Josep M. Huerta
Atomic force microscopyPharmacokineticsChemical synthesisMuscarinic acetylcholine receptor M3Light scatteringOpticsAmine gas treatingMitogen-activated protein kinaseSolubilityMedicinal chemistryWhole bloodDesorptionCarbon-13 NMRReceptorOrganic chemistryKinaseAqueous solutionChemistryParticle sizePartition coefficientMaterials scienceStructure–activity relationshipLipophilicityIn vitroIn vivoStandard deviationBicyclic moleculeVilanterolBromideAbediterolSalmeterolMuscarinic antagonistAntagonistEnzyme inhibitorOral administrationOlodaterolResidence time (statistics)SulfoneBenzoic acidIndacaterolAgonistAclidinium bromideRespiratory tractOxazoloneAmmoniumReductive aminationTrifluoroacetic acidAlkylBronchoconstrictionTrisSulfonamideAlcoholAntimuscarinic AgentHistamine H1 AntagonistsPulmonary AbsorptionLaser light scatteringAqueous solubilityShake flaskMuscarinic acetylcholine receptorPartition (number theory)ChromatographyOptoelectronicsBiochemistryPotencyCadmium telluride photovoltaicsStereochemistryMedicineAcetylcholine receptorMicronizationDissolutionAlkoxy groupPharmacology
10Publications
7H-index
276Citations
Publications 10
Newest
Abstract This study describes the association rate and residence time of abediterol, a novel long-acting β 2 -adrenoceptor agonist (LABA) in Phase II development for treatment of asthma and COPD, in comparison with indacaterol, olodaterol, vilanterol and salmeterol, for both human β 1 - and β 2 -adrenoceptors. Abediterol association and dissociation rates were monitored directly by using its tritiated form. Moreover, association was determined indirectly using experimental K i and k off obtained...
6 CitationsSource
#1Axel Andrés (University of Barcelona)H-Index: 5
#2Martí Rosés (University of Barcelona)H-Index: 58
Last. Josep M. HuertaH-Index: 7
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Abstract Several procedures based on the shake-flask method and designed to require a minimum amount of drug for octanol–water partition coefficient determination have been established and developed. The procedures have been validated by a 28 substance set with a lipophilicity range from −2.0 to 4.5 (log D 7.4 ). The experimental partition is carried out using aqueous phases buffered with phosphate (pH 7.4) and n-octanol saturated with buffered water and the analysis is performed by liquid chrom...
62 CitationsSource
The key factors governing the absorption of drugs from the lungs are deposition pattern, dissolution rate, solubility and permeability. Whereas the thin epithelium in the respiratory airways is generally considered to constitute a minor barrier in the overall absorption process, the other two components depend, among other parameters, on the formulation and the particle size. This is of particular importance for compounds with very low solubility. The aim of this work was to evaluate strategies ...
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Abstract Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M3 muscarinic antagonists with long duration of action in an in vivo model of bronchoconstriction. These compounds have also presented a high level of metabolic transformation (human liver microsomes). The synthesis, structure–activity relationships and biological evaluation of these compounds are reported.
17 CitationsSource
#1Wenceslao LumerasH-Index: 3
#2Francisco CaturlaH-Index: 8
Last. Bernat VidalH-Index: 14
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A novel series of aminopyridine N-oxides were designed, synthesized, and tested for their ability to inhibit p38α MAP kinase. Some of these compounds showed a significant reduction in the LPS-induced TNFα production in human whole blood. Structure−activity relationship studies revealed that N-oxide oxygen was essential for activity and was probably a determinant factor for a marked selectivity against other related kinases. Compound 45 was identified as a potent and selective p38α inhibitor with...
25 CitationsSource
#1Maria PratH-Index: 6
#2Dolors FernándezH-Index: 2
Last. Hamish RyderH-Index: 19
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The objective of this work was to discover a novel, long-acting muscarinic M3 antagonist for the inhaled treatment of chronic obstructive pulmonary disease (COPD), with a potentially improved risk−benefit profile compared with current antimuscarinic agents. A series of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters were synthesized and evaluated. On the basis of its overall profile, (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bro...
80 CitationsSource
#1Silvia FonquernaH-Index: 6
#2Montse MiralpeixH-Index: 4
Last. Hamish RyderH-Index: 16
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A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H1 antagonists. Structure−activity relationship studies were directed toward improving in vivo activity and pharmacokinetic profile of our first lead (1). Substitution of fluorine in position 6 on the indolyl ring led to higher in vivo activity in the inhibition of histamine-induced cutaneous vascular permeability assay but lower selectivity toward 5HT2 receptor. Extensive optimization was carr...
20 CitationsSource
#2Josep M. HuertaH-Index: 7
Last. Fernando Albericio (University of Barcelona)H-Index: 89
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Abstract The solid-phase synthesis of N -substituted carbamates using the tris(alkoxy)benzyl (BAL) resin is reported. The incorporation of the primary amine was carried out by reductive amination, which was followed by reaction with an alkyl succinimidyl carbonate prepared in situ from the alcohol and N,N ′-disuccinimidyl carbonate (DSC). Final cleavage with trifluoroacetic acid rendered the target compounds. Scope and limitations of these methods are discussed. The reactions were controlled by ...
8 CitationsSource
#1Carles PuigH-Index: 7
#2María I. CrespoH-Index: 11
Last. José M. PalaciosH-Index: 97
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A series of 3,4-diaryloxazolones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure−activity relationship work was carried out within this series, and a number of potent and selective COX-2 inhibitors were identified. The replacement of the methyl sulfone group on the 4-phenyl ring by a sulfonamide moiety resulted in compounds with superior in vivo antiinflammatory properties. In the sulfonamide series, the introduction of a methyl group at the...
102 CitationsSource
#1Josep M. HuertaH-Index: 7
view all 3 authors...
Resumen en: We have studied by Laser Light Scattering (LLS) the oxides surface desorption of InSb substrates, and the subsequentgrowth of CdTe layers by molecular be...