A5042717549- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Eicosanoids and Hypertension Pharmacology
- Synthesis and biological activity
- Synthesis and Reactions of Organic Compounds
- Organic Chemistry Cycloaddition Reactions
- Chemical Reaction Mechanisms
- Synthesis and Biological Evaluation
- Inflammatory mediators and NSAID effects
- Structural and Chemical Analysis of Organic and Inorganic Compounds
- Analytical Chemistry and Chromatography
- Coordination Chemistry and Organometallics
- Asymmetric Synthesis and Catalysis
- Pharmacological Receptor Mechanisms and Effects
- Phenothiazines and Benzothiazines Synthesis and Activities
- Inorganic and Organometallic Chemistry
- Synthesis and pharmacology of benzodiazepine derivatives
- Chemical Synthesis and Reactions
- Synthesis of β-Lactam Compounds
- Drug Transport and Resistance Mechanisms
- Synthesis and Catalytic Reactions
- Synthesis of heterocyclic compounds
- Synthesis and Reactivity of Sulfur-Containing Compounds
- Pharmacological Effects and Assays
- Click Chemistry and Applications
University of Pisa
2004-2016
Goodwin College
2008
University of Illinois Urbana-Champaign
2008
University of Benghazi
2008
GlaxoSmithKline (Spain)
2002
Some new oxime ethers of types 7 and 8, in which the methyleneaminoxy group, CN−O, oxiconazole 6 is an inverted atomic sequence, were synthesized tested for their antifungal activities. Among them, type compounds, such as N-ethoxy-morpholino-substituted derivatives 7l−o (Table 1), showed good properties against Candida strains tested, with minimum inhibitory concentration (MIC) values similar to those reference drug 6. A remarkable result was obtained these azoles, had shown a cidal...
Transthyretin (TTR) is one of thirty non-homologous proteins whose misfolding, dissociation, aggregation, and deposition linked to human amyloid diseases. Previous studies have identified that TTR amyloidogenesis can be inhibited through stabilization the native tetramer state by small molecule binding thyroid hormone sites TTR. We evaluated a new series beta-aminoxypropionic acids (compounds 5-21), with single aromatic moiety (aryl or fluorenyl) flexible oxime tether carboxylic acid. These...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTAn interdisciplinary approach to the design of new structures active at .beta.-adrenergic receptor. Aliphatic oxime ether derivativesB. Macchia, A. Balsamo, Lapucci, Martinelli, F. M. C. Breschi, B. Fantoni, and E. MartinottiCite this: J. Med. Chem. 1985, 28, 2, 153–160Publication Date (Print):February 1, 1985Publication History Published online1 May 2002Published inissue 1 February...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTStructure-activity relationship in cinnamamides. 3. Synthesis and anticonvulsant activity evaluation of some derivatives (E)- (Z)-m-(trifluoromethyl)cinnamamideA. Balsamo, P. Crotti, A. Lapucci, B. Macchia, F. Cuttica, N. PasseriniCite this: J. Med. Chem. 1981, 24, 5, 525–532Publication Date (Print):May 1, 1981Publication History Published online1 May 2002Published inissue 1...
This study was aimed at investigating the antitumor activity of novel 2-oxindole derivatives against a well-characterized human nonsmall cell lung cancer (NSCLC) line. Test compounds produced an antiproliferative in low micromolar/submicromolar range concentrations and significantly induced typical apoptotic morphology with shrinkage, nuclear condensation fragmentation, rupture cells into debris relatively percentage A549 cells. Cell cycle arrest occurred G1/S phase (1a 2), Akt...
Salicylaldoximes possess a hydrogen-bonded pseudocyclic A′ ring in place of the typical phenolic A that is characteristic most estrogen receptor (ER) ligands. Monoaryl-substituted salicylaldoximes were obtained by replacing phenol moiety (ring A) ERβ pharmacophore with pseudocycle ring, which has previously been shown to behave as bioequivalent phenols nonselective ER In this series, small substituents (CH3, CN, Cl) introduced into central phenyl scaffold. An efficient sequential...
Abstract Aldose reductase (ARL2) is the first enzyme in polyol pathway which catalyzes NADPH‐dependent reduction of glucose to sorbitol. Its involvement on diabetic complications makes this a challenge therapeutic target widely investigated limit and/or prevent them. On basis, limited series 4‐spiro‐oxazolidinone‐benzopyran derivatives ( 1–7 ) were synthesized evaluate them as potential ARL2 inhibitors. The activity was determined spectrophotometrically by monitoring oxidation NADPH...
Previous experimental and theoretical studies carried out on the mechanism of action adrenergic drugs have shown that (methyleneaminoxy)methyl moiety (C = NOCH2, MAOMM) can be considered as a "bioisostere" an aryl group (Ar). On this basis, series substituted beta-aminoxypropionic acids (AOPAs) were synthesized analogues antiinflammatory arylacetic (ArAAs), in which Ar portion is by MAOMM, with aim evaluating whether any activity could obtained from class after substitution MAOMM. The AOPAs...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTConformational effects on the activity of drugs. 10. Synthesis, conformation, and pharmacological properties 1-(2,5-dimethoxyphenyl)-2-aminoethanols their morpholine analogsE. Epifani, A. Lapucci, B. Macchia, F. P. Tognetti, M. C. Breschi, Del Tacca, E. Martinotti, L. GiovanniniCite this: J. Med. Chem. 1983, 26, 2, 254–259Publication Date (Print):February 1, 1983Publication History Published online1 May 2002Published inissue 1 February...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTSynthesis and antimicrobial properties of substituted .beta.-aminoxypropionyl penicillins cephalosporinsA. Balsamo, G. Broccali, A. Lapucci, B. Macchia, F. E. Orlandini, RosselloCite this: J. Med. Chem. 1989, 32, 6, 1398–1401Publication Date (Print):June 1, 1989Publication History Published online1 May 2002Published inissue 1 June 1989https://pubs.acs.org/doi/10.1021/jm00126a041https://doi.org/10.1021/jm00126a041research-articleACS...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTConformational effects on the activity of drugs. 13. A revision previously proposed models for activation .alpha.- and .beta.-adrenergic receptorsBruno Macchia, Aldo Balsamo, Maria C. Breschi, Annalina Lapucci, Antonio Lucacchini, Franco Clementina Manera, Adriano Martinelli, Claudia Martini, Cite this: J. Med. Chem. 1992, 35, 6, 1009–1018Publication Date (Print):March 1, 1992Publication History Published online1 May 2002Published inissue 1 March...
In previous papers dealing with the study of conformations and biopharmacological activity conformationally restrained analogs sympathomimetic catecholamines (NE ISO), proposals were advanced for three-dimensional molecular models A, B, C; these provided information about steric requirements direct activation alpha 1, 2,beta beta 2 adrenoceptors, respectively. The 1-(aminomethyl)-6,7-dihydroxyisochromans 11 12 1-(aminomethyl)-5,6-dihydroxyisochromans 13 14 (1-AMDICs) are two different types...
Two kinds of cyclic analogues norepinephrine (NE, 7) and isoprenaline (ISO, 8), in which the C(1)-C(2) side chain these amino alcohols is incorporated its preferred conformation ring 2-(3,4-dihydroxyphenyl)-morpholines 9 10 (2-DPMs) 3-(3,4-dihydroxyphenyl)-3-piperidinols 11 12 (3-DPPs), respectively, were synthesized assayed for their adrenergic activity on various isolated preparations. The 2-DPMs 3-DPPs showed an alpha- beta-agonist comparable to that NE ISO...
ADVERTISEMENT RETURN TO ISSUEPREVArticleNEXTRole of the (acyloxy)methyl moiety in eliciting adrenergic .beta.-blocking activity 3-(acyloxy)propanolaminesB. Macchia, A. Balsamo, Lapucci, F. Martinelli, H. L. Ammon, S. M. Prasad, C. Breschi, Ducci, and E. MartinottiCite this: J. Med. Chem. 1987, 30, 4, 616–622Publication Date (Print):April 1, 1987Publication History Published online1 May 2002Published inissue 1 April...
Abstract Objectives The aim of the study was to evaluate antitumour effect in vitro newly synthesized 7-substituted 2,3-dihydro-1,8-naphthyridines. Methods Characterization tools included cell viability assay, caspase 3/7 induction, DNA fragmentation, fibroblast growth factor type 1 receptor kinase inhibition, and in-vitro antiangiogenic analysis. Key findings Treatment MIA PaCa-2 human pancreatic cancer cells with test compounds showed time- concentration-dependent cytotoxicity IC50 values...
A series of 1-(p-nitrophenyl)-2-aminoethanol derivatives and their morpholine analogues have been synthesized pharmacologically investigated in order to confirm some pharmacological observations made with the N-isopropyl-substituted compounds. In agreement previously obtained results, weak alpha-adrenergic-stimulating activity potentiating effect on responses norepinephrine found open-chain compounds persist corresponding semirigid cyclic analogues. The results are discussed light common...