Browsing by Title
Now showing items 24031-24050 of 35040
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Parsimonious Least Norm Approximation
(1997)A theoretically justifiable fast finite successive linear approximation algorithm is proposed for obtaining a parsimonious solution to a corrupted linear system Ax=b+p, where the corruption p is due to noise or error in ... -
Parsimonious Side Propagation
(1997)A fast parsimonious linear-programming-based algorithm for training neural networks is proposed that suppresses redundant features while using a minimal number of hidden units. This is achieved by propagating sideways to ... -
Part 1. Design and Synthesis of Cysteine/Cystine Prodrugs and Bioisosteres Including Symmetrical and Unsymmetrical Disulfides Designed to Increase Cystine Levels in the CNS in Order to Drive the Cystine/Glutamate Antiporter: A Novel Treatment for Schizophrenia and Drug Addiction. Part 2. Design and Synthesis of Subtype Selective Ester Bioisosteres of BZR Ligands for Gabaa/Benzodiazepine Receptors to Enhance Metabolic Stability
(2012-12-01)Part 1. Schizophrenia is a debilitating disorder that affects almost 1% of the world's population; pharmacotherapy expenditures for this disorder exceed $10 billion dollars even though existing medications exhibit a poor ... -
Part 1: Design, Synthesis, and Evaluation of Novel Gram-positive Antibiotics Part 2: Synthesis of Dihydrobenzofurans Via a New Transition Metal Catalyzed Reaction Part 3: Design, Synthesis, and Evaluation of Bz/gabaa Α6 Positive Allosteric Modulators
(2016-12-01)Part 1. Lead compound SK-03-92 represents a new scaffold for antibiotic drug discovery. Development of a new process for the synthesis of analogs has led to the development of a number of new ligands with even more potent ... -
PART 1: SYNTHESIS OF BENZODIAZEPINES AS GABAAR POSITIVE MODULATORS TO TREAT INFLAMMATORY BOWEL DISEASE. PART 2: UNSYMMETRICAL FERROCENE LIGANDS IN PALLADIUM CATALYZED SYNTHESIS USING ARYL HALIDES
(2023-12-01)PART 1: The GABAA receptor is a pentameric, ligand-gated ion channel which plays a major role in inhibition of the central nervous system. Recent reports have identified GABAAR subunits expression on non-CNS cells such as ... -
Part I Enantiospecific Total Synthesis of Unnatural Enantiomers of C-19 Methylated Sarpagine/Macroline/Ajmaline-Type Biologically Active Indole Alkaloids via the Pictet-Spengler Reaction/Dieckmann Cyclization Process. Part II Design, Synthesis, and Characterization of Novel Gamma-Aminobutyric Acid Type A (GABAA) Receptor Ligands for the Treatment of Neurological Disorders Including Epilepsy, Depr
(2023-05-01)Abstract-Part I Nature has been an extensive and sustainable pool of biologically active compounds. Many molecules from nature are secondary metabolites, which are, presumably, used in the defense mechanisms of plants or ... -
Part I, Unified Pharmacophore Protein Models of the Benzodiazepine Receptor Subtypes ; Part II, Subtype
(2011-12-01)Part I. New models of unified pharmacophore/receptors have been constructed guided by the synthesis of subtype selective compounds in light of recent developments both in ligand synthesis and structural studies of the ... -
Part I. The Development of Non-secosteroidal Vitamin D Receptor Modulators Part II. The Development of a Universal GTP-ase Assay
(2015-12-01)The vitamin D receptor is a nuclear hormone receptor that regulates cell proliferation, cell differentiation, calcium homeostasis and immunomodulation. The receptor is activated by the vitamin D metabolite, 1,25-dihydroxyvitamin ... -
Part I. The First Enantiospecific, Stereospecific Total Synthesis of the Indole Alkaloid Ervincidine. Part II. The Synthesis of Alpha 5 Subtype Selective Ligands for Gaba(a) /Benzodiazepine Receptors
(2012-12-01)Part I. The first enantiospecific, stereospecific total synthesis of ervincidine 89 has been accomplished from commercially available D-(+)-tryptophan 37 which has served both as the chiral auxiliary and the starting ... -
PART I: IMPROVEMENTS TO THE SYNTHESIS OF CALCITROIC ACID PART II: SYNTHESIS OF NEW IMIDAZODIAZEPINES TO TARGET NON-CENTRAL NERVOUS SYSTEM GABA(A) RECEPTORS PART III: IMPROVED 2-PYRIDYL REDUCTIVE HOMOCOUPLING REACTION USING BIORENEWABLE SOLVENT CYRENETM (DIHYDROLEVOGLUCOSENONE)
(2023-12-01)Abstract Part I: Calcitroic acid (CTA) was first isolated and characterized over four decades ago.6 At that time, radiolabeled calcitriol (1,25-dihydroxyvitamin D3) was utilized to facilitate the detection of radioactive ... -
Part I: A Concise Asymmetric Synthesis of Microtubule Inhibitor Tryprostatin B Part II: Synthesis and Biological Assessment of Histone Deacetylase (HDAC) Inhibitors Part III: Acid Catalyzed Reactions of Aromatic Ketones with Ethyl Diazoacetate
(2019-12-01)PART I: A CONCISE ASYMMETRIC SYNTHESIS OF MICROTUBULE INHIBITOR TRYPROSTATIN B Tryprostatin (TPS) A and B, microtubule inhibitor, are the members of a family of prenylated Trp-Pro diketopiperzine alkaloids. These two natural ... -
Part I: A Concise Synthesis of Microtubule Inhibitor Tryprostatin A and B and Its Analogs Part II: Brønsted Acid Catalyzed Reactions of Aromatic Ketones with Ethyl Diazoacetate and Its Synthetic Scope
(2021-12-01)PART I: A CONCISE SYNTHESIS OF MICROTUBULE INHIBITOR TRYPROSTATIN A AND B AND ITS ANALOGSMicrotubules are promising targets for treating cancer by stopping the cell division in mitosis(M). Tryprostatins A and B (TPS A and ... -
Part I: An Investigation of Calcitroic Acid and Its Phase II Conjugates. Part II: Toward the Development of a Novel Orally-available Asthma Treatment Targeting Gabaa Receptors in the Lungs
(2019-05-01)PART I Calcitroic acid (CTA) was isolated and characterized more than four decades ago.5 Radiolabeled calcitriol (1,25-dihydroxyvitamin D3) was used at that time to enable the identification of radioactive CTA formed in ... -
Part I: an Investigation of Calcitroic Acid and Its Phase II Conjugates. Part II: Toward the Development of a Novel Orally-available Asthma Treatment Targeting Gabaa Receptors in the Lungs
(2019-05-01)PART I Calcitroic acid (CTA) was isolated and characterized more than four decades ago.5 Radiolabeled calcitriol (1,25-dihydroxyvitamin D3) was used at that time to enable the identification of radioactive CTA formed in ... -
Part I: Design and Synthesis of Novel Drugs to Treat Asthma By Targeting GABAA Receptors in the Lung Part II: Design and Synthesis of Novel Α2/α3 Subtype Selective GABAAR Ligands for CNS Disorders
(2019-05-01)Part I. Asthma is a major healthcare challenge affecting an estimated 300 million people globally. Over $56 billion in asthma-related healthcare expenses occur in the United States annually. Moreover, asthma accounts for ... -
Part I: Development of a Novel, Small-Molecule Histone Deacetylase Inhibitor That Enhances Spatial Memory Formation in Mice Part II: Synthesis and SAR Studies of Novel HDAC Inhibitors on Prostate Cancer Cell Line: Mechanistic Insights Towards Anticancer Activity
(2022-05-01)PART I: DEVELOPMENT OF A NOVEL, SMALL-MOLECULE HISTONE DEACETYLASE INHIBITOR THAT ENHANCES SPATIAL MEMORY FORMATION IN MICE Histone acetylation is a prominent epigenetic modification linked to the memory loss symptoms ... -
Part I: Development of Small-Molecule-Based Probes for the Vitamin D Receptor; Part II: Development of a Scalable Manufacturing Process for Orcein Dye
(2021-05-01)PART I:The vitamin D receptor (VDR) is a ligand-dependent transcription factor and member of the nuclear hormone receptor superfamily. VDR is expressed in the epithelia of endocrine organs, digestive system, bronchi, ... -
Part I: Studies Towards Asymmetric α-halogenation and Mechanistic Studies of the Acrylate System with Organocatalyst and Part Ii: Synthesis of α-aryl Quaternary Carbon Centers
(2014-05-01)Organocatalytic transformations and asymmetric α-halogenation have become an important and dynamic research topic in organic chemistry in recent years. Despite the growing research in asymmetric halogenation of carbonyl ... -
Part I: Synthesis and Biological Evaluations of Potent Class L Selective Histone Deacetylase Inhibitors Part II: Aqueous Complexes for Efficient Sizebased Separation of Americium from Curium Part III: Designing Strong Chiral Bronsted Acids and Their Application for Oxaxinanones Derivatization and the Aza-henry Reaction
(2014-12-01)PART I: SYNTHESIS AND BIOLOGICAL EVALUATIONS OF POTENT CLASS l SELECTIVE HISTONE DEACETYLASE INHIBITORS Histone deacetylase inhibitors (HDACi) have found a wide variety of medicinal uses and are most noted for their specific ... -
Part I: Synthesis of Quinolones for Inhibition of the Β-barrel Assembly Machine in Gram Negative Bacteria; Part II: Synthesis of Azo Dye Sensors for Detection of Metal Ions in Aqueous Environments
(2022-05-01)Part I: Antibiotic resistance in Gram-negative bacteria is a growing cause of concern worldwide. Thousands of people die from antibiotic resistant bacteria every year. The β-Barrel Assembly Machine (BAM) in Gram-negative ...