Search Results - "Buil, Maria Antonia"
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Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists III: The role of a hydrogen-bond acceptor in long receptor residence times
Published in Bioorganic & medicinal chemistry letters (01-11-2014)“…The correct positioning and orientation of an hydrogen bond acceptor (HBA) in the tail portion of the biaryl series of CRTh2 antagonists is a requirement for…”
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Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure–Activity Relationships
Published in Journal of medicinal chemistry (08-12-2016)“…Cyclic nucleotide cAMP is a ubiquitous secondary messenger involved in a plethora of cellular responses to biological agents involving activation of adenylyl…”
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Structure-activity relationships (SAR) and structure-kinetic relationships (SKR) of sulphone-based CRTh2 antagonists
Published in European journal of medicinal chemistry (04-05-2016)“…Monocyclic and bicyclic ring systems were investigated as the “core” section of a series of diphenylsulphone-containing acetic acid CRTh2 receptor antagonists…”
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2-(1H-Pyrazol-1-yl)acetic acids as chemoattractant receptor-homologous molecule expressed on Th2 lymphocytes (CRTh2) antagonists
Published in European journal of medicinal chemistry (01-01-2014)“…In this manuscript, the synthesis and biological activity of a series of pyrazole acetic acid derivatives as CRTh2 antagonists is presented. Biological…”
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Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of bicyclic heteroaromatic acetic acids as potent CRTh2 antagonists I
Published in Bioorganic & medicinal chemistry letters (01-11-2014)“…A knowledge-based design strategy led to the discovery of several new series of potent and orally bioavailable CRTh2 antagonists where a bicyclic…”
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6
2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists
Published in Bioorganic & medicinal chemistry letters (01-06-2013)“…High throughput screening identified the pyrazole-4-acetic acid substructure as CRTh2 receptor antagonists. Optimisation of the compounds uncovered a tight SAR…”
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Discovery of novel quaternary ammonium derivatives of (3 R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists
Published in Bioorganic & medicinal chemistry letters (01-06-2011)“…Novel quaternary ammonium derivatives of N, N-disubstituted (3 R)-quinuclidinyl carbamates have been identified as potent M 3 muscarinic antagonists with long…”
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Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists
Published in Bioorganic & medicinal chemistry letters (15-04-2015)“…Novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides have been identified as potent M3 muscarinic antagonists with a long duration of action in…”
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Structure–activity relationships (SAR) and structure–kinetic relationships (SKR) of pyrrolopiperidinone acetic acids as CRTh2 antagonists
Published in Bioorganic & medicinal chemistry letters (01-11-2014)“…Pyrrolopiperidinone acetic acids (PPAs) were identified as highly potent CRTh2 receptor antagonists. In addition, many of these compounds displayed…”
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