Search Results - "Schiehser, Guy"

Triclosan Derivatives: Towards Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis by Freundlich, Joel S., Wang, Feng, Vilchèze, Catherine, Gulten, Gulcin, Langley, Robert, Schiehser, Guy A., Jacobus, David P., Jacobs Jr, William R., Sacchettini, James C.

“…Overcoming resistance: Isoniazid (INH) is a frontline antitubercular drug that inhibits the enoyl acyl carrier protein reductase InhA. Novel inhibitors of InhA…”
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Characterization of the Preclinical Pharmacology of the New 2-Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention by Birrell, Geoffrey W, Heffernan, Gavin D, Schiehser, Guy A, Anderson, John, Ager, Arba L, Morales, Pablo, MacKenzie, Donna, van Breda, Karin, Chavchich, Marina, Jacobus, Laura R, Shanks, G Dennis, Jacobus, David P, Edstein, Michael D

“…The new 2-aminomethylphenol, JPC-3210, has potent antimalarial activity against multidrug-resistant lines, low cytotoxicity, and high efficacy against murine…”
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Lead Selection of a New Aminomethylphenol, JPC-3210, for Malaria Treatment and Prevention by Chavchich, Marina, Birrell, Geoffrey W, Ager, Arba L, MacKenzie, Donna O, Heffernan, Gavin D, Schiehser, Guy A, Jacobus, Laura R, Shanks, G Dennis, Jacobus, David P, Edstein, Michael D

“…Structure-activity relationship studies of trifluoromethyl-substituted pyridine and pyrimidine analogues of 2-aminomethylphenols (JPC-2997, JPC-3186, and…”
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JPC-2997, a new aminomethylphenol with high in vitro and in vivo antimalarial activities against blood stages of Plasmodium by Birrell, Geoffrey W, Chavchich, Marina, Ager, Arba L, Shieh, Hong-Ming, Heffernan, Gavin D, Zhao, Wenyi, Krasucki, Peter E, Saionz, Kurt W, Terpinski, Jacek, Schiehser, Guy A, Jacobus, Laura R, Shanks, G Dennis, Jacobus, David P, Edstein, Michael D

“…4-(tert-Butyl)-2-((tert-butylamino)methyl)-6-(6-(trifluoromethyl)pyridin-3-yl)-phenol (JPC-2997) is a new aminomethylphenol compound that is highly active in…”
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Novel Triazine JPC-2067-B Inhibits Toxoplasma gondii In Vitro and In Vivo by Mui, Ernest J, Schiehser, Guy A, Milhous, Wilbur K, Hsu, Honghue, Roberts, Craig W, Kirisits, Michael, Muench, Stephen, Rice, David, Dubey, J.P, Fowble, Joseph W, Rathod, Pradipsinh K, Queener, Sherry F, Liu, Susan R, Jacobus, David P, McLeod, Rima

“…Background and Methodology: Toxoplasma gondii causes substantial morbidity, mortality, and costs for healthcare in the developed and developing world. Current…”
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X-ray Structural Analysis of Plasmodium falciparum Enoyl Acyl Carrier Protein Reductase as a Pathway toward the Optimization of Triclosan Antimalarial Efficacy by Freundlich, Joel S., Wang, Feng, Tsai, Han-Chun, Kuo, Mack, Shieh, Hong-Ming, Anderson, John W., Nkrumah, Louis J., Valderramos, Juan-Carlos, Yu, Min, Kumar, T.R. Santha, Valderramos, Stephanie G., Jacobs, William R., Schiehser, Guy A., Jacobus, David P., Fidock, David A., Sacchettini, James C.

“…The x-ray crystal structures of five triclosan analogs, in addition to that of the isoniazid-NAD adduct, are described in relation to their integral role in…”
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Novel diaryl ureas with efficacy in a mouse model of malaria by Anderson, John W., Sarantakis, Dimitri, Terpinski, Jacek, Santha Kumar, T.R., Tsai, Han-Chun, Kuo, Mack, Ager, Arba L., Jacobs, William R., Schiehser, Guy A., Ekins, Sean, Sacchettini, James C., Jacobus, David P., Fidock, David A., Freundlich, Joel S.

“…Exploration of triclosan analogs has led to novel diaryl ureas with significant potency against in vitro cultures of drug-resistant and drug-sensitive strains…”
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Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4′-Substituted triclosan derivatives by Freundlich, Joel S., Anderson, John W., Sarantakis, Dimitri, Shieh, Hong-Ming, Yu, Min, Valderramos, Juan-Carlos, Lucumi, Edinson, Kuo, Mack, Jacobs, William R., Fidock, David A., Schiehser, Guy A., Jacobus, David P., Sacchettini, James C.

“…Nanomolar inhibitors of P. falciparum enoyl acyl carrier protein reductase are presented that demonstrate potent anti-parasitic efficacy. A structure-based…”
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Synthesis and biological activity of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 2: 2′-Substituted triclosan derivatives by Freundlich, Joel S., Yu, Min, Lucumi, Edinson, Kuo, Mack, Tsai, Han-Chun, Valderramos, Juan-Carlos, Karagyozov, Luchezar, Jacobs, William R., Schiehser, Guy A., Fidock, David A., Jacobus, David P., Sacchettini, James C.

“…Inhibitors of Plasmodium falciparum enoyl acyl carrier protein reductase are presented that demonstrate nanomolar anti-parasitic efficacy. 2′-Substituted…”
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Role of Specific Cytochrome P450 Isoforms in the Conversion of Phenoxypropoxybiguanide Analogs in Human Liver Microsomes to Potent Antimalarial Dihydrotriazines by DIAZ, Damaris S, KOZAR, Michael. P, SMITH, Kirsten S, ASHER, Constance O, SOUSA, Jason C, SCHIEHSER, Guy A, JACOBUS, David. P, MILHOUS, Wilbur. K, SKILLMAN, Donald. R, SHEARER, Todd. W

“…Phenoxypropoxybiguanides, such as PS-15, are antimalarial prodrugs analogous to the relationship of proguanil and its active metabolite cycloguanil. Unlike…”
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Triazine Inhibits Toxoplasma gondii Tachyzoites In Vitro and In Vivo by MUI, Ernest J, JACOBUS, David, MILHOUS, Wilbur K, SCHIEHSER, Guy, HONGHUE HSU, ROBERTS, Craig W, KIRISITS, Michael J, MCLEOD, Rima

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Identification of the optimal third generation antifolate against P. falciparum and P. vivax by Hunt, Sonia Y., Detering, Carsten, Varani, Gabriele, Jacobus, David P., Schiehser, Guy A., Shieh, Hong-Ming, Nevchas, Isabelle, Terpinski, Jacek, Sibley, Carol Hopkins

“…Inhibitors of dihydrofolate reductase (DHFR) have been mainstays in the treatment of falciparum malaria. Resistance to one of these antifolates, pyrimethamine,…”
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Antimalarial pharmacodynamics and pharmacokinetics of a third-generation antifolate—JPC2056—in cynomolgus monkeys using an in vivo–in vitro model by Edstein, Michael D., Kotecka, Barbara M., Ager, Arba L., Smith, Kirsten S., DiTusa, Charles A., Diaz, Damaris S., Kyle, Dennis E., Schiehser, Guy A., Jacobus, David P., Rieckmann, Karl H., O'Neil, Michael T.

“…Objectives To assess the antimalarial pharmacodynamics and pharmacokinetics of the novel dihydrofolate reductase (DHFR) inhibitor, JPC2056 and its principal…”
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In Vitro Metabolism of Phenoxypropoxybiguanide Analogues in Human Liver Microsomes to Potent Antimalarial Dihydrotriazines by Shearer, Todd. W, Kozar, Michael. P, O'Neil, Michael T, Smith, Philip L, Schiehser, Guy A, Jacobus, David. P, Diaz, Damaris S, Yang, Young-Sun, Milhous, Wilbur. K, Skillman, Donald. R

“…Phenoxypropoxybiguanides, such as 1 (PS-15), are prodrugs analogous to the relationship of proguanil and its active metabolite cycloguanil. Unlike cycloguanil,…”
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Analysis of the Energetics of Gas-Phase Immunophilin-Ligand Complexes by Ion Spray Mass Spectrometry by Li, Yu-Tsyr, Hsieh, Yin-Liang, Henion, Jack D, Ocain, Timothy D, Schiehser, Guy A, Ganem, Bruce

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The fatty acid biosynthesis enzyme FabI plays a key role in the development of liver-stage malarial parasites by Yu, Min, Kumar, T R Santha, Nkrumah, Louis J, Coppi, Alida, Retzlaff, Silke, Li, Celeste D, Kelly, Brendan J, Moura, Pedro A, Lakshmanan, Viswanathan, Freundlich, Joel S, Valderramos, Juan-Carlos, Vilcheze, Catherine, Siedner, Mark, Tsai, Jennifer H-C, Falkard, Brie, Sidhu, Amar Bir Singh, Purcell, Lisa A, Gratraud, Paul, Kremer, Laurent, Waters, Andrew P, Schiehser, Guy, Jacobus, David P, Janse, Chris J, Ager, Arba, Jacobs, Jr, William R, Sacchettini, James C, Heussler, Volker, Sinnis, Photini, Fidock, David A

“…The fatty acid synthesis type II pathway has received considerable interest as a candidate therapeutic target in Plasmodium falciparum asexual blood-stage…”
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Total synthesis of (.+-.)-9-pupukeanone by Schiehser, Guy A, White, James D

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Syntheses and gastric acid antisecretory properties of the H2-receptor antagonist N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]thieno[3,4-d]isothiazol-3-amine 1,1-dioxide and related derivatives by Santilli, Arthur A, Scotese, Anthony C, Morris, Robert L, Schiehser, Guy A, Teller, Daniel M, Nielsen, Susan T, Strike, Donald P

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Triclosan Derivatives: Towards Potent Inhibitors of Drug-Sensitive and Drug-Resistant Mycobacterium tuberculosis by Freundlich, Joel S., Wang, Feng, Vilchèze, Catherine, Gulten, Gulcin, Langley, Robert, Schiehser, Guy A., Jacobus, David P., Jacobs, William R., Sacchettini, James C.

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Erratum to “Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4′-Substituted triclosan derivatives” [Bioorg. Med. Chem. Lett. 15 (2005) 5247–5252] by Freundlich, Joel S., Anderson, John W., Sarantakis, Dimitri, Shieh, Hong-Ming, Yu, Min, Valderramos, Juan-Carlos, Lucumi, Edinson, Kuo, Mack, Jacobs, William R., Fidock, David A., Schiehser, Guy A., Jacobus, David P., Sacchettini, James C.

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