Search Results - "Franzblau, Scott"

New tuberculosis drug targets, their inhibitors, and potential therapeutic impact by Shetye, Gauri S., Franzblau, Scott G., Cho, Sanghyun

“…The current tuberculosis (TB) predicament poses numerous challenges and therefore every incremental scientific work and all positive socio-political…”
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Structure−Activity Relationships for a Series of Quinoline-Based Compounds Active against Replicating and Nonreplicating Mycobacterium tuberculosis by Lilienkampf, Annamaria, Mao, Jialin, Wan, Baojie, Wang, Yuehong, Franzblau, Scott G, Kozikowski, Alan P

“…Tuberculosis (TB) remains as a global pandemic that is aggravated by a lack of health care, the spread of HIV, and the emergence of multidrug-resistant TB…”
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Discovery of natural-product-derived sequanamycins as potent oral anti-tuberculosis agents by Zhang, Jidong, Lair, Christine, Roubert, Christine, Amaning, Kwame, Barrio, María Belén, Benedetti, Yannick, Cui, Zhicheng, Xing, Zhongliang, Li, Xiaojun, Franzblau, Scott G., Baurin, Nicolas, Bordon-Pallier, Florence, Cantalloube, Cathy, Sans, Stephanie, Silve, Sandra, Blanc, Isabelle, Fraisse, Laurent, Rak, Alexey, Jenner, Lasse B., Yusupova, Gulnara, Yusupov, Marat, Zhang, Junjie, Kaneko, Takushi, Yang, T.J., Fotouhi, Nader, Nuermberger, Eric, Tyagi, Sandeep, Betoudji, Fabrice, Upton, Anna, Sacchettini, James C., Lagrange, Sophie

“…The emergence of drug-resistant tuberculosis has created an urgent need for new anti-tubercular agents. Here, we report the discovery of a series of macrolides…”
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Improved BM212 MmpL3 inhibitor analogue shows efficacy in acute murine model of tuberculosis infection by Poce, Giovanna, Bates, Robert H, Alfonso, Salvatore, Cocozza, Martina, Porretta, Giulio Cesare, Ballell, Lluís, Rullas, Joaquin, Ortega, Fátima, De Logu, Alessandro, Agus, Emanuela, La Rosa, Valentina, Pasca, Maria Rosalia, De Rossi, Edda, Wae, Baojie, Franzblau, Scott G, Manetti, Fabrizio, Botta, Maurizio, Biava, Mariangela

“…1,5-Diphenyl pyrroles were previously identified as a class of compounds endowed with high in vitro efficacy against M. tuberculosis. To improve the physical…”
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Novel insights into the mechanism of inhibition of MmpL3, a target of multiple pharmacophores in Mycobacterium tuberculosis by Li, Wei, Upadhyay, Ashutosh, Fontes, Fabio L, North, E Jeffrey, Wang, Yuehong, Crans, Debbie C, Grzegorzewicz, Anna E, Jones, Victoria, Franzblau, Scott G, Lee, Richard E, Crick, Dean C, Jackson, Mary

“…MmpL3, a resistance-nodulation-division (RND) superfamily transporter, has been implicated in the formation of the outer membrane of Mycobacterium…”
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QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity by Gomes, Marcelo N., Braga, Rodolpho C., Grzelak, Edyta M., Neves, Bruno J., Muratov, Eugene, Ma, Rui, Klein, Larry L., Cho, Sanghyun, Oliveira, Guilherme R., Franzblau, Scott G., Andrade, Carolina Horta

“…New anti-tuberculosis (anti-TB) drugs are urgently needed to battle drug-resistant Mycobacterium tuberculosis strains and to shorten the current 6–12-month…”
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In Vitro Profiling of Antitubercular Compounds by Rapid, Efficient, and Nondestructive Assays Using Autoluminescent Mycobacterium tuberculosis by Shetye, Gauri S, Choi, Kyung Bae, Kim, Chang-Yub, Franzblau, Scott G, Cho, Sanghyun

“…Anti-infective drug discovery is greatly facilitated by the availability of assays that are more proficient at predicting the preclinical success of screening…”
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Design, synthesis and investigation on the structure–activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents by Pieroni, Marco, Wan, Baojie, Cho, Sanghyun, Franzblau, Scott G., Costantino, Gabriele

“…Tuberculosis (TB) is one of the deadliest infectious diseases of all times, and its recent resurgence is a supreme matter of concern. Co-infection with HIV…”
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Strategies in anti-Mycobacterium tuberculosis drug discovery based on phenotypic screening by Grzelak, Edyta M., Choules, Mary P., Gao, Wei, Cai, Geping, Wan, Baojie, Wang, Yuehong, McAlpine, James B., Cheng, Jinhua, Jin, Yingyu, Lee, Hanki, Suh, Joo-Won, Pauli, Guido F., Franzblau, Scott G., Jaki, Birgit U., Cho, Sanghyun

“…The rise of multi- and extensively drug-resistant Mycobacterium tuberculosis ( M. tb ) strains and co-infection with human immunodeficiency virus has escalated…”
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Design, synthesis and biological evaluation of novel 1,2,3-triazole analogues of Imidazo-[1,2-a]-pyridine-3-carboxamide against Mycobacterium tuberculosis by Nandikolla, Adinarayana, Srinivasarao, Singireddi, Khetmalis, Yogesh Mahadu, Kumar, Banoth Karan, Murugesan, Sankaranarayanan, Shetye, Gauri, Ma, Rui, Franzblau, Scott G., Sekhar, Kondapalli Venkata Gowri Chandra

“…Twenty-eight novel 1,2,3-triazole analogues of imidazo-[1,2-a]-pyridine-3-carboxamide were designed and synthesized based on hybridization approach. The…”
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3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel by Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Blaser, Adrian, Conole, Daniel, Franzblau, Scott G., Lotlikar, Manisha U., Cooper, Christopher B., Upton, Anna M., Denny, William A., Palmer, Brian D.

“…[Display omitted] Bedaquiline is a new drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but…”
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Targeting mycobacterium protein tyrosine phosphatase B for antituberculosis agents by Zhou, Bo, He, Yantao, Zhang, Xian, Xu, Jie, Luo, Yong, Wang, Yuehong, Franzblau, Scott G, Yang, Zhenyun, Chan, Rebecca J, Liu, Yan, Zheng, Jianyu, Zhang, Zhong-Yin

“…Protein tyrosine phosphatases are often exploited and subverted by pathogenic bacteria to cause human diseases. The tyrosine phosphatase mPTPB from…”
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The cyclic peptide ecumicin targeting ClpC1 is active against Mycobacterium tuberculosis in vivo by Gao, Wei, Kim, Jin-Yong, Anderson, Jeffrey R, Akopian, Tatos, Hong, Seungpyo, Jin, Ying-Yu, Kandror, Olga, Kim, Jong-Woo, Lee, In-Ae, Lee, Sun-Young, McAlpine, James B, Mulugeta, Surafel, Sunoqrot, Suhair, Wang, Yuehong, Yang, Seung-Hwan, Yoon, Tae-Mi, Goldberg, Alfred L, Pauli, Guido F, Suh, Joo-Won, Franzblau, Scott G, Cho, Sanghyun

“…Drug-resistant tuberculosis (TB) has lent urgency to finding new drug leads with novel modes of action. A high-throughput screening campaign of >65,000…”
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Discovery of a capuramycin analog that kills nonreplicating Mycobacterium tuberculosis and its synergistic effects with translocase I inhibitors by Siricilla, Shajila, Mitachi, Katsuhiko, Wan, Bajoie, Franzblau, Scott G, Kurosu, Michio

“…Capuramycin ( 1 ) and its analogs are strong translocase I (MurX/MraY) inhibitors. In our structure–activity relationship studies of capuramycin analogs…”
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Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent by Huang, Zhigang, Luo, Wei, Xu, Deming, Guo, Fengxun, Yang, Meng, Zhu, Yusong, Shen, Liang, Chen, Shuhui, Tang, Dongdong, Li, Lei, Li, Yongguo, Wang, Bin, Franzblau, Scott G, Ding, Charles Z.

“…[Display omitted] Multidrug resistant tuberculosis (MDR-TB) remains a major human health challenge. Bedaquiline was approved in 2012 by the US FDA, and listed…”
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Low-Oxygen-Recovery Assay for High-Throughput Screening of Compounds against Nonreplicating Mycobacterium tuberculosis by Cho, Sang Hyun, Warit, Saradee, Wan, Baojie, Hwang, Chang Hwa, Pauli, Guido F, Franzblau, Scott G

“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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1,3-Oxazine-2-one derived dual-targeted molecules against replicating and non-replicating forms of Mycobacterium tuberculosis by Velappan, Anand Babu, Kesamsetty, Dhanunjaya, Datta, Dhrubajyoti, Ma, Rui, Hari, Natarajan, Franzblau, Scott G., Debnath, Joy

“…The high mortality rate and increasing prevalence of resistant Mtb are the major concerns for the Tuberculosis (TB) treatment in this century. To curtail the…”
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Enhancing hit identification in Mycobacterium tuberculosis drug discovery using validated dual-event Bayesian models by Ekins, Sean, Reynolds, Robert C, Franzblau, Scott G, Wan, Baojie, Freundlich, Joel S, Bunin, Barry A

“…High-throughput screening (HTS) in whole cells is widely pursued to find compounds active against Mycobacterium tuberculosis (Mtb) for further development…”
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Comprehensive analysis of methods used for the evaluation of compounds against Mycobacterium tuberculosis by Franzblau, Scott G, DeGroote, Mary Ann, Cho, Sang Hyun, Andries, Koen, Nuermberger, Eric, Orme, Ian M, Mdluli, Khisimuzi, Angulo-Barturen, Iñigo, Dick, Thomas, Dartois, Veronique, Lenaerts, Anne J

“…Summary In drug development, there are typically a series of preclinical studies that must be completed with new compounds or regimens before use in humans. A…”
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Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles by Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Conole, Daniel, Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha U., Denny, William A., Palmer, Brian D.

“…[Display omitted] Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing…”
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