Josep Maria Huerta

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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 (logD7.4). The experimental partition is carried out using aqueous(More)
A novel series of aminopyridine N-oxides were designed, synthesized, and tested for their ability to inhibit p38alpha MAP kinase. Some of these compounds showed a significant reduction in the LPS-induced TNFalpha production in human whole blood. Structure-activity relationship studies revealed that N-oxide oxygen was essential for activity and was probably(More)
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(More)
The objective of this work was to discover a novel, long-acting muscarinic M(3) 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(More)
A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H(1) 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(More)
Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M(3) 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(More)
Novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides have been identified as potent M3 muscarinic antagonists with a long duration of action in an in vivo model of bronchoconstriction. The synthesis, structure-activity relationships and biological evaluation of this series of compounds are reported.
To a conventional silver amalgam alloy was added 1% of stanous fluoride, to prove in vitro, if it presents any antibacteria actions against S. mutans and Lactobacillus acidophilus. Thirteen Petri plate were seeded with S. mutans and 12 Petri plate with Lactobacillus, in both cases, was disposited fluoride containing amalgam and conventional amalgam. The(More)
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(More)
Carious lesions surrounding restorations represent one of the main causes of restoration failure. The addition of fluoride compounds to dental restorative materials prevents or reduces recurrent caries. The purpose of this study was to compare the capacity of three restorative materials to inhibit the development of recurrent caries in vitro. Thirty(More)
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