Alpha 2.0
Login Register
» Authors » Eric E Easom

Eric E Easom

Explore the profile of Eric E Easom including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 12
Citations 229
Followers 0
Related Specialties
Biochemistry
Pharmacology
Microbiology
Top 10 Co-Authors
Jacob J Plattner
Yvonne R Freund
Yong-Kang Zhang
Yasheen Zhou
Tsutomu Akama
Robert T Jacobs
Francisco-Javier Gamo
Philip J Rosenthal
Min Ge
Laura M Sanz
Published In
Bioorg Med Chem Lett
J Med Chem
ACS Infect Dis
mBio
Antimicrob Agents Chemother
Affiliations
Soon will be listed here.
Recent Articles
1.
Plasmodium falciparum Resistance to a Lead Benzoxaborole Due to Blocked Compound Activation and Altered Ubiquitination or Sumoylation
Sindhe K, Wu W, Legac J, Zhang Y, Easom E, Cooper R, et al.
mBio . 2020 Jan; 11(1). PMID: 31992618
New antimalarial drugs are needed. The benzoxaborole AN13762 showed excellent activity against cultured , against fresh Ugandan isolates, and in murine malaria models. To gain mechanistic insights, we selected for...
2.
Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 1. Amide Linked Analogs
Akama T, Freund Y, Berry P, Carter D, Easom E, Jarnagin K, et al.
ACS Infect Dis . 2019 Dec; 6(2):173-179. PMID: 31876154
A series of benzimidazole-benzoxaborole hybrid molecules linked via an amide linker are described that exhibit good activity against , a filarial nematode responsible for the disease onchocerciasis, also known as...
3.
Macrofilaricidal Benzimidazole-Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 2. Ketone Linked Analogs
Carter D, Jacobs R, Freund Y, Berry P, Akama T, Easom E, et al.
ACS Infect Dis . 2019 Dec; 6(2):180-185. PMID: 31876143
The optimization of a series of benzimidazole-benzoxaborole hybrid molecules linked via a ketone that exhibit good activity against , a filarial nematode responsible for the disease onchocerciasis, also known as...
4.
Identification of a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT)
Akama T, Zhang Y, Freund Y, Berry P, Lee J, Easom E, et al.
Bioorg Med Chem Lett . 2017 Nov; 28(1):6-10. PMID: 29169674
Novel l-valinate amide benzoxaboroles and analogues were designed and synthesized for a structure-activity-relationship (SAR) investigation to optimize the growth inhibitory activity against Trypanosoma congolense (T. congolense) and Trypanosoma vivax (T....
5.
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...
6.
Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate
Zhang Y, Plattner J, Easom E, Jacobs R, Guo D, Freund Y, et al.
J Med Chem . 2017 Jun; 60(13):5889-5908. PMID: 28635296
Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered...
7.
Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase
Palencia A, Li X, Bu W, Choi W, Ding C, Easom E, et al.
Antimicrob Agents Chemother . 2016 Aug; 60(10):6271-80. PMID: 27503647
The recent development and spread of extensively drug-resistant and totally drug-resistant resistant (TDR) strains of Mycobacterium tuberculosis highlight the need for new antitubercular drugs. Protein synthesis inhibitors have played an...
8.
Optimization of isoxazoline amide benzoxaboroles for identification of a development candidate as an oral long acting animal ectoparasiticide
Zhang Y, Plattner J, Easom E, Akama T, Zhou Y, White W, et al.
Bioorg Med Chem Lett . 2016 May; 26(13):3182-3186. PMID: 27210432
Novel isoxazoline amide benzoxaboroles were designed and synthesized to optimize the ectoparasiticide activity of this chemistry series against ticks and fleas. The study identified an orally bioavailable molecule, (S)-N-((1-hydroxy-3,3-dimethyl-1,3-dihydrobenzo[c][1,2]oxaborol-6-yl)methyl)-2-methyl-4-(5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl)benzamide (23),...
9.
Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide
Zhang Y, Plattner J, Easom E, Zhou Y, Akama T, Bu W, et al.
Bioorg Med Chem Lett . 2015 Oct; 25(23):5589-93. PMID: 26508546
A novel series of isoxazoline benzoxaborole small molecules was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the ectoparasiticide activity against ticks and fleas. The study identified...
10.
Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
Zhang Y, Plattner J, Easom E, Jacobs R, Guo D, Sanders V, et al.
J Med Chem . 2015 Jun; 58(13):5344-54. PMID: 26067904
A series of 6-hetaryloxy benzoxaborole compounds was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the changes in antimalarial activity which result from 6-aryloxy structural variation, substituent...