Research Topics
| R CirilliSummaryAffiliation: Istituto Superiore di Sanit Country: Italy Publications
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Detail Information
Publications
HPLC enantioseparation and absolute configuration of novel anti-inflammatory pyrrole derivativesMariangela Biava
Universita La Sapienza, Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, 00185 Rome, Italy
Chirality 20:775-80. 2008..The key step of our stereochemical characterization approach is the production at mg-scale of enantiomerically pure forms by HPLC on Chiralpak IA stationary phase...- A chromatographic study on the exceptional enantioselectivity of cellulose tris(4-methylbenzoate) towards C5-chiral 4,5-dihydro-(1H)-pyrazole derivativesRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, I 00161 Rome, Italy
J Chromatogr A 1218:5653-7. 2011..In order to clarify some aspects of the chiral discrimination process, the thermodynamic parameters associated to the enantiorecognition and the enantiomer elution order were established... - High-performance liquid chromatography enantioseparation of proton pump inhibitors using the immobilized amylose-based Chiralpak IA chiral stationary phase in normal-phase, polar organic and reversed-phase conditionsRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy
J Chromatogr A 1177:105-13. 2008..A very simple method based on on-line detection of optical rotational sign during enantioselective HPLC was developed to assign the absolute configuration and enantiomeric elution order... - Direct HPLC enantioseparation of chiral aptazepine derivatives on coated and immobilized polysaccharide-based chiral stationary phasesRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Rome, Italy
Chirality 18:621-32. 2006..Assignment of the absolute configuration of the separated enantiomers is empirically established by comparing their chiroptical data with those of structurally related Mianserin... - High-performance liquid chromatography separation of enantiomers of flavanone and 2'-hydroxychalcone under reversed-phase conditionsRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy
J Chromatogr A 1190:95-101. 2008..It was clearly demonstrated that the 2'-hydroxychalcone was involved as intermediate in the on-column and off-column enantiomerization process of flavanone... - Analytical and semipreparative high performance liquid chromatography enantioseparation of new substituted 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)-pyrazoles on polysaccharide-based chiral stationary phases in normal-phase, polar organic and reversed-pR Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy
J Chromatogr A 1101:198-203. 2006..Due to its bonded nature, it was successfully employed at analytical and semipreparative scale in combination with normal-phase eluents containing "non-standards" solvents such as acetone... - Enantioseparation of kavain on Chiralpak IA under normal-phase, polar organic and reversed-phase conditionsRoberto Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanita, Rome, Italy
J Sep Sci 31:2206-10. 2008..A water-dependent enantioselectivity was clearly demonstrated. Performance of the Chiralpak IA CSP in polar organic and RP conditions was compared with that of five coated polysaccharide-derived CSPs used in normal-phase mode... - Chiral HPLC separation and absolute configuration of novel S-DABO derivativesRoberto Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanita, Rome, Italy
Chirality 21:604-12. 2009..The results of this study indicated a correlation between the absolute configuration at C-1 of alkyl side chain of the dihydropyrimidinone structure and the sign of the CD band at around 245 nm... - Semipreparative HPLC enantioseparation, chiroptical properties, and absolute configuration of two novel cyclooxygenase-2 inhibitorsRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Rome, Italy
Chirality 22:56-62. 2010..The absolute configuration of both compounds was unequivocally established by single-crystal X-ray diffraction method and correlated to the chiroptical properties of isolated enantiomers... - A new application of stopped-flow chiral HPLC: inversion of enantiomer elution orderR Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanita, Rome, Italy
J Chromatogr A 1061:27-34. 2004..This procedure may be applied to each enantiomer pair that is separated by chiral HPLC under an appreciable enthalpy-control... - Perturbing effects of chiral stationary phase on enantiomerization second-order rate constants determined by enantioselective dynamic high-performance liquid chromatography: a practical tool to quantify the accessible acid and basic catalytic sites bondedRoberto Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanita, Viale Regina Elena 299, I 00161 Rome, Italy
Anal Chem 81:3560-70. 2009..Such an approach might be of general application, supplying a useful way to characterize the attitude of SPs to speed acid- or base-catalyzed equilibria possibly active during chromatographic separations... - Unusually high enantioselectivity in high-performance liquid chromatography using cellulose tris(4-methylbenzoate) as a chiral stationary phaseRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Rome, Italy
J Chromatogr A 1216:4673-8. 2009.... - Enantioselective liquid chromatography of C3-chiral 2,3-dihydro-1,2,5-benzothiadiazepin-4(5H)-one and thione 1,1-dioxides on polyacrylamide- and polysaccharide-based chiral stationary phasesR Cirilli
Laboratorio di Chimica del Farmaco, Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Rome, Italy
J Chromatogr A 993:17-28. 2003..The assignment of the absolute configuration was empirically established by comparing the CD spectra of the separated enantiomers with those obtained from structural analogues... - Enantioselective HPLC combined with spectroscopic methods: a valid strategy to determine the absolute configuration of potential beta-secretase inhibitorsRoberto Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Rome, Italy
Talanta 82:1306-12. 2010..The results from the NMR/CD study fully correlated the configurational assignment obtained by a second approach involving single crystal X-ray diffraction... - High-performance liquid chromatographic separation of enantiomers and diastereomers of 2-methylcyclohexanone thiosemicarbazone, and determination of absolute configuration and configurational stabilityR Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy
J Chromatogr A 1172:160-9. 2007..The findings obtained by chromatographic and kinetic experiments were used to develop a simple method to convert the racemic form of 2-MCET into a single enantiomer... - Conformational and temperature effects on separation of stereoisomers of a C3,C4-substituted beta-lactamic cholesterol absorption inhibitor on amylose-based chiral stationary phasesR Cirilli
, Laboratorio di Chimica del Farmaco, Rome, Italy
J Chromatogr A 923:27-36. 2001..Thermodynamic parameters associated with adsorption equilibria between acyclic and cyclic stereoisomers and CSPs were calculated from chromatographic runs at various temperatures... - Comparative study between the polysaccharide-based chiralcel OJ and chiralcel OD CSPSs in chromatographic enantioseparation of imidazole analogues of fluoxetine and miconazoleRoberto Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanit, Viale Regina Elena 299, 1-00161 Roma, Italy
J Sep Sci 28:627-34. 2005..Assignment of the absolute configuration was empirically established by comparing the CD spectra of the separated enantiomers with those obtained from the enantiomers of Miconazole... - Analytical and semipreparative high performance liquid chromatography separation of stereoisomers of novel 3,4-dihydropyrimidin-4(3H)-one derivatives on the immobilised amylose-based Chiralpak IA chiral stationary phaseRoberto Cirilli
Dipartimento del Farmaco, Istituto Superiore di Sanit, Roma, Italy
J Sep Sci 29:1399-406. 2006..In order to study the chiroptical properties of single stereoisomers, mg-scale separations were performed on analytical and semipreparative size Chiralpak IA columns in combination with ethyl acetate-based eluents... - Enantiomers of C(5)-chiral 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives: Analytical and semipreparative HPLC separation, chiroptical properties, absolute configuration, and inhibitory activity against monoamine oxidaseRoberto Cirilli
Istituto Superiore di Sanit, Dipartimento del Farmaco, Rome, Italy
Chirality 16:625-36. 2004..The inhibitory activity against MAO of racemic samples and single enantiomers were evaluated in vitro... - Analytical and semipreparative enantiomeric separation of azole antifungal agents by high-performance liquid chromatography on polysaccharide-based chiral stationary phases. Application to in vitro biological studiesR Cirilli
Istituto Superiore di Sanit, Laboratorio di Chimica del Farmaco, Rome, Italy
J Chromatogr A 942:107-14. 2002..The influence of the nature and content of an alcoholic modifier in the mobile phase was studied. The isolated enantiomers, separated on semipreparative columns, were submitted to in vitro biological investigations... - A rational approach to predict and modulate stereolability of chiral alpha substituted ketonesRoberto Cirilli
Istituto Superiore di Sanita, Dipartimento del Farmaco, Rome, Italy
Chirality 21:24-34. 2009..The possibility to extend easily the procedure to other classes of C-H acids appears of interest... - Direct HPLC enantioseparation of omeprazole and its chiral impurities: application to the determination of enantiomeric purity of esomeprazole magnesium trihydrateLeo Zanitti
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, I 00161 Rome, Italy
J Pharm Biomed Anal 52:665-71. 2010..5-25 microg/ml for (R)-enantiomer was obtained. The limits of detection and quantification were 99 and 333 ng/ml, respectively. The intra and inter-day assay precision was less than 2% (RSD%)... - Development and validation of an enantioselective and chemoselective HPLC method using a Chiralpak IA column to simultaneously quantify (R)-(+)- and (S)-(-)-lansoprazole enantiomers and related impuritiesRoberto Cirilli
Department of Therapeutic Research and Medicines Evaluation, Istituto Superiore di Sanita, Rome, Italy
J Pharm Biomed Anal 50:9-14. 2009..55-1.24 and 0.66-1.19% in terms of retention times and area response RSD% for (R)-(+)- and (S)-(-)-lansoprazole, respectively. The method was also able to resolve impurities from the enantiomers of lansoprazole... - Direct high-performance liquid chromatography enantioseparation of terazosin on an immobilised polysaccharide-based chiral stationary phase under polar organic and reversed-phase conditionsRosella Ferretti
Istituto Superiore di Sanita, Dipartimento del Farmaco, Viale Regina Elena 299, I 00161 Rome, Italy
J Chromatogr A 1216:5385-90. 2009..The absolute configuration of TER enantiomers was assigned by comparison of the measured specific rotations with those reported in the literature... - Synthesis and pharmacological characterization of chiral pyrrolidinylfuran derivatives: the discovery of new functionally selective muscarinic agonistsSerena Scapecchi
Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
J Med Chem 51:3905-12. 2008.... - Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-(1H)- pyrazole derivativesFranco Chimenti
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, , P.le A. Moro 5, 00185 Rome, Italy
J Med Chem 48:7113-22. 2005..The docking study was carried out using several computational approaches with the aim of proposing possible binding modes of the MAO enantioselective compounds 1 and 4... - Synthesis and selective inhibitory activity of 1-acetyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives against monoamine oxidaseFranco Chimenti
Dipartimento di Studi di Chimica e Tossicologia delle Sostanze Biologicamente Attive, , Piazzale A. Moro 5, 00185 Rome, Italy
J Med Chem 47:2071-4. 2004..The (-)-6 enantiomer shows K(i(MAO-A)) = 2 nM and SI = 165 000, (+)-6 shows K(i(MAO-A)) = 6 nM and SI = 166 666, (-)-11 shows K(i(MAO-A)) = 4 nM and SI = 80 000, and (+)-11 shows K(i(MAO-A)) = 7 nM and SI = 38 571... - Design, synthesis, and biological activities of pyrrolylethanoneamine derivatives, a novel class of monoamine oxidases inhibitorsRoberto Di Santo
Istituto Pasteur Fondazione Cenci Bolognetti, Dipartimento di Studi Farmaceutici Dip 63, Universita di Roma La Sapienza, Piazzale A Moro 5, I 00185 Roma, Italy
J Med Chem 48:4220-3. 2005..Interestingly, amino alcohol 25 selectively inhibited MAO-B enzyme and could be a lead compound for designing more potent and selective MAO-B inhibitors... - Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agentsMariangela Biava
Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro, 5, I 00185 Roma, Italy
Bioorg Med Chem 16:8072-81. 2008..The affinity data have been rationalized through docking simulations... - Synthesis, stereochemical identification, and selective inhibitory activity against human monoamine oxidase-B of 2-methylcyclohexylidene-(4-arylthiazol-2-yl)hydrazonesFranco Chimenti
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita degli Studi di Roma La Sapienza, P le A Moro 5, 00185 Roma, Italy
J Med Chem 51:4874-80. 2008..A computational study was performed by molecular mechanics, DFT-based quantomechanics, and docking techniques on the most active and human MAO-B selective inhibitor 8... - Chiral resolution and binding study of 1,3,4,14b-tetrahydro-2,10-dimethyl-2H,10H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzotriazepine (10-methyl-10-azaaptazepine) and 2-methyl-1,3,4,14b-tetrahydro-2H-pyrazino[2,1-d]pyrrolo[1,2-b] [1,2,5]benzothiadiazepineGabriella De Martino
Dipartimento di Studi Farmaceutici, , Piazzale A. Moro 5, I-00185 Roma, Italy
Farmaco 60:931-7. 2005..Compound (+)-(S)-5 showed an interesting pharmacological profile different from those of the reference compounds mirtazepine, mianserin and 6-methoxymianserin... - 1-[(3-Aryloxy-3-aryl)propyl]-1H-imidazoles, new imidazoles with potent activity against Candida albicans and dermatophytes. Synthesis, structure-activity relationship, and molecular modeling studiesGiuseppe La Regina
Dipartimento di Studi Farmaceutici, Istituto Pasteur Fondazione Cenci Bolognetti, Sapienza Universita di Roma, Piazzale Aldo Moro 5, I 00185 Roma, Italy
J Med Chem 51:3841-55. 2008..SARs of imidazoles 10- 44 were rationalized with reasonable accuracy by a previously developed quantitative pharmacophore for antifungal agents... - Synthesis, biological evaluation and 3D-QSAR of 1,3,5-trisubstituted-4,5-dihydro-(1H)-pyrazole derivatives as potent and highly selective monoamine oxidase A inhibitorsFranco Chimenti
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita degli Studi di Roma La Sapienza, Piazzale Aldo Moro 5, 00185 Rome, Italy
Curr Med Chem 13:1411-28. 2006.... - Synthesis and cerebral uptake of 1-(1-[(11)C]methyl-1H-pyrrol-2-yl)-2-phenyl-2-(1-pyrrolidinyl)ethanone, a novel tracer for positron emission tomography studies of monoamine oxidase type ASvend Borup Jensen
PET Centre, Aarhus University Hospital, Nørrebrogade 44, Arhus C, Denmark
J Med Chem 51:1617-22. 2008..Its binding was highly vulnerable to MAO blockade, suggesting a binding potential as high as 2 for MAO-A sites. The slow plasma metabolism of 4 and 5 may present advantages over [ (11)C]harmine for routine PET studies of MAO-A...