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394 results on '"Baraldi, P. G."'

2. Synthesis and Biological Studies of a New Series of 5-Heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as Human A3 Adenosine Receptor Antagonists. Influence of the Heteroaryl Substituent on Binding Affinity and Molecular Modeling Investigations

Author

Pastorin, G, DA ROS, Tatiana, Bolcato, C, Montopoli, C, Moro, S, Cacciari, B, Baraldi, P. G., Varani, K, Borea, P. A., Spalluto, Giampiero, Pastorin, G, DA ROS, Tatiana, Bolcato, C, Montopoli, C, Moro, S, Cacciari, B, BARALDI P., G, Varani, K, BOREA P., A, and Spalluto, Giampiero

Subjects
adenosine
Abstract

Some pyrazolotriazolopyrimidines bearing different heteroarylcarbamoylamino moieties at the N5-position are described. We previously reported the synthesis of a water soluble compound with high potency and selectivity versus the human A3 adenosine receptor as antagonist, and herein we present an enlarged series of compounds related to the previously mentioned one. These compounds showed A3 adenosine receptor affinity in the nanomolar range and different levels of selectivity evaluated in radioligand binding assays at human A1, A2A, A2B, and A3 adenosine receptors. In particular, the effect of the heteroaryl substituents at the N5 position has been analyzed. This study allows us to recognize that the presence of a pyridinium moiety in this position not only increases water solubility but also improves or retains potency and selectivity at the human A3 adenosine receptors. In contrast, replacement of pyridine with different heterocycles produces loss of affinity and selectivity at the human A3 adenosine receptors. A molecular modeling study has been carried out with the aim to explain these various binding profiles.

Published
2006

3. Combined Target-based and Ligand-based Drug Design Approach as Tool to Define a Novel Pharmacophore Model of Human A3 Adenosine Receptor Antagonists: Pyrazolo[4,3-E]1,2,4-Triazolo[1,5-C]Pyrimidine Derivatives as a Key Study

Author

MORO S, BRAIUCA P., DEFLORIAN F, PASTORIN G, FERRARI C, CACCIARI B, BARALDI P. G, VARANI K, BOREA P. A, SPALLUTO, GIAMPIERO, Moro, S, Braiuca, P., Deflorian, F, Pastorin, G, Ferrari, C, Cacciari, B, BARALDI P., G, Varani, K, BOREA P., A, and Spalluto, Giampiero

Subjects
adenosine, Receptors, Antagonists, Receptor
Abstract

A combined target-based and ligand-based drug design approach has been carried out to define a novel pharmacophore model of the human A3 receptor antagonists. High throughput molecular docking and comparative molecular field analysis (CoMFA) have been used in tandem to assemble a new target based pharmacophore model.

Published
2005

5. Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists

Author

Baraldi P. G., Baraldi S., Saponaro G., Preti D., Romagnoli R., Piccagli L., Moorman A. R., Zaid A. N., Varani K., Borea P. A., Tabrizi M. A., CAVALLI, ANDREA, RECANATINI, MAURIZIO, Baraldi P.G., Baraldi S., Saponaro G., Preti D., Romagnoli R., Piccagli L., Cavalli A., Recanatini M., Moorman A.R., Zaid A.N., Varani K., Borea P.A., and Tabrizi M.A.

Subjects
3D QSAR
Abstract

Molecular modeling studies, including the comparative molecular field analysis (CoMFA) method, on 52 antagonists of the A(2B) adenosine receptor with known biological activity were performed to identify the three-dimensional features responsible for A(2B) adenosine receptor antagonist activity. On the basis of these and previous results on the potent antagonist effect of 8-pyrazolyl-xanthines at human A(2B)AR, a new series of compounds was synthesized and evaluated in binding studies against the human A(1), A(2A), A(3), and A(2B)ARs. A remarkable improvement in selectivity with respect to the previous series, maintaining the potency at human A(2B) receptor, was achieved, as exemplified by the 8-[3-(4-chloro-6-trifluoromethyl-1H-benzoimidazol-2-yl-methoxy)-1-methyl-1H-pyrazol-5-yl]-1,3-dipropyl-3,7-dihydro-purine-2,6-dione derivative 66: K(i) A(2B) = 9.4 nM, IC(50) hA(2B) = 26 nM hA(1)/hA(2B) = 269, hA(2A)/hA(2B) > 106, hA(3)/hA(2B) >106. This study also led to the identification of a series of pyrazole-xanthine compounds with a simplified structure, exemplified by 8-(3-hydroxy-1-methyl-1H-pyrazol-5-yl)-xanthine 80 displaying very high affinity at A(2B)AR with good selectivity over AR subtypes (K(i) = 4.0 nM, IC(50) hA(2B) = 20 nM hA(1)/hA(2B) = 183, hA(2A),hA(3)/hA(2B) > 250).

Published
2012

13. Occurrence of anti-Brucella antibodies in intensive pig farming and in non-technified pig herds.

Author

Ricardo, Paloma, Oliveira, Luís G., Baraldi, Thaís G., Mechler, Marina L., Almeida, Henrique M. S., da Silva, Glaucenyra C. P., Gatto, Igor R. H., and Mathias, Luis A.

Abstract

Copyright of Pesquisa Veterinaria Brasileira is the property of Colegio Brasileiro de Patologia Animal - CBPA and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Published
2016
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36. Protection by pyroglutamic acid and some of its newly synthesized derivatives against glutamate-induced seizures in mice

Author

Beani, L., Bianchi, C., Baraldi, P. G., Stefano Manfredini, and Pollini, G. P.

Subjects
Male, N-Methylaspartate, Behavior, Animal, synthesis, Glutamic Acid, Motor Activity, Anticonvulsives, Pyroglutamic acid, Pyrrolidonecarboxylic Acid, NO, CAS 98-79-3, Mice, Antiepileptics, Glutamates, Seizures, derivatives, Animals, Anticonvulsants, Indicators and Reagents, pharmacology, Pyroglutamic acid, derivatives, pharmacology, synthesis, Injections, Intraperitoneal, Injections, Intraventricular
Abstract

The protection by pyroglutamic acid (CAS 98-79-3) and derivatives Ia-i (injected i.p.) against glutamate- and NMDA (N-methyl-D-aspartate) (i.c.v.) induced seizures in mice has been studied in comparison with known antiepileptics and antagonists of excitatory aminoacids. The potency of pyroglutamic acid and some derivatives (Id,f,g,h) against glutamate-induced convulsions was similar to that shown by glutamic acid diethylester and by valproic acid. Interestingly, pyroglutamic acid did not affect NMDA-induced convulsions which were well antagonized by both 2-amino-5-phosphono valeric acid and by diazepam. Thus, pyroglutamic acid may represent the starting for synthesis of excitatory aminoacid antagonists acting at non NMDA receptors.

Published
1990

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