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Expanding the knowledge around antitubercular 5-(2-aminothiazol-4-yl)isoxazole-3-carboxamides: Hit-to-lead optimization and release of a novel antitubercular chemotype via scaffold derivatization.
Girardini M, Ferlenghi F, Annunziato G, Degiacomi G, Papotti B, Marchi C, Sammartino JC, Rasheed SS, Contini A, Pasca MR, Vacondio F, Evans JC, Dick T, Müller R, Costantino G, Pieroni M. Girardini M, et al. Among authors: ferlenghi f. Eur J Med Chem. 2023 Jan 5;245(Pt 2):114916. doi: 10.1016/j.ejmech.2022.114916. Epub 2022 Nov 11. Eur J Med Chem. 2023. PMID: 36399878 Free PMC article.
Inhibition of Eph/ephrin interaction with the small molecule UniPR500 improves glucose tolerance in healthy and insulin-resistant mice.
Giorgio C, Incerti M, Pala D, Russo S, Chiodelli P, Rusnati M, Cantoni AM, Di Lecce R, Barocelli E, Bertoni S, Ravassard P, Manenti F, Piemonti L, Ferlenghi F, Lodola A, Tognolini M. Giorgio C, et al. Among authors: ferlenghi f. Pharmacol Res. 2019 Mar;141:319-330. doi: 10.1016/j.phrs.2019.01.011. Epub 2019 Jan 6. Pharmacol Res. 2019. PMID: 30625359
Balancing reactivity and antitumor activity: heteroarylthioacetamide derivatives as potent and time-dependent inhibitors of EGFR.
Castelli R, Bozza N, Cavazzoni A, Bonelli M, Vacondio F, Ferlenghi F, Callegari D, Silva C, Rivara S, Lodola A, Digiacomo G, Fumarola C, Alfieri R, Petronini PG, Mor M. Castelli R, et al. Among authors: ferlenghi f. Eur J Med Chem. 2019 Jan 15;162:507-524. doi: 10.1016/j.ejmech.2018.11.029. Epub 2018 Nov 13. Eur J Med Chem. 2019. PMID: 30472599
Benzisothiazolinone Derivatives as Potent Allosteric Monoacylglycerol Lipase Inhibitors That Functionally Mimic Sulfenylation of Regulatory Cysteines.
Castelli R, Scalvini L, Vacondio F, Lodola A, Anselmi M, Vezzosi S, Carmi C, Bassi M, Ferlenghi F, Rivara S, Møller IR, Rand KD, Daglian J, Wei D, Dotsey EY, Ahmed F, Jung KM, Stella N, Singh S, Mor M, Piomelli D. Castelli R, et al. Among authors: ferlenghi f. J Med Chem. 2020 Feb 13;63(3):1261-1280. doi: 10.1021/acs.jmedchem.9b01679. Epub 2019 Dec 2. J Med Chem. 2020. PMID: 31714779
Optimization of EphA2 antagonists based on a lithocholic acid core led to the identification of UniPR505, a new 3α-carbamoyloxy derivative with antiangiogenetic properties.
Incerti M, Russo S, Corrado M, Giorgio C, Ballabeni V, Chiodelli P, Rusnati M, Scalvini L, Callegari D, Castelli R, Vacondio F, Ferlenghi F, Tognolini M, Lodola A. Incerti M, et al. Among authors: ferlenghi f. Eur J Med Chem. 2020 Mar 1;189:112083. doi: 10.1016/j.ejmech.2020.112083. Epub 2020 Jan 22. Eur J Med Chem. 2020. PMID: 32000051
Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Derivatives with Antiosteoarthritic Activity In Vivo.
Mugnaini C, Kostrzewa M, Bryk M, Mahmoud AM, Brizzi A, Lamponi S, Giorgi G, Ferlenghi F, Vacondio F, Maccioni P, Colombo G, Mor M, Starowicz K, Di Marzo V, Ligresti A, Corelli F. Mugnaini C, et al. Among authors: ferlenghi f. J Med Chem. 2020 Jul 9;63(13):7369-7391. doi: 10.1021/acs.jmedchem.0c00595. Epub 2020 Jun 22. J Med Chem. 2020. PMID: 32515588
The GABAB receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives.
Ferlenghi F, Maccioni P, Mugnaini C, Brizzi A, Fara F, Mostallino R, Castelli MP, Colombo G, Mor M, Vacondio F, Corelli F. Ferlenghi F, et al. Eur J Pharm Sci. 2020 Dec 1;155:105544. doi: 10.1016/j.ejps.2020.105544. Epub 2020 Sep 12. Eur J Pharm Sci. 2020. PMID: 32927068
Correction to Design, Synthesis, and Physicochemical and Pharmacological Profiling of 7-Hydroxy-5-oxopyrazolo[4,3-b]pyridine-6-carboxamide Derivatives with Antiosteoarthritic Activity In Vivo.
Mugnaini C, Kostrzewa M, Bryk M, Mahmoud AM, Brizzi A, Lamponi S, Giorgi G, Ferlenghi F, Vacondio F, Maccioni P, Colombo G, Mor M, Starowicz K, Di Marzo V, Ligresti A, Corelli F. Mugnaini C, et al. Among authors: ferlenghi f. J Med Chem. 2020 Oct 8;63(19):11303. doi: 10.1021/acs.jmedchem.0c01567. Epub 2020 Sep 28. J Med Chem. 2020. PMID: 32985883 No abstract available.
25 results