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Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept.
Intratracheal administration of 9e effectively inhibited allergen-induced airway inflammation without inducing cytokines systemically, suggesting the TLR7 agonist with antedrug characteristics 9e (SM-324405) is a novel candidate for immunotherapy of allergic diseases. Expand
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
We report the discovery of novel series of highly potent TLR7 agonists based on 8-oxoadenines, 1 and 2 by introducing and optimizing various tertiary amines onto the N(9)-position of the adenineExpand
Total Synthesis of the Posttranslationally Modified Polyazole Peptide Antibiotic Plantazolicin A.
The power of rhodium-carbene methodology in chemistry is demonstrated by the synthesis of a structurally complex polyazole antibiotic and a likely dynamic hairpin conformation with a hinge region around the two isoleucine residues is revealed. Expand
Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists.
The synthesis and properties of an indane based series of ghrelin receptor full agonists are reported, which have been shown to generate a sustained increase of IGF-1 levels in dog and have been thoroughly investigated with respect to their functional activity. Expand
Preparation of kinase‐biased compounds in the search for lead inhibitors of kinase targets
This work describes the preparation of approximately 13,000 compounds for rapid identification of hits in high‐throughput screening (HTS). These compounds were designed as potential serine/threonineExpand
Highly Selective One-Pot Synthesis of Polysubstituted Isoflavanes using Styryl Ethers and Electron-Withdrawing ortho -Quinone Methides Generated in Situ
A highly selective one-pot synthesis of polysubstituted isoflavanes has been developed. The reaction proceeds through the cycloaddition of methyl styryl ethers, derived from phenylacetaldehydeExpand
Large-scale synthesis of new cyclazines, 5-thia-1,8b-diazaacenaphthylene-3-carboxylic acid derivatives having the peripheral 12π-electron ring system
Abstract The 5-thia-1,8b-diazaacenaphthylenes ( 2 and its ester, 8 ) are new cyclazines, in which a paramagnetic ring is present in the peripheral 12π-electron ring system. Three convenient methodsExpand
Improved selectivity for Cu(II) of methyl-substituted poly(pyrazolyl)-borates, [HB(3-Mepz)3]- and [B(3-Mepz)4]-, through steric contact
The separation of first-series transition metal and Cd2+ ions has been studied by solvent extraction using methyl substituted poly(pyrazolyl)borates. These ligands did not extract all of the studiedExpand
Practical Synthesis of Low-Density Lipoprotein Receptor Upregulator, N-[1-(3-Phenylpropane-1-yl)piperidin-4-yl]-5-thia-1,8b-diazaacenaphthylene-4- carboxamide
A shorter and more practical method for the preparation of N-[1-(3-phenylpropane-1-yl)piperidin-4-yl]-5-thia-1,8b-diazaacenaphthylene-4-carboxamide (4) as an upregulator of the LDL receptor has beenExpand