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Volume 14
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10.3390/ECMC2022-13445
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Abstract

Pyridazin-3(2H)-one as New FABP4 Inhibitors Suggested by Molecular Growing Experiments †

by
Giuseppe Floresta
1,*,
Letizia Crocetti
2,
Chiara Zagni
1 and
Agostino Cilibrizzi
3,*
1
Dipartimento di Scienze del Farmaco e della Salute, Università di Catania, Viale A. Doria 6, 95125 Catania, Italy
2
Dipartimento NEUROFARBA—Pharmaceutical and Nutraceutical Section, via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
3
Institute of Pharmaceutical Science, King’s College London, Stamford Street, London SE1 9NH, UK
*
Authors to whom correspondence should be addressed.
†
Presented at the 8th International Electronic Conference on Medicinal Chemistry, 1–30 November 2022; Available online: https://ecmc2022.sciforum.net/.
Med. Sci. Forum 2022, 14(1), 19; https://doi.org/10.3390/ECMC2022-13445
Published: 1 November 2022
(This article belongs to the Proceedings of The 8th International Electronic Conference on Medicinal Chemistry)
Versions Notes

Abstract

:
The therapeutic potential of fatty acid binding protein 4 (FABP4) is widely acknowledged. Currently, there are numerous clinical studies that indicate how fatty acid binding protein 4 inhibitors could be useful in the treatment of various diseases. To identify new and more potent inhibitors, we utilized a two-step computational approach to design novel structures. Through the use of this approach, we were able to identify a new class of FABP4 inhibitors (FABP4i IC50 2.97 to 23.18 µM) that are capable of inhibiting the activity of FABP4 as low as Arachidonic acid (FABP4i IC50 3.42 ± 0.54 µM). In this study, we present the detailed structural and biological evaluation, and the synthetic procedures of the new pyridazinone-based scaffold FABP4i.

Supplementary Materials

The following are available online at https://www.mdpi.com/article/10.3390/ECMC2022-13445/s1.

Author Contributions

Conceptualization, L.C., G.F. and A.C.; methodology, L.C., G.F.; software, G.F. and C.Z.; formal analysis, L.C., G.F. and A.C.; resources, G.F., C.Z., A.C.; data curation, L.C., G.F.; writing—original draft preparation, L.C., G.F., C.Z.; writing—review and editing, L.C., G.F., A.C.; supervision, A.C.; project administration. All authors have read and agreed to the published version of the manuscript.

Funding

This research received no external funding.

Institutional Review Board Statement

Not applicable.

Informed Consent Statement

Not applicable.

Data Availability Statement

Not applicable.

Conflicts of Interest

The authors declare no conflict of interest.
Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations.

Share and Cite

MDPI and ACS Style

Floresta, G.; Crocetti, L.; Zagni, C.; Cilibrizzi, A. Pyridazin-3(2H)-one as New FABP4 Inhibitors Suggested by Molecular Growing Experiments. Med. Sci. Forum 2022, 14, 19. https://doi.org/10.3390/ECMC2022-13445

AMA Style

Floresta G, Crocetti L, Zagni C, Cilibrizzi A. Pyridazin-3(2H)-one as New FABP4 Inhibitors Suggested by Molecular Growing Experiments. Medical Sciences Forum. 2022; 14(1):19. https://doi.org/10.3390/ECMC2022-13445

Chicago/Turabian Style

Floresta, Giuseppe, Letizia Crocetti, Chiara Zagni, and Agostino Cilibrizzi. 2022. "Pyridazin-3(2H)-one as New FABP4 Inhibitors Suggested by Molecular Growing Experiments" Medical Sciences Forum 14, no. 1: 19. https://doi.org/10.3390/ECMC2022-13445

APA Style

Floresta, G., Crocetti, L., Zagni, C., & Cilibrizzi, A. (2022). Pyridazin-3(2H)-one as New FABP4 Inhibitors Suggested by Molecular Growing Experiments. Medical Sciences Forum, 14(1), 19. https://doi.org/10.3390/ECMC2022-13445

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