Search Results - "Nigade, Prashant B"
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Dual PI3Kδγ inhibition demonstrates potent anticancer effects in diffuse large B-cell lymphoma models: Discovery and preclinical characterization of LL-00084282
Published in Biochemical and biophysical research communications (31-12-2022)“…Phosphoinositide 3-kinase (PI3K) pathway mediates key signaling events downstream to B-cell receptor (BCR) for survival of mature B-cells, and overexpression…”
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Prediction of volume of distribution in preclinical species and humans: application of simplified physiologically based algorithms
Published in Xenobiotica (04-05-2019)“…The present study was aimed at developing simplified physiologically based semi-mechanistic algorithms to predict V and interspecies scaling factors to predict…”
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Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure–Activity Relationship and Preclinical Characterization
Published in Journal of medicinal chemistry (13-02-2020)“…The discovery of a series of thiophenephenylsulfonamides as positive allosteric modulators (PAM) of α7 nicotinic acetylcholine receptor (α7 nAChR) is…”
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LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization
Published in European journal of pharmacology (15-01-2021)“…α7 nicotinic acetylcholine receptor (α7 nAChR) is an extensively validated target for several neurological and psychiatric conditions namely, dementia and…”
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Discovery of Potent, Selective, and State-Dependent Na V 1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides
Published in Journal of medicinal chemistry (11-06-2020)“…Voltage-gated sodium channel Na 1.7 is a genetically validated target for pain. Identification of Na 1.7 inhibitors with all of the desired properties to…”
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Prediction of Tissue-to-Plasma Ratios of Basic Compounds in Mice
Published in European journal of drug metabolism and pharmacokinetics (01-10-2017)“…Background Majority of reported studies so far developed correlation regression equations using the rat muscle-to-plasma drug concentration ratio (Kp-muscle)…”
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Prediction of Tumor-to-Plasma Ratios of Basic Compounds in Subcutaneous Xenograft Mouse Models
Published in European journal of drug metabolism and pharmacokinetics (01-06-2018)“…Background Predicting target site drug concentrations is of key importance for rank ordering compounds before proceeding to chronic pharmacodynamic models. We…”
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Cardioprotective effect of Azadirachta indica A. Juss. on isoprenaline induced myocardial infarction in rats
Published in International journal of cardiology (07-05-2008)“…Abstract The present study was designed to evaluate the cardioprotective potential of aqueous leaf extract of Azadirachta indica A. Juss. (AI) on the basis of…”
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Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization
Published in Bioorganic & medicinal chemistry (15-12-2020)“…[Display omitted] The exploitation of GLU988 and LYS903 residues in PARP1 as targets to design isoquinolinone (I & II) and naphthyridinone (III) analogues is…”
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