(1) Ammazzalorso, A.; D’Angelo, A.; Giancristofaro, A.; De Filippis, B.; Di Matteo, M.; Fantacuzzi, M.; Giampietro, L.; Linciano, P.; Maccallini, C.; Amoroso, R. Fibrate-Derived N-(Methylsulfonyl)Amides with Antagonistic Properties on PPARα. Eur. J. Med. Chem. 2012, 58, 317–322. https://doi.org/10.1016/j.ejmech.2012.10.019.
(2) Giampietro, L.; D’Angelo, A.; Giancristofaro, A.; Ammazzalorso, A.; De Filippis, B.; Fantacuzzi, M.; Linciano, P.; Maccallini, C.; Amoroso, R. Synthesis and Structure-Activity Relationships of Fibrate-Based Analogues inside PPARs. Bioorganic Med. Chem. Lett. 2012, 22 (24), 7662–7666. https://doi.org/10.1016/j.bmcl.2012.09.111.
(3) Linciano, P.; Pizzetti, M.; Porcheddu, A. Use of Primary Amines for the Selective N-Alkylation of Anilines by a Reusab- Le Heterogeneous Catalyst. Synlett 2013, 24, 2249–2254. https://doi.org/10.1055/s-0033-1339667.
(4) Giampietro, L.; D’Angelo, A.; Giancristofaro, A.; Ammazzalorso, A.; De Filippis, B.; Di Matteo, M.; Fantacuzzi, M.; Linciano, P.; Maccallini, C.; Amoroso, R. Effect of Stilbene and Chalcone Scaffolds Incorporation in Clofibric Acid on PPARα Agonistic Activity. Med. Chem. 2014, 10 (1), 59–65.
(5) De Filippis, B.; Linciano, P.; Ammazzalorso, A.; Di Giovanni, C.; Fantacuzzi, M.; Giampietro, L.; Laghezza, A.; Maccallini, C.; Tortorella, P.; Lavecchia, A.; et al. Structural Development Studies of PPARs Ligands Based on Tyrosine Scaffold. Eur. J. Med. Chem. 2015, 89, 817–825. https://doi.org/10.1016/j.ejmech.2014.10.083.
(6) Quotadamo, A.; Linciano, P.; Davoli, P.; Tondi, D.; Costi, M. P.; Venturelli, A. An Improved Synthesis of CENTA, a Chromogenic Substrate for β-Lactamases. Synlett 2016, 27 (17), 2447–2450. https://doi.org/10.1055/s-0035-1562454.
(7) Linciano, P.; Ammazzalorso, A.; De Filippis, B.; Fantacuzzi, M.; Giampietro, L.; Maccallini, C.; Amoroso, R. Geometric Isomerism of an Acetamidino Derivative Determined by NMR Investigations. ChemistrySelect 2017, 2 (30), 9706–9710. https://doi.org/10.1002/slct.201701646.
(8) Borsari, C.; Santarem, N.; Torrado, J.; Olías, A. I.; Corral, M. J.; Baptista, C.; Gul, S.; Wolf, M.; Kuzikov, M.; Ellinger, B.; Linciano, P.; et al. Methoxylated 2’-Hydroxychalcones as Antiparasitic Hit Compounds. Eur. J. Med. Chem. 2017, 126, 1129–1135. https://doi.org/10.1016/j.ejmech.2016.12.017.
(9) Linciano, P.; Dawson, A.; Pöhner, I.; Costa, D. M.; Sa, M. S.; Cordeiro-Da-Silva, A.; Luciani, R.; Gul, S.; Witt, G.; Ellinger, B.; et al. Exploiting the 2‑Amino-1,3,4-Thiadiazole Scaffold to Inhibit Trypanosoma Brucei Pteridine Reductase in Support of Early-Stage Drug Discovery. ACS Omega 2017, 2 (9), 5666–5683. https://doi.org/10.1021/acsomega.7b00473.
(10) Linciano, P.; Moraes, C. B.; Alcantara, L. M.; Franco, C. H.; Pascoalino, B.; Freitas-Junior, L. H.; Macedo, S.; Santarem, N.; Cordeiro-da-Silva, A.; Gul, S.; et al. Aryl Thiosemicarbazones for the Treatment of Trypanosomatidic Infections. Eur. J. Med. Chem. 2018, 146, 423–434. https://doi.org/10.1016/j.ejmech.2018.01.043.
(11) Celenza, G.; Vicario, M.; Bellio, P.; Linciano, P.; Perilli, M.; Oliver, A.; Blazquez, J.; Cendron, L.; Tondi, D. Phenylboronic Acid Derivatives as Validated Leads Active in Clinical Strains Overexpressing KPC-2: A Step against Bacterial Resistance. ChemMedChem 2018. https://doi.org/10.1002/cmdc.201700788.
(12) Klein, R.; Linciano, P.; Celenza, G.; Bellio, P.; Papaioannou, S.; Blazquez, J.; Cendron, L.; Brenk, R.; Tondi, D. In Silico Identification and Experimental Validation of Hits Active against KPC-2 β-Lactamase. PLoS One 2018, 13 (11), 1–22. https://doi.org/10.1371/journal.pone.0203241.
(13) Franchini, S.; Sorbi, C.; Linciano, P.; Brasili, L.; Tait, A. Effect of the Rigidification of Propranolol, a Mixed Beta-Adrenoceptor and 5-HT1AR Antagonist. Pharmazie 2019, 74 (3), 131–135. https://doi.org/10.1691/ph.2019.8878.
(14) Landi, G.; Linciano, P.; Borsari, C.; Bertolacini, C. P.; Moraes, C. B.; Cordeiro-Da-Silva, A.; Gul, S.; Witt, G.; Kuzikov, M.; Costi, M. P.; et al. Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma Brucei Pteridine-Reductase-1 Inhibitors. ACS Infect. Dis. 2019, 5, 1105–1114. https://doi.org/10.1021/acsinfecdis.8b00358.
(15) Citti, C.; Linciano, P.; Panseri, S.; Vezzalini, F.; Forni, F.; Vandelli, M. A.; Cannazza, G. Cannabinoid Profiling of Hemp Seed Oil by Liquid Chromatography Coupled to High-Resolution Mass Spectrometry. Front. Plant Sci. 2019, 10 (February), 1–17. https://doi.org/10.3389/fpls.2019.00120.
(16) Spyrakis, F.; Bellio, P.; Quotadamo, A.; Linciano, P.; Benedetti, P.; D’Arrigo, G.; Baroni, M.; Cendron, L.; Celenza, G.; Tondi, D. First Virtual Screening and Experimental Validation of Inhibitors Targeting GES-5 Carbapenemase. J. Comput. Aided. Mol. Des. 2019, 33 (2), 295–305. https://doi.org/10.1007/s10822-018-0182-2.
(17) Moraes, C. B.; Witt, G.; Kuzikov, M.; Ellinger, B.; Calogeropoulou, T.; Prousis, K. C.; Mangani, S.; Di Pisa, F.; Landi, G.; Iacono, L. Dello; Linciano, P. et al. Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform. SLAS Discov. Adv. Life Sci. R&D 2019, 24 (3), 346–361. https://doi.org/10.1177/2472555218823171.
(18) Quotadamo, A.; Linciano, P.; Costi, M. P.; Venturelli, A. Optimization of N ‐alkylation in the Synthesis of Methotrexate and Pteridine‐based Derivatives Under Microwave‐Irradiation. ChemistrySelect 2019, 4 (15), 4429–4433. https://doi.org/10.1002/slct.201900721.
(19) Linciano, P.*; Pozzi, C.; Iacono, L. Dello; Di Pisa, F.; Landi, G.; Bonucci, A.; Gul, S.; Kuzikov, M.; Ellinger, B.; Witt, G.; et al. Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections. J. Med. Chem. 2019, 62 (8), 3989–4012. https://doi.org/10.1021/acs.jmedchem.8b02021.
(20) Franchini, S.; Sorbi, C.; Linciano, P.; Carnevale, G.; Tait, A.; Ronsisvalle, S.; Buccioni, M.; Del Bello, F.; Cilia, A.; Pirona, L.; et al. 1,3-Dioxane as a Scaffold for Potent and Selective 5-HT 1A R Agonist with in-Vivo Anxiolytic, Anti-Depressant and Anti-Nociceptive Activity. Eur. J. Med. Chem. 2019, 176, 310–325. https://doi.org/10.1016/j.ejmech.2019.05.024.
(21) Linciano, P.; Cendron, L.; Gianquinto, E.; Spyrakis, F.; Tondi, D. Ten Years with New Delhi Metallo-β-Lactamase-1 (NDM-1): From Structural Insights to Inhibitor Design. ACS Infect. Dis. 2019, 5 (1), 9–34. https://doi.org/10.1021/acsinfecdis.8b00247.
(22) Vanossi, D.; Casell, M.; Pavesi, G.; Borsari, C.; Linciano, P.; Costi, M. P.; Ponterini, G. Excited-State Intramolecular Proton Transfer in a Bioactive Flavonoid Provides Fluorescence Observables for Recognizing Its Engagement with Target Proteins. Photochem. Photobiol. Sci. 2019. https://doi.org/10.5860/choice.51-2070.
(23) Citti, C.; Linciano, P. (co-first); Forni, F.; Vandelli, M. A.; Gigli, G.; Laganà, A.; Cannazza, G. Analysis of Impurities of Cannabidiol from Hemp. Isolation, Characterization and Synthesis of Cannabidibutol, the Novel Cannabidiol Butyl Analog. J. Pharm. Biomed. Anal. 2019. https://doi.org/10.1016/j.jpba.2019.06.049.
(24) Linciano, P.; De Filippis, B.; Ammazzalorso, A.; Amoia, P.; Fantacuzzi, M.; Giampietro, L.; Maccallini, C.; Petit, C.; Amoroso, R. Druggability Profile of Stilbene-Derived PPAR Agonists : Determination of Physicochemical Properties and PAMPA Druggability Profile of Stilbene-Derived PPAR Agonists : Determination of Physicochemical Properties and PAMPA Study. Medchemcomm 2019, https://doi.org/10.1039/C9MD00286C.
(25) Borsari, C.; Jiménez-antón, M. D.; Eick, J.; Bifeld, E.; José, J.; Olías-molero, A. I.; Corral, M. J.; Santarem, N.; Severi, L.; Gul, S.; Linciano, P. et al. Discovery of a Benzothiophene-Flavonol Halting Miltefosine and Antimonial Drug Resistance in Leishmania Parasites through the Application of Medicinal Chemistry, Screening and Genomics. Eur. J. Med. Chem. 2019, 111676, https://doi.org/10.1016/j.ejmech.2019.111676.
(26) Citti, C.; Linciano, P. (co-first); Forni, F.; Vandelli, M. A.; Gigli, G.; Laganà, A.; Cannazza, G. Chemical and Spectroscopic Characterization Data of ‘Cannabidibutol’, a Novel Cannabidiol Butyl Analog. Data Br. 2019, 104463, https://doi.org/10.1016/j.dib.2019.104463.
(27) Linciano, P.; Vicario, M.; Kekez, I.; Bellio, P.; Celenza, G.; Martin-Blecua, I.; Blazquez, J.; Cendron, L.; Tondi, D. Phenyl boronic acids probing molecular recognition 3 against class A and class C β-lactamases. Antibiotics, 2019, 8 (4), art. no. 171. DOI: 10.3390/antibiotics804017.
(28) Linciano, P.; Cullia, G.; Borsari, C.; Santucci, M.; Ferrari, S.; Witt, G.; Gul, S.; Santarem, N.; Cordeiro da Silva, A.; et al. Trypanosoma brucei screening fishes out a 2,4-diaminopyrimidine scaffold targeting pteridine reductase 1 from the LIBRA compound library HTS campaign. Eur. J. Med. Chem. 2019, 189, art. No. 112047.DOI: 10.1016/j.ejmech.2020.112047.
(29) Pacifico, S.; Santucci, M.; Luciani, R.; Saxena P.; Linciano, P.; Ponterini, G.; D’Arca, D.; Marverti, G.; Guerrini, R.; Costi, M. P. Cyclic peptides acting as allosteric inhibitors of human thymidylate synthase and cancer cell growth. Molecules. 2019, 24 (19), art. no. 3493. DOI: 10.3390/molecules24193493.
(30) Linciano, P.; Citti, C.; Luongo, L.; Belardo, C.; Vandelli, M.A.; Forni, F.; Gigli, G.; Laganà, A.; Montone, C; Cannazza, C.; Isolation of a high affinity cannabinoid for human CB1 receptor from a medicinal cannabis variety: tetrahydrocannabutol, the butyl analog of tetrahydrocannabinol. Journal of Natural Products. 2019. 175, art. no. 112752. DOI: 10.1016/j.jpba.2019.06.049.
(31) Citti, C., Linciano, P. (co-first), Russo, F., Luongo, L., Iannotta, M., Maione, S., Laganà, A., Capriotti, A.L., Forni, F., Vandelli, M.A., Gigli, G., Cannazza, G. A novel phytocannabinoid isolated from Cannabis sativa L. with an in vivo cannabimimetic activity higher than Δ9-tetrahydrocannabinol: Δ9-Tetrahydrocannabiphorol. Scientific Reports. 2019, 9 (1), art. no. 20335. DOI: 10.1038/s41598-019-56785-1.
(32) Linciano, P., Gianquinto, E., Montanari, M., Maso, L., Bellio, P., Cebrián-Sastre, E., Celenza, G., Blázquez, J., Cendron, L., Spyrakis, F., Tondi, D. 4-amino-1,2,4-triazole-3-thione as a promising scaffold for the inhibition of serine and metallo-β-lactamases. Pharmaceuticals. 2020, 13 (3), art. no. 52. DOI: 10.3390/ph13030052.
(33) Citti, C., Linciano, P., Cannazza, G. Is cannabidiol a scheduled controlled substance? Origin makes the difference. Drug Discovery Today. 2020, 25 (4), pp. 628-632. DOI: 10.1016/j.drudis.2020.02.001.
(34) Franchini, S., Linciano, P., Puja, G., Tait, A., Borsari, C., Denora, N., Iacobazzi, R.M., Brasili, L., Sorbi, C. Novel Dithiolane-Based Ligands Combining Sigma and NMDA Receptor Interactions as Potential Neuroprotective Agents. ACS Medicinal Chemistry Letters. 2020, 11 (5), pp. 1028-1034. DOI: 10.1021/acsmedchemlett.0c00129.
(35) Landi, G., Linciano, P., Tassone, G., Costi, M.P., Mangani, S., Pozzi, C. High-resolution crystal structure of Trypanosoma brucei pteridine reductase 1 in complex with an innovative tricyclic-based inhibitor. Acta Crystallographica Section D: Structural Biology. 2020, 76, pp. 558-564. DOI: 10.1107/S2059798320004891.
(36) Linciano, P., Rossino, G., Listro, R., Rossi, D., Collina, S. The sigma-1 receptor antagonists, promising players in fighting neuropathic pain. Pharmaceutical Patent Analysis. 2020, DOI: 10.4155/ppa-2020-0007.
(37) Citti, C., Russo, F., Linciano, P., Strallhofer, S.S., Tolomeo, F., Forni, F., Vandelli, M.A., Gigli, G., Cannazza, G. Origin of D9-Tetrahydrocannabinol Impurity in Synthetic Cannabidiol. Cannabis and Cannabinoids Research. 2020, DOI: 10.1089/can.2020.0021.
(38) Rossino, G., Rui, M., Pozzetti, L., Schepmann, D., Wünsch, B., Zambieri, D, Pellavio, G., Laforenza, U., Rinaldi, S., Colombo, G., Morelli, L., Linciano, P., Rossi, D., Collina, S. Setup and Validation of a Reliable Docking Protocol for the Development of Neuroprotective Agents by Targeting the Sigma-1 Receptor (S1R). Int. J. Mol. Sci. 2020. Just accepted.