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Carlos Alemparte

Explore the profile of Carlos Alemparte including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 16
Citations 368
Followers 0
Related Specialties
Chemistry
Science
General Medicine
Top 10 Co-Authors
David Barros
Gurdyal S Besra
Katherine A Abrahams
Lluis Ballell
Jonathan A G Cox
Nicholas J Loman
Joaquin Rullas
Jorge Esquivias
Esther Perez-Herran
Modesto J Remuinan
Published In
PLoS One
J Med Chem
J Org Chem
Sci Rep
Org Lett
Affiliations
Soon will be listed here.
Recent Articles
1.
Development of a whole-cell high-throughput phenotypic screen to identify inhibitors of mycobacterial amino acid biosynthesis
Burke C, Abrahams K, Richardson E, Loman N, Alemparte C, Lelievre J, et al.
FASEB Bioadv . 2020 Mar; 1(4):246-254. PMID: 32123830
Anti-tubercular drug discovery continues to be dominated by whole-cell high-throughput screening campaigns, enabling the rapid discovery of new inhibitory chemical scaffolds. Target-based screening is a popular approach to direct inhibitor...
2.
Decaprenylphosphoryl-β-d-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity
Borthwick J, Alemparte C, Wall I, Whitehurst B, Argyrou A, Burley G, et al.
J Med Chem . 2020 Jan; 63(5):2557-2576. PMID: 31922409
Decaprenylphosphoryl-β-d-ribose 2'-epimerase (DprE1) is an essential enzyme in and has recently been studied as a potential drug target, with inhibitors progressing to clinical studies. Here we describe the identification of...
3.
Easy-To-Synthesize Spirocyclic Compounds Possess Remarkable in Vivo Activity against Mycobacterium tuberculosis
Guardia A, Baiget J, Cacho M, Perez A, Ortega-Guerra M, Nxumalo W, et al.
J Med Chem . 2018 Nov; 61(24):11327-11340. PMID: 30457865
Society urgently needs new, effective medicines for the treatment of tuberculosis. To kick-start the required hit-to-lead campaigns, the libraries of pharmaceutical companies have recently been evaluated for starting points. The...
4.
Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656)
Li X, Hernandez V, Rock F, Choi W, Mak Y, Mohan M, et al.
J Med Chem . 2017 Sep; 60(19):8011-8026. PMID: 28953378
There is an urgent need to develop new and safer antitubercular agents that possess a novel mode of action. We synthesized and evaluated a novel series of 3-aminomethyl 4-halogen benzoxaboroles...
5.
Inhibiting mycobacterial tryptophan synthase by targeting the inter-subunit interface
Abrahams K, Cox J, Futterer K, Rullas J, Ortega-Muro F, Loman N, et al.
Sci Rep . 2017 Aug; 7(1):9430. PMID: 28842600
Drug discovery efforts against the pathogen Mycobacterium tuberculosis (Mtb) have been advanced through phenotypic screens of extensive compound libraries. Such a screen revealed sulfolane 1 and indoline-5-sulfonamides 2 and 3...
6.
Novel inhibitors of Mycobacterium tuberculosis GuaB2 identified by a target based high-throughput phenotypic screen
Cox J, Mugumbate G, Del Peral L, Jankute M, Abrahams K, Jervis P, et al.
Sci Rep . 2016 Dec; 6:38986. PMID: 27982051
High-throughput phenotypic screens have re-emerged as screening tools in antibiotic discovery. The advent of such technologies has rapidly accelerated the identification of 'hit' compounds. A pre-requisite to medicinal chemistry optimisation...
7.
THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria
Cox J, Abrahams K, Alemparte C, Ghidelli-Disse S, Rullas J, Angulo-Barturen I, et al.
Nat Microbiol . 2016 Aug; 1:15006. PMID: 27571973
Phenotypic screens for bactericidal compounds against drug-resistant tuberculosis are beginning to yield novel inhibitors. However, reliable target identification remains challenging. Here, we show that tetrahydropyrazo[1,5-a]pyrimidine-3-carboxamide (THPP) selectively pulls down EchA6...
8.
Biochemical and structural characterization of mycobacterial aspartyl-tRNA synthetase AspS, a promising TB drug target
Gurcha S, Usha V, Cox J, Futterer K, Abrahams K, Bhatt A, et al.
PLoS One . 2014 Nov; 9(11):e113568. PMID: 25409504
The human pathogen Mycobacterium tuberculosis is the causative agent of pulmonary tuberculosis (TB), a disease with high worldwide mortality rates. Current treatment programs are under significant threat from multi-drug and...
9.
Tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and N-benzyl-6',7'-dihydrospiro[piperidine-4,4'-thieno[3,2-c]pyran] analogues with bactericidal efficacy against Mycobacterium tuberculosis targeting MmpL3
Remuinan M, Perez-Herran E, Rullas J, Alemparte C, Martinez-Hoyos M, Dow D, et al.
PLoS One . 2013 Apr; 8(4):e60933. PMID: 23613759
Mycobacterium tuberculosis is a major human pathogen and the causative agent for the pulmonary disease, tuberculosis (TB). Current treatment programs to combat TB are under threat due to the emergence...
10.
Identification of novel imidazo[1,2-a]pyridine inhibitors targeting M. tuberculosis QcrB
Abrahams K, Cox J, Spivey V, Loman N, Pallen M, Constantinidou C, et al.
PLoS One . 2013 Jan; 7(12):e52951. PMID: 23300833
Mycobacterium tuberculosis is a major human pathogen and the causative agent for the pulmonary disease, tuberculosis (TB). Current treatment programs to combat TB are under threat due to the emergence...