality resulting from infectious disease, with over 10.6 million new cases and 1.4 million deaths in 2021. This global emergency is exacerbated by the emergence …

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Azetidines kill Mycobacterium tuberculosis without detectable resistance by blocking mycolate assembly

Alice Lanne, Yixin Cui, Edward P. Browne, Philip G. E. Craven et autres

Abstract Tuberculosis (TB) is the leading cause of global morbidity and mortality resulting from infectious disease, with over 10 million new cases and 1.5 million deaths in 2019. This global emergency is exacerbated by the emergence of multi-drug-resistant MDR-TB and extensively-drug-resistant XDR-TB, …

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Novel nitrogen-containing heterocyclics with bactericidal activity against Mycobacterium tuberculosis

Alice Lanne, Yixin Cui, Mariwan Hama Salih, Philip G. E. Craven et autres

Tuberculosis (TB) is the leading cause of global morbidity and mortality caused by an infectious disease, with over 10 million new cases emerging in 2017. This global emergency is exacerbated by the emergence of multi-drug and extensively-drug resistant TB, therefore new drugs …

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2,7-Diazabicyclo[2.2.1]heptanes: novel asymmetric access and controlled bridge-opening

Gary R. Peczkowski, Philip G. E. Craven, Darren Stead, Nigel S. Simpkins

Organocatalysed asymmetric Michael additions of substituted triketopiperazines to enones afford products in high yield and enantiomeric ratio (er). Further modification delivers products possessing natural product (NP) scaffolds including diazabicyclo[2.2.1]heptane, prolinamide and harmicine.

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CCDC 1880502: Experimental Crystal Structure Determination

Gary R. Peczkowski, Philip G. E. Craven, Darren Stead, Nigel S. Simpkins

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 1880503: Experimental Crystal Structure Determination

Gary R. Peczkowski, Philip G. E. Craven, Darren Stead, Nigel S. Simpkins

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, …

Phosphino-Triazole Ligands for Palladium-Catalyzed Cross-Coupling

Yiming Zhao, Huy V. Nguyen, Louise Male, Philip G. E. Craven et autres

Twelve 1,5-disubtituted and fourteen 5-substituted 1,2,3-triazole derivatives bearing diaryl or dialkyl phosphines at the 5-position were synthesized and used as ligands for palladium-catalyzed Suzuki-Miyaura cross-coupling reactions. Bulky substrates were tested, and lead-like product formation was demonstrated. The online tool SambVca2.0 was used …

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Phosphino-Triazole Ligands for Palladium-Catalysed Cross-Coupling

Yiming Zhao, Huy V. Nguyen, Louise Male, Philip G. E. Craven et autres

Twelve 1,5-disubtituted and fourteen 5-substituted 1,2,3-triazole derivatives bearing diaryl or dialkyl phosphines at the 5-position were synthesised and used as ligands for palladium-catalysed Suzuki-Miyaura cross-coupling reactions. Bulky substrates were tested, and lead-like product formation was demonstrated. The online tool SambVca 2.0 was …

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Realisation of small molecule libraries based on frameworks distantly related to natural products

A. Aimon, George Karageorgis, Jacob Masters, Mark Dow et autres

The availability of high-quality screening compounds is of paramount importance for the discovery of innovative new medicines. Natural product (NP) frameworks can inspire the design of productive compound libraries. Here, we describe the design and synthesis of four compound libraries based on …

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CCDC 1577645: Experimental Crystal Structure Determination

A. Aimon, George Karageorgis, Jacob Masters, Mark Dow 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, …

Synthesis and Demonstration of the Biological Relevance of sp3‐rich Scaffolds Distantly Related to Natural Product Frameworks

Daniel J. Foley, Philip G. E. Craven, P.M. Collins, Richard G. Doveston et autres

Abstract The productive exploration of chemical space is an enduring challenge in chemical biology and medicinal chemistry. Natural products are biologically relevant, and their frameworks have facilitated chemical tool and drug discovery. A “top‐down” synthetic approach is described that enabled a range …

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