Search Results - "Rajeswaran, Walajapet"
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Optimization of Eliglustat-Based Glucosylceramide Synthase Inhibitors as Substrate Reduction Therapy for Gaucher Disease Type 3
Published in ACS chemical neuroscience (21-10-2020)“…There remain no approved therapies for rare but devastating neuronopathic glyocosphingolipid storage diseases, such as Sandhoff, Tay-Sachs, and Gaucher disease…”
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Novel inhibitors of bacterial virulence: Development of 5,6-dihydrobenzo[h]quinazolin-4(3H)-ones for the inhibition of group A streptococcal streptokinase expression
Published in Bioorganic & medicinal chemistry (01-04-2013)“…Resistance to antibiotics is an increasingly dire threat to human health that warrants the development of new modes of treating infection. We recently…”
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Massive Bioaccumulation and Self‐Assembly of Phenazine Compounds in Live Cells
Published in Advanced science (01-08-2015)“…Clofazimine is an orally administered drug that massively bioaccumulates in macrophages, forming membrane‐bound intracellular structures possessing nanoscale…”
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The Physicochemical Basis of Clofazimine-Induced Skin Pigmentation
Published in Journal of investigative dermatology (01-03-2018)“…Clofazimine is a weakly basic, Food and Drug Administration-approved antibiotic recommended by the World Health Organization to treat leprosy and…”
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Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma
Published in Bioorganic & medicinal chemistry letters (15-04-2017)“…[Display omitted] We recently reported the development of a novel inhibitor of Rho-mediated gene transcription (1, CCG-203971) that is efficacious in multiple…”
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CARP-1 functional mimetics are novel inhibitors of drug-resistant triple negative breast cancers
Published in Oncotarget (08-11-2016)“…Doxorubicin and Cisplatin are the frontline therapeutics for treatment of the triple negative breast cancers (TNBCs). Emergence of drug-resistance often…”
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Optimization of Benzoxazinorifamycins to Improve Mycobacterium tuberculosis RNA Polymerase Inhibition and Treatment of Tuberculosis
Published in ACS infectious diseases (12-08-2022)“…Rifampin (RMP), a very potent inhibitor of the Mycobacterium tuberculosis (MTB) RNA polymerase (RNAP), remains a keystone in the treatment of tuberculosis…”
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Optimization of Benzoxazinorifamycins to Minimize hPXR Activation for the Treatment of Tuberculosis and HIV Coinfection
Published in ACS infectious diseases (12-08-2022)“…Tuberculosis (TB) is one of the most significant world health problems, responsible for 1.5 M deaths in 2020, and yet, current treatments rely largely on 40…”
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Pharmacokinetic Optimization of CCG-203971: Novel Inhibitors of the Rho/MRTF/SRF Transcriptional Pathway as Potential Antifibrotic Therapeutics for Systemic Scleroderma
Published in Bioorganic & medicinal chemistry letters (10-03-2017)“…We recently reported the development of a novel inhibitor of Rho-mediated gene transcription ( 1 , CCG-203971) that is efficacious in multiple animal models of…”
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Studies on protection of oxindoles
Published in Tetrahedron (17-09-1998)“…Protection of amide nitrogen of oxindole and methyloxindole using Boc and Z-groups has been described. Sodium carbonate was found to be an effective base for…”
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A convenient method of protecting oxindoles
Published in Tetrahedron letters (10-11-1997)“…The nitrogens of oxindoles and indole were protected by dichloroacetyl group in refluxing DCE. The deprotection of these protected oxindoles and indole has…”
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