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Fabrizio Bruni

Explore the profile of Fabrizio Bruni including associated specialties, affiliations and a list of published articles. Areas
Snapshot
Articles 11
Citations 53
Followers 0
Related Specialties
Chemistry
Biochemistry
Top 10 Co-Authors
Annarella Costanzo
Silvia Selleri
Claudia Martini
Giovanna Ciciani
Gabriella Guerrini
Fabrizio Melani
Francois Besnard
Marina Montali
Camilla Costagli
Carla Ghelardini
Published In
Bioorg Med Chem
J Med Chem
Affiliations
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Recent Articles
1.
Development of ligands at γ-aminobutyrric acid type A (GABAA) receptor subtype as new agents for pain relief
Guerrini G, Ciciani G, Bruni F, Selleri S, Martini C, Daniele S, et al.
Bioorg Med Chem . 2011 Nov; 19(24):7441-52. PMID: 22094278
The identification of compounds with selective anxiolytic-like effects, exerted through the benzodiazepine site on γ-aminobutyric acid type A (GABA(A)) receptors, and that show pronounced antihyperalgesia in several pain models, has...
2.
New 3-, 8-disubstituted pyrazolo[5,1-c][1,2,4]benzotriazines useful for studying the interaction with the HBp-3 area (hydrogen bond point area) in the benzodiazepine site on the γ-aminobutyric acid type A (GABAA) receptor
Guerrini G, Ciciani G, Bruni F, Selleri S, Melani F, Daniele S, et al.
Bioorg Med Chem . 2011 May; 19(10):3074-85. PMID: 21530274
The pharmacophoric model using ADLR procedure, based on pyrazolo[5,1-c][1,2,4]benzotriazine system, studied in our laboratory, allowed us to identify the essential interaction points (HBp-1, HBp-2, and Lp-1) and the important areas...
3.
New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular...
Guerrini G, Ciciani G, Bruni F, Selleri S, Guarino C, Melani F, et al.
J Med Chem . 2010 Oct; 53(21):7532-48. PMID: 20939501
In the search for potent ligands at the benzodiazepine site on the GABA(A) receptor, new fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine system were synthesized to evaluate the importance of the introduction...
4.
Synthesis, in vivo evaluation, and molecular modeling studies of new pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide derivatives. Identification of a bifunctional hydrogen bond area related to the inverse agonism
Guerrini G, Ciciani G, Cambi G, Bruni F, Selleri S, Guarino C, et al.
J Med Chem . 2009 Jul; 52(15):4668-82. PMID: 19591485
A new series of pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 8-alkyloxy-/aryloxy-/arylalkyloxy and 8-aryl-/arylalkylderivatives variously substituted at the 3-position were synthesized and binding studies at the benzodiazepine site on GABA(A) receptor were carried out. The...
5.
Novel 3-aroylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted, ligands at GABAA/benzodiazepine receptor complex: synthesis, pharmacological and molecular modeling studies
Guerrini G, Ciciani G, Cambi G, Bruni F, Selleri S, Melani F, et al.
Bioorg Med Chem . 2008 Mar; 16(8):4471-89. PMID: 18325771
The synthesis and binding studies of a series of 3-acylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted are reported. High-affinity ligands at benzodiazepine site on GABA(A) receptor complex (GABA(A)/BzR complex) were obtained when the 3-aroyl...
6.
Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage
Guerrini G, Ciciani G, Cambi G, Bruni F, Selleri S, Besnard F, et al.
Bioorg Med Chem . 2007 Feb; 15(7):2573-86. PMID: 17306981
The synthesis and the binding study of new 3-iodiopyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides 8-alkyloxy substituted are reported. The replacement at position 3 with an iodine atom, with respect to substituents capable to...
7.
A novel selective GABA(A) alpha1 receptor agonist displaying sedative and anxiolytic-like properties in rodents
Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, et al.
J Med Chem . 2005 Oct; 48(21):6756-60. PMID: 16220991
In our pursuit to identify selective ligands for Bz/GABA(A) receptor subtypes, a novel pyrazolo[1,5-a]pyrimidine derivative (4), the azaisostere of zolpidem, was synthesized and evaluated in vitro on bovine brain homogenate...
8.
Benzodiazepine receptor ligands. 8: synthesis and pharmacological evaluation of new pyrazolo[5,1-c] [1,2,4]benzotriazine 5-oxide 3- and 8-disubstituted: high affinity ligands endowed with inverse-agonist pharmacological efficacy
Guerrini G, Costanzo A, Ciciani G, Bruni F, Selleri S, Costagli C, et al.
Bioorg Med Chem . 2005 Oct; 14(3):758-75. PMID: 16214350
The synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 8-substituted are reported. The nature of these substituents (in terms of lipophilic and electronic features) seems to influence...
9.
Insight into 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as peripheral benzodiazepine receptor ligands: synthesis, biological evaluation and 3D-QSAR investigation
Selleri S, Gratteri P, Costagli C, Bonaccini C, Costanzo A, Melani F, et al.
Bioorg Med Chem . 2005 Jun; 13(16):4821-34. PMID: 15975799
The present paper reports the synthesis and binding studies of new 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamides as selective Peripheral Benzodiazepine Receptor (PBR) ligands. The variability of substituents at the 3-position was investigated and...
10.
Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands
Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, et al.
J Med Chem . 2003 Jan; 46(2):310-3. PMID: 12519068
New 3-aryl-6-(3-thienyl)pyrazolo[1,5-a]pyrimidin-7-ones (2a-j) are synthesized and evaluated in vitro on Bz/GABA(A) receptors and on recombinant benzodiazepine receptors (alpha x beta 2/3 gamma 2; x = 1-3, 5) expressed in HEK293...