Search results for: Wilma Quaglia

Items from 1 to 20 out of 38 results

article

New potent muscarinic receptor ligands bearing the 1,4‐dioxane nucleus: Investigation on the nature of the substituent in position 2

Gianfabio Giorgioni, Alessandro Bonifazi, Rosanna Matucci, Federica Matteucci, more

Archiv der Pharmazie > 357 > 10 > n/a - n/a

A new series of muscarinic acetylcholine receptor (mAChR) ligands obtained by inserting different substituents in position 2 of the potent 6,6‐diphenyl‐1,4‐dioxane antagonists 4 and 5 was designed and synthesized to investigate the influence of steric bulk on the mAChR affinity. Specifically, the insertion of a 2‐methyl group, affording compounds 6 and 9, resulted as the most favorable modification...

article

Advances in drug design and therapeutic potential of selective or multitarget 5‐HT1A receptor ligands

Gianfabio Giorgioni, Alessandro Bonifazi, Luca Botticelli, Carlo Cifani, more

Medicinal Research Reviews > 44 > 6 > 2640 - 2706

5‐HT1A receptor (5‐HT1A‐R) is a serotoninergic G‐protein coupled receptor subtype which contributes to several physiological processes in both central nervous system and periphery. Despite being the first 5‐HT‐R identified, cloned and studied, it still represents a very attractive target in drug discovery and continues to be the focus of a myriad of drug discovery campaigns due to its involvement...

article

Targeting orexin receptors: Recent advances in the development of subtype selective or dual ligands for the treatment of neuropsychiatric disorders

Alessandro Bonifazi, Fabio Del Bello, Gianfabio Giorgioni, Alessandro Piergentili, more

Medicinal Research Reviews > 43 > 5 > 1607 - 1667

Orexin‐A and orexin‐B, also named hypocretin‐1 and hypocretin‐2, are two hypothalamic neuropeptides highly conserved across mammalian species. Their effects are mediated by two distinct G protein‐coupled receptors, namely orexin receptor type 1 (OX1‐R) and type 2 (OX2‐R), which share 64% amino acid identity. Given the wide expression of OX‐Rs in different central nervous system and peripheral areas...

article

β‐Catenin signaling is important for osteogenesis and hematopoiesis recovery following methotrexate chemotherapy in rats

Jian Fan, Yu‐Wen Su, Mohammadhossein Hassanshahi, Chia‐Ming Fan, more

Journal of Cellular Physiology > 236 > 5 > 3740 - 3751

Cancer chemotherapy can significantly impair the bone formation and cause myelosuppression; however, their recovery potentials and mechanisms remain unclear. This study investigated the roles of the β‐catenin signaling pathway in bone and bone marrow recovery potentials in rats treated with antimetabolite methotrexate (MTX) (five once‐daily injections, 0.75 mg/kg) with/without β‐catenin inhibitor...

article

Syntheses and biological studies of nitroimidazole conjugated heteroscorpionate ligands and related Cu(I) and Cu(II) complexes

Maura Pellei, Valentina Gandin, Cristina Cimarelli, Wilma Quaglia, more

Journal of Inorganic Biochemistry > 2018 > 187 > C > 33-40

Copper(I) and copper(II) complexes of 5-nitroimidazole conjugated heteroscorpionate ligands have been synthesized. In particular, the new 2,2-bis(pyrazol-1-yl)-N-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl)acetamide ligand (L^HMN) was synthesized by direct coupling of preformed side chain acid with 5-nitroimidazole and its coordination chemistry was investigated towards Cu(I) and Cu(II) acceptors and...

article

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments

Fabio Del Bello, Alessandro Bonifazi, Gianfabio Giorgioni, Riccardo Petrelli, more

European Journal of Medicinal Chemistry > 2017 > 137 > C > 327-337

To obtain novel muscarinic acetylcholine receptor (mAChR) antagonists, the enantiomers of the hybrid compounds 3–5, in which the quinuclidin-3-yloxy fragment of solifenacin and the 6,6-diphenyl-1,4-dioxane-2-yl moiety of 2 linked by an ester or ether spacer were embedded in the same chemical entity, were prepared and evaluated for their affinity at the five mAChR subtypes (M₁-M₅). Stereochemistry...

article

Synergic stimulation of serotonin 5-HT1A receptor and α2-adrenoceptors for neuropathic pain relief: Preclinical effects of 2-substituted imidazoline derivatives

Lorenzo Di Cesare Mannelli, Carla Ghelardini, Laura Micheli, Fabio Del Bello, more

European Journal of Pharmacology > 2017 > 810 > C > 128-133

Neuropathic pain affects millions of people causing disability and impairing quality of life. Commonly used analgesics are generally characterized by limited therapeutic outcomes. The serotonin 5‐HT_1A receptor and the α₂ adrenergic receptors are involved in central nociceptive mechanisms with a pivotal role in the inhibitory descending pain pathway. Since their stimulation may modulate the nervous...

article

The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes

Fabio Del Bello, Alessandro Bonifazi, Mario Giannella, Gianfabio Giorgioni, more

European Journal of Medicinal Chemistry > 2017 > 125 > C > 233-244

N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine (3) is a potent 5-HT_1A receptor and α_1d-adrenoceptor (α_1d-AR) ligand. Analogues 5–10 were rationally designed and prepared to evaluate whether electronic and/or lipophilic properties of substituents in the ortho position of its phenoxy moiety exert any favorable effects on the affinity/activity at 5-HT_1A receptor and improve...

article

Identification of 2-aminopyrimidine derivatives as inhibitors of the canonical Wnt signaling pathway

Fabio Del Bello, Aniket Farande, Mario Giannella, Alessandro Piergentili, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 17 > 5725-5733

The canonical Wnt signaling pathway plays a fundamental role in embryonic as well as in adult development. Consequently, dysregulation of the pathway has been linked to a wide spectrum of pathological conditions. In a program aimed at the identification of small molecule inhibitors of the canonical Wnt pathway we identified a series of 2-aminopyrimidine derivatives which specifically inhibited the...

article

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites

Fabio Del Bello, Alessandro Bonifazi, Wilma Quaglia, Angelica Mazzolari, more

Bioorganic & Medicinal Chemistry Letters > 2014 > 24 > 15 > 3255-3259

The methyl group in cis stereochemical relationship with the basic chain of all pentatomic cyclic analogues of ACh is crucial for the agonist activity at mAChR. Among these only cevimeline (1) is employed in the treatment of xerostomia associated with Sjögren’s syndrome. Here we demonstrated that, unlike 1,3-dioxolane derivatives, in the 1,4-dioxane series the methyl group is not essential for the...

article

Cross-talk between alpha_1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation

Maria Beatrice Morelli, Consuelo Amantini, Massimo Nabissi, Sonia Liberati, more

BMC Cancer > 2014 > 14 > 1 > 1-13

Background There is evidence that calcium (Ca²⁺) increases the proliferation of human advanced prostate cancer (PCa) cells but the ion channels involved are not fully understood. Here, we investigated the correlation between alpha_1D-adrenergic receptor (alpha_1D-AR) and the transient receptor potential vanilloid type 1 (TRPV1) expression levels in human PCa tissues and evaluated the ability of alpha...

article

Roles of Wnt/β-catenin signalling pathway in the bony repair of injured growth plate cartilage in young rats

Rosa Chung, Derick Wong, Carmen Macsai, Alessandro Piergentili, more

Bone > 2013 > 52 > 2 > 651-658

Growth plate cartilage is responsible for longitudinal growth of the long bone in children, and its injury is often repaired by bony tissue, which can cause limb length discrepancy and/or bone angulation deformities. Whilst earlier studies with a rat growth plate injury repair model have identified inflammatory, mesenchymal infiltration, osteogenesis and remodeling responses, the molecular mechanisms...

article

Favourable involvement of α2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement

Valerio Mammoli, Alessandro Bonifazi, Fabio Del Bello, Eleonora Diamanti, more

Bioorganic & Medicinal Chemistry > 2012 > 20 > 7 > 2259-2265

Aim of the present study was to obtain novel α ₂ -adrenoreceptor (α ₂ -AR) antagonists, possibly endowed with subtype-selectivity. Therefore, inspired by the non subtype-selective α ₂ -AR antagonist idazoxan, we designed 1,4-dioxane derivatives bearing an aromatic area in position 5 or 6 and the imidazoline nucleus in position 2. Among the novel molecules 1–6, compound 2, with...

article

Might the observed α2A-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?

Eleonora Diamanti, Fabio Del Bello, Giuseppe Carbonara, Antonio Carrieri, more

Bioorganic & Medicinal Chemistry > 2012 > 20 > 6 > 2082-2090

We recently reported that the α ₂ -adrenoreceptor (AR) ligand allyphenyline (9) significantly enhanced morphine analgesia (due to its α _2C -AR agonism), was devoid of sedative side effects (due to its α _2A -AR antagonism), prevented and reversed morphine tolerance and dependence. To highlight the molecular characteristics compatible with this behaviour and to obtain novel agents...

article

Fruitful Adrenergic α _2C -Agonism/α _2A -Antagonism Combination to Prevent and Contrast Morphine Tolerance and Dependence(1) ^, ^†

Fabio Del Bello, Laura Mattioli, Francesca Ghelfi, Mario Giannella, more

Journal of Medicinal Chemistry > 2010 > 53 > 21 > 7825 - 7835

article

Structure–activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: Synthesis, biological evaluation, and α1d computational study

Antonio Carrieri, Alessandro Piergentili, Fabio Del Bello, Mario Giannella, more

Bioorganic & Medicinal Chemistry > 2010 > 18 > 19 > 7065-7077

A series of novel openphendioxan analogues were synthesized and tested at α ₁ -adrenoreceptor (AR) subtypes by binding and functional assays. The α _1d -AR binding profile was also examined by means of 2D, 3D-QSAR together with docking studies. Multiple regression analysis suggested the relevance of adequate number of heteroatoms in the whole molecule and of passive membrane diffusion...

article

Novel Highly Potent and Selective σ ₁ Receptor Antagonists Related to Spipethiane

Alessandro Piergentili, Consuelo Amantini, Fabio Del Bello, Mario Giannella, more

Journal of Medicinal Chemistry > 2010 > 53 > 3 > 1261 - 1269

article

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation

Alessandro Piergentili, Wilma Quaglia, Fabio Del Bello, Mario Giannella, more

Bioorganic & Medicinal Chemistry > 2009 > 17 > 24 > 8174-8185

Novel analogues of cis-N,N,N-trimethyl-(6-methyl-1,4-dioxan-2-yl)methanaminium iodide (2a) were synthesized by inserting methyl groups alternatively or simultaneously in positions 5 and 6 of the 1,4-dioxane nucleus in all combinations. Their biological profile was assessed by receptor binding assays at human muscarinic M ₁ –M ₅ receptors stably expressed in CHO cells and by functional...

article

Might Adrenergic α _2C -Agonists/α _2A -Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?(1)

Claudia Cardinaletti, Laura Mattioli, Francesca Ghelfi, Fabio Del Bello, more

Journal of Medicinal Chemistry > 2009 > 52 > 22 > 7319 - 7322

article

Structure−Activity Relationships in 1,4-Benzodioxan-Related Compounds. 9.(1) From 1,4-Benzodioxane to 1,4-Dioxane Ring as a Promising Template of Novel α _1D -Adrenoreceptor Antagonists, 5-HT _1A Full Agonists, and Cytotoxic Agents ^†

Wilma Quaglia, Alessandro Piergentili, Fabio Del Bello, Yogita Farande, more

Journal of Medicinal Chemistry > 2008 > 51 > 20 > 6359 - 6370

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Search results for: Wilma Quaglia

New potent muscarinic receptor ligands bearing the 1,4‐dioxane nucleus: Investigation on the nature of the substituent in position 2

Advances in drug design and therapeutic potential of selective or multitarget 5‐HT1A receptor ligands

Targeting orexin receptors: Recent advances in the development of subtype selective or dual ligands for the treatment of neuropsychiatric disorders

β‐Catenin signaling is important for osteogenesis and hematopoiesis recovery following methotrexate chemotherapy in rats

Syntheses and biological studies of nitroimidazole conjugated heteroscorpionate ligands and related Cu(I) and Cu(II) complexes

Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments

Synergic stimulation of serotonin 5-HT1A receptor and α2-adrenoceptors for neuropathic pain relief: Preclinical effects of 2-substituted imidazoline derivatives

The replacement of the 2-methoxy substituent of N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine improves the selectivity for 5-HT1A receptor over α1-adrenoceptor and D2-like receptor subtypes

Identification of 2-aminopyrimidine derivatives as inhibitors of the canonical Wnt signaling pathway

Mode of interaction of 1,4-dioxane agonists at the M2 and M3 muscarinic receptor orthosteric sites

Cross-talk between alpha_1D-adrenoceptors and transient receptor potential vanilloid type 1 triggers prostate cancer cell proliferation

Roles of Wnt/β-catenin signalling pathway in the bony repair of injured growth plate cartilage in young rats

Favourable involvement of α2A-adrenoreceptor antagonism in the I2-imidazoline binding sites-mediated morphine analgesia enhancement

Might the observed α2A-adrenoreceptor agonism or antagonism of allyphenyline analogues be ascribed to different molecular conformations?

Fruitful Adrenergic α _2C -Agonism/α _2A -Antagonism Combination to Prevent and Contrast Morphine Tolerance and Dependence(1) ^, ^†

Structure–activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: Synthesis, biological evaluation, and α1d computational study

Novel Highly Potent and Selective σ ₁ Receptor Antagonists Related to Spipethiane

Properly substituted 1,4-dioxane nucleus favours the selective M3 muscarinic receptor activation

Might Adrenergic α _2C -Agonists/α _2A -Antagonists Become Novel Therapeutic Tools for Pain Treatment with Morphine?(1)

Structure−Activity Relationships in 1,4-Benzodioxan-Related Compounds. 9.(1) From 1,4-Benzodioxane to 1,4-Dioxane Ring as a Promising Template of Novel α _1D -Adrenoreceptor Antagonists, 5-HT _1A Full Agonists, and Cytotoxic Agents ^†

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