Search Results - "ZHOU, Yasheen"
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A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue
Published in Nature communications (06-03-2017)“…Benzoxaboroles are effective against bacterial, fungal and protozoan pathogens. We report potent activity of the benzoxaborole AN3661 against Plasmodium…”
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2
Linking phenotype to kinase: identification of a novel benzoxaborole hinge-binding motif for kinase inhibition and development of high-potency rho kinase inhibitors
Published in The Journal of pharmacology and experimental therapeutics (01-12-2013)“…Benzoxaboroles are a novel class of drug-like compounds that have been rich sources of novel inhibitors for various enzymes and of new drugs. While examining…”
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3
Chalcones and flavonoids as anti-tuberculosis agents
Published in Bioorganic & medicinal chemistry (01-08-2002)“…A series of flavonoids, chalcones and chalcone-like compounds were evaluated for inhibitory activity against Mycobacterium tuberculosis H37Rv. Among them,…”
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4
Discovery of an orally bioavailable isoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide
Published in Bioorganic & medicinal chemistry letters (01-12-2015)“…A novel series of isoxazoline benzoxaborole small molecules was designed and synthesized for a structure–activity relationship (SAR) investigation to assess…”
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5
Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
Published in Bioorganic & medicinal chemistry letters (01-02-2012)“…A series of new boron-containing benzoxaborole compounds was designed and synthesized for a continuing structure–activity relationship (SAR) investigation…”
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Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
Published in Bioorganic & medicinal chemistry letters (15-12-2010)“…We disclose here a series of P4-benzoxaborole-substituted macrocyclic HCV protease inhibitors. These inhibitors are potent against HCV NS3 protease, their…”
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Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease
Published in Bioorganic & medicinal chemistry letters (15-04-2012)“…A novel series of P3 oxo-modified macrocyclic hepatitis C virus NS3/4A serine protease inhibitor was designed, synthesized and biologically evaluated. The…”
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Methylenedioxy- and ethylenedioxy-fused indolocarbazoles: potent human topoisomerase I inhibitors and antitumor agents
Published in Anti-cancer agents in medicinal chemistry (01-11-2012)“…The indolo[2,3-a]carbazole alkaloids constitute an important class of natural products with interesting and diverse biological activities. A series of novel…”
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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)
Published in Journal of medicinal chemistry (12-10-2017)“…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…”
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10
Design and synthesis of highly constrained factor Xa inhibitors: amidine-Substituted bis(benzoyl)- [1,3]-diazepan-2-ones and bis(benzylidene)-bis( gem-dimethyl)cycloketones
Published in Bioorganic & medicinal chemistry (05-08-2003)“…Two conformationally constrained templates have been designed to provide selective inhibitors of the coagulation cascade serine protease, Factor Xa (FXa). The…”
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Treatment of Skin Inflammation with Benzoxaborole Phosphodiesterase Inhibitors: Selectivity, Cellular Activity, and Effect on Cytokines Associated with Skin Inflammation and Skin Architecture Changes
Published in The Journal of pharmacology and experimental therapeutics (01-09-2016)“…Psoriasis and atopic dermatitis are skin diseases affecting millions of patients. Here, we characterize benzoxaborole phosphodiesterase (PDE)-4 inhibitors, a…”
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Discovery of Novel Oral Protein Synthesis Inhibitors of Mycobacterium tuberculosis That Target Leucyl-tRNA Synthetase
Published in Antimicrobial agents and chemotherapy (01-10-2016)“…The recent development and spread of extensively drug-resistant and totally drug-resistant resistant (TDR) strains of Mycobacterium tuberculosis highlight the…”
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13
Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center
Published in FEBS letters (21-09-2012)“…► Novel boron-containing small molecule inhibitors of phosphodiesterase 4. ► Co-crystal structure shows unique binding compared to catechol inhibitors. ► Boron…”
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14
Discovery of a Novel Class of Boron-Based Antibacterials with Activity against Gram-Negative Bacteria
Published in Antimicrobial Agents and Chemotherapy (01-03-2013)“…OA Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Exploring boron applications in modern agriculture: A structure-activity relationship study of a novel series of multi-substitution benzoxaboroles for identification of potential fungicides
Published in Bioorganic & medicinal chemistry letters (01-07-2021)“…[Display omitted] Several boron-containing small molecules have been approved by the US FDA to treat human diseases. We explored potential applications of…”
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Inhibiting Protein Prenylation with Benzoxaboroles to Target Fungal Plant Pathogens
Published in ACS chemical biology (17-07-2020)“…Fungal pathogens pose an increasing threat to global food security through devastating effects on staple crops and contamination of food supplies with…”
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Inhibiting C‑4 Methyl Sterol Oxidase with Novel Diazaborines to Target Fungal Plant Pathogens
Published in ACS chemical biology (17-06-2022)“…With resistance to current agricultural fungicides rising, a great need has emerged for new antifungals with unexploited targets. In response, we report a…”
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Efficacy and Improved Resistance Potential of a Cofactor-Independent InhA Inhibitor of Mycobacterium tuberculosis in the C3HeB/FeJ Mouse Model
Published in Antimicrobial agents and chemotherapy (01-04-2019)“…AN12855 is a direct, cofactor-independent inhibitor of InhA in In the C3HeB/FeJ mouse model with caseous necrotic lung lesions, AN12855 proved efficacious with…”
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The 7-phenyl benzoxaborole series is active against Mycobacterium tuberculosis
Published in Tuberculosis (Edinburgh, Scotland) (01-01-2018)“…We identified a series of novel 7-phenyl benzoxaborole compounds with activity against Mycobacterium tuberculosis. Compounds had a range of activity with…”
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AN2728, a new boron-based topical anti-inflammatory agent, inhibits phosphodiesterase 4 (IRC4P.611)
Published in The Journal of immunology (1950) (01-05-2015)“…Abstract The novel boron-containing compound, AN2728, is being investigated in phase 3 trials for atopic dermatitis treatment. It exerts its anti-inflammatory…”
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