Design and Synthesis of Covalent Inhibitors of FabA

Autor: James S. Martin, Claire J. Mackenzie, De Lin, Nadine Homeyer, David W. Gray, Fabio Zuccotto, Ian H. Gilbert

Publikováno v: ACS Omega. 8:12787-12804

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3ce02eeb04ff7b9d23bcab7c2b09d305
https://doi.org/10.1021/acsomega.2c08031

Synthesis of a Series of Diaminoindoles

Autor: Claire J. MacKenzie, Ian H. Gilbert, James Martin

Publikováno v: The Journal of Organic Chemistry

A selection of 3,4-diaminoindoles were required for a recent drug discovery project. To this end, a 10-step synthesis was developed from 4-nitroindole. This synthesis was subsequently adapted and used to synthesize 3,5-; 3,6-; and 3,7-diaminoindoles

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8af9200db1347cd4aaebdca1490c6916
https://pubmed.ncbi.nlm.nih.gov/34351743

Screening of a Novel Fragment Library with Functional Complexity against Mycobacterium tuberculosis InhA

Autor: Peter C. Ray, Margaret Huggett, Robert H. Bates, Paco De Dios Anton, Daniel A. Fletcher, Chun-wa Chung, Alfonso Mendoza-Losana, Simon Green, Jingkun Zeng, Fabio Zuccotto, David Barros, Lourdes Encinas, Paul G. Wyatt, Claire J. MacKenzie, Raquel Fernandez-Menendez, Máire A. Convery, Federica Prati

Publikováno v: Chemmedchem
'ChemMedChem ', vol: 13, pages: 672-677 (2018)

Our findings reported herein provide support for the benefits of including functional group complexity (FGC) within fragments when screening against protein targets such as Mycobacterium tuberculosis InhA. We show that InhA fragment actives with FGC

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cb7bb532b4852aa902492b02c72ca407
http://europepmc.org/articles/PMC5915743

Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis

Autor: Lucy Ellis, Yumi Park, Ola Epemolu, Paul G. Wyatt, Stefano Donini, Laura E. Via, Carolyn Selenski, Matthew Axtman, Thomas R. Ioerger, Menico Rizzi, Tom L. Blundell, Nian Zhou, Simon Green, Olalla Sanz, Maria Osuna-Cabello, David B. Ascher, Helena I. Boshoff, Laste Stojanovski, Travis Hartman, Dale J. Kempf, Clifton E. Barry, Joël Lelièvre, Tracy Bayliss, Zhe Wang, Fred Simeons, Claire J. MacKenzie, Hannah Pflaumer, Valerie Mizrahi, Fabio Zuccotto, James C. Sacchettini, Gracia Santos Diaz, Véronique Dartois, Angela Pacitto, Susan Davis, Kyu Y. Rhee, Laura A. T. Cleghorn, Margaret Huggett, Matthew D. Kurnick, Dinakaran Murugesan, Penelope A. Turner, Kriti Arora, Gerard Drewes, Lluis Ballell, Markus Bösche, Gail M. Freiberg, Kevin D. Read, Surendranadha Reddy Jonnala, Kirsteen I. Buchanan, Maria Jose Lafuente-Monasterio, María José Rebollo-López, Sonja Ghidelli-Disse, Peter C. Ray, Alasdair Smith, Myron Srikumaran, Ardala Breda

Publikováno v: Repositorio Institucional de la Consejería de Sanidad de la Comunidad de Madrid
Consejería de Sanidad de la Comunidad de Madrid

A potent, noncytotoxic indazole sulfonamide was identified by high-throughput screening of >100,000 synthetic compounds for activity against Mycobacterium tuberculosis (Mtb). This noncytotoxic compound did not directly inhibit cell wall biogenesis bu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::896be08dd9046b3b0b9f82d81de880f5
https://doi.org/10.1021/acsinfecdis.6b00103

Correction for Arora et al., 'Respiratory Flexibility in Response to Inhibition of Cytochrome

Autor: Kriti, Arora, Bernardo, Ochoa-Montaño, Patricia S, Tsang, Tom L, Blundell, Stephanie S, Dawes, Valerie, Mizrahi, Tracy, Bayliss, Claire J, Mackenzie, Laura A T, Cleghorn, Peter C, Ray, Paul G, Wyatt, Eugene, Uh, Jinwoo, Lee, Clifton E, Barry, Helena I, Boshoff

Publikováno v: Antimicrobial agents and chemotherapy. 61(9)

We report here a series of five chemically diverse scaffolds that have in vitro activities on replicating and hypoxic nonreplicating bacilli by targeting the respiratory bc1 complex in Mycobacterium tuberculosis in a strain-dependent manner. Deletion

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::180dcd622cce8f6a973ff754bb677823
https://pubmed.ncbi.nlm.nih.gov/25155596