Search Results - "Ujjini, Manjunatha"
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Use-case scenarios for an anti-Cryptosporidium therapeutic
Published in PLoS neglected tropical diseases (01-03-2021)“…Cryptosporidium is a widely distributed enteric parasite that has an increasingly appreciated pathogenic role, particularly in pediatric diarrhea. While…”
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Perspective: Challenges and opportunities in TB drug discovery from phenotypic screening
Published in Bioorganic & medicinal chemistry (15-08-2015)“…[Display omitted] Tuberculosis poses a major global health problem and multi-drug resistant strains are increasingly prevalent. Hence there is an urgent need…”
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Comprehensive physicochemical, pharmacokinetic and activity profiling of anti-TB agents
Published in Journal of antimicrobial chemotherapy (01-03-2015)“…The discovery and development of TB drugs has met limited success, with two new drugs approved over the last 40 years. Part of the difficulty resides in the…”
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4
A Cryptosporidium PI(4)K inhibitor is a drug candidate for cryptosporidiosis
Published in Nature (London) (15-06-2017)“…Diarrhoeal disease is responsible for 8.6% of global child mortality. Recent epidemiological studies found the protozoan parasite Cryptosporidium to be a…”
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Drug discovery for parasitic diseases: powered by technology, enabled by pharmacology, informed by clinical science
Published in Trends in parasitology (01-04-2023)“…Patients suffering from parasitic diseases face considerable unmet therapeutic needs.Recent scientific advances in drug discovery technology, and in…”
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6
Potent Allosteric Dengue Virus NS5 Polymerase Inhibitors: Mechanism of Action and Resistance Profiling
Published in PLoS pathogens (01-08-2016)“…Flaviviruses comprise major emerging pathogens such as dengue virus (DENV) or Zika virus (ZIKV). The flavivirus RNA genome is replicated by the…”
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Vitamin B6 biosynthesis is essential for survival and virulence of Mycobacterium tuberculosis
Published in Molecular microbiology (01-11-2010)“…With 500 000 cases of multidrug‐resistant tuberculosis there is an urgent need for attractive targets to enable the discovery of novel antimycobacterials. The…”
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Design, Synthesis, and Biological Evaluation of Indole-2-carboxamides: A Promising Class of Antituberculosis Agents
Published in Journal of medicinal chemistry (14-11-2013)“…Indole-2-carboxamides have been identified as a promising class of antituberculosis agents from phenotypic screening against mycobacteria. One of the hits,…”
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9
PA-824 Kills Nonreplicating Mycobacterium tuberculosis by Intracellular NO Release
Published in Science (American Association for the Advancement of Science) (28-11-2008)“…Bicyclic nitroimidazoles, including PA-824, are exciting candidates for the treatment of tuberculosis. These prodrugs require intracellular activation for…”
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10
Discovery of Potent Non-Nucleoside Inhibitors of Dengue Viral RNA-Dependent RNA Polymerase from a Fragment Hit Using Structure-Based Drug Design
Published in Journal of medicinal chemistry (28-04-2016)“…The discovery and optimization of non-nucleoside dengue viral RNA-dependent-RNA polymerase (RdRp) inhibitors are described. An X-ray-based fragment screen of…”
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11
Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections
Published in Science (American Association for the Advancement of Science) (30-06-2023)“…Millions who live in Latin America and sub-Saharan Africa are at risk of trypanosomatid infections, which cause Chagas disease and human African…”
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12
Direct inhibitors of InhA are active against Mycobacterium tuberculosis
Published in Science translational medicine (07-01-2015)“…New chemotherapeutic agents are urgently required to combat the global spread of multidrug-resistant tuberculosis (MDR-TB). The mycobacterial enoyl reductase…”
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13
Pyrrolo[3,4‑c]pyridine-1,3(2H)‑diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration
Published in Journal of medicinal chemistry (10-12-2015)“…High-throughput screening of a library of small polar molecules against Mycobacterium tuberculosis led to the identification of a phthalimide-containing ester…”
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14
Tuberculous Granulomas Are Hypoxic in Guinea Pigs, Rabbits, and Nonhuman Primates
Published in Infection and Immunity (01-06-2008)“…Understanding the physical characteristics of the local microenvironment in which Mycobacterium tuberculosis resides is an important goal that may allow the…”
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Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging
Published in Journal of medicinal chemistry (08-07-2021)“…Screening of a library of small polar molecules against Mycobacterium tuberculosis (Mtb) led to the identification of a potent benzoheterocyclic oxime…”
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16
Pharmacokinetics-pharmacodynamics analysis of bicyclic 4-nitroimidazole analogs in a murine model of tuberculosis
Published in PloS one (20-08-2014)“…PA-824 is a bicyclic 4-nitroimidazole, currently in phase II clinical trials for the treatment of tuberculosis. Dose fractionation…”
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Structure of Ddn, the Deazaflavin-Dependent Nitroreductase from Mycobacterium tuberculosis Involved in Bioreductive Activation of PA-824
Published in Structure (London) (11-01-2012)“…Tuberculosis continues to be a global health threat, making bicyclic nitroimidazoles an important new class of therapeutics. A deazaflavin-dependent…”
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18
A novel F420‐dependent anti‐oxidant mechanism protects Mycobacterium tuberculosis against oxidative stress and bactericidal agents
Published in Molecular microbiology (01-02-2013)“…Summary Mycobacterium tuberculosis (Mtb) is an aerobic bacterium that persists intracellularly in host macrophages and has evolved diverse mechanisms to combat…”
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Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis
Published in Science translational medicine (04-12-2013)“…New chemotherapeutic compounds against multidrug-resistant Mycobacterium tuberculosis (Mtb) are urgently needed to combat drug resistance in tuberculosis (TB)…”
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Identification of a Nitroimidazo-Oxazine-Specific Protein Involved in PA-824 Resistance in Mycobacterium tuberculosis
Published in Proceedings of the National Academy of Sciences - PNAS (10-01-2006)“…PA-824 is a promising new compound for the treatment of tuberculosis that is currently undergoing human trials. Like its progenitors metronidazole and…”
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