Search Results - "Cirillo, Pier F"
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Selective CB2 receptor agonists. Part 1: The identification of novel ligands through computer-aided drug design (CADD) approaches
Published in Bioorganic & medicinal chemistry letters (01-02-2015)“…[Display omitted] Computer-aided drug design scaffold hopping strategies were utilized to identify new classes of CB2 agonists when compounds of an established…”
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Green Fischer Indole Synthesis Using a Steroidal Ketone in a Conductively Heated Sealed-Vessel Reactor for the Advanced Undergraduate Laboratory
Published in Journal of chemical education (09-02-2021)“…Highly efficient microwave-assisted organic synthesis is now commonplace in both industry and academia. Recently, a conductively heated sealed-vessel reactor…”
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Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site
Published in Nature structural biology (01-04-2002)“…The p38 MAP kinase plays a crucial role in regulating the production of proinflammatory cytokines, such as tumor necrosis factor and interleukin-1. Blocking…”
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Inhibition of Macrophage Migration Inhibitory Factor by a Chimera of Two Allosteric Binders
Published in ACS medicinal chemistry letters (08-10-2020)“…Human Macrophage Migration Inhibitory Factor (MIF) is a trimeric cytokine implicated in a number of inflammatory and autoimmune diseases and cancer. We…”
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Structure−Activity Relationships of the p38α MAP Kinase Inhibitor 1-(5-tert-Butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796)
Published in Journal of medicinal chemistry (23-10-2003)“…We report on the structure−activity relationships (SAR) of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea (BIRB…”
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The non-diaryl heterocycle classes of p38 MAP kinase inhibitors
Published in Current topics in medicinal chemistry (01-09-2002)“…The p38 mitogen activated protein (MAP) kinase is an integral enzyme involved in the production of a wide variety of pro-inflammatory cytokines from various…”
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1,4-Diazepane compounds as potent and selective CB2 agonists: Optimization of metabolic stability
Published in Bioorganic & medicinal chemistry letters (01-04-2011)“…A high-throughput screening campaign has identified 1,4-diazepane compounds which are potent Cannabinoid receptor 2 agonists with excellent selectivity against…”
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Studies Directed toward the Synthesis of (+)-Sesbanimide A: Construction of the AB-Ring System (A Formal Total Synthesis)
Published in Journal of organic chemistry (01-06-1994)Get full text
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New modifications to the area of pyrazole-naphthyl urea based p38 MAP kinase inhibitors that bind to the adenine/ATP site
Published in Bioorganic & medicinal chemistry letters (01-08-2007)“…Discovery of the pyrazole-naphthyl urea class of p38 MAP kinase inhibitors typified by the clinical candidate BIRB 796 has encouraged further exploration of…”
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Discovery and characterization of the N-phenyl- N′-naphthylurea class of p38 kinase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2009)“…An effort aimed at exploring structural diversity in the N-pyrazole- N′-naphthylurea class of p38 kinase inhibitors led to the synthesis and characterization…”
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pi.-Facial selectivity in catalytic osmylation reactions of chiral C1-oxygenated allylic silanes
Published in Journal of the American Chemical Society (01-06-1990)Get full text
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The kinetics of binding to p38MAP kinase by analogues of BIRB 796
Published in Bioorganic & medicinal chemistry letters (15-09-2003)“…BIRB 796, a member of the N-pyrazole-N'-naphthly urea class of p38MAPK inhibitors, binds to the kinase with both slow association and dissociation rates. Prior…”
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The kinetics of binding to p38 MAP kinase by analogues of BIRB 796
Published in Bioorganic & medicinal chemistry letters (2003)“…BIRB 796, a member of the N-pyrazole- N′-naphthly urea class of p38 MAPK inhibitors, binds to the kinase with both slow association and dissociation rates…”
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Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796)
Published in Journal of medicinal chemistry (23-10-2003)“…We report on the structure-activity relationships (SAR) of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naphthalen-1-yl]urea (BIRB…”
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An efficient procedure for the preparation of chiral β-substituted ( E)-crotylsilanes: Application of a rhodium(II) catalyzed silylformylation of terminal alkynes
Published in Tetrahedron letters (1995)“…Functionalized β-substituted ( E)-crotylsilanes ( R)-7 and ( S)-8, bearing an alkyl or aryl group adjacent to the stereogenic C-Si center have been synthesized…”
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Double stereodifferentiation in the lewis acid promoted crotylation of ( S)-2-Alkoxypropanal with chiral β-Alkyl ( E)-Crotylsilanes
Published in Tetrahedron letters (1995)“…The sense and level of 1,2-asymmetric induction have been evaluated in the Lewis acid promoted addition of ( E)crotylsilanes ( S)-1 and ( R)-2 to (…”
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