TY - JOUR
T1 - PDE4 Inhibitors
T2 - Profiling Hits through the Multitude of Structural Classes
AU - Jin, Jian
AU - Mazzacuva, Francesca
AU - Crocetti, Letizia
AU - Giovannoni, Maria Paola
AU - Cilibrizzi, Agostino
N1 - Publisher Copyright:
© 2023 by the authors.
PY - 2023/7/15
Y1 - 2023/7/15
N2 - Cyclic nucleotide phosphodiesterases 4 (PDE4) are a family of enzymes which specifically promote the hydrolysis and degradation of cAMP. The inhibition of PDE4 enzymes has been widely investigated as a possible alternative strategy for the treatment of a variety of respiratory diseases, including chronic obstructive pulmonary disease and asthma, as well as psoriasis and other autoimmune disorders. In this context, the identification of new molecules as PDE4 inhibitors continues to be an active field of investigation within drug discovery. This review summarizes the medicinal chemistry journey in the design and development of effective PDE4 inhibitors, analyzed through chemical classes and taking into consideration structural aspects and binding properties, as well as inhibitory efficacy, PDE4 selectivity and the potential as therapeutic agents.
AB - Cyclic nucleotide phosphodiesterases 4 (PDE4) are a family of enzymes which specifically promote the hydrolysis and degradation of cAMP. The inhibition of PDE4 enzymes has been widely investigated as a possible alternative strategy for the treatment of a variety of respiratory diseases, including chronic obstructive pulmonary disease and asthma, as well as psoriasis and other autoimmune disorders. In this context, the identification of new molecules as PDE4 inhibitors continues to be an active field of investigation within drug discovery. This review summarizes the medicinal chemistry journey in the design and development of effective PDE4 inhibitors, analyzed through chemical classes and taking into consideration structural aspects and binding properties, as well as inhibitory efficacy, PDE4 selectivity and the potential as therapeutic agents.
KW - dual activity
KW - PDE4 inhibitors
KW - PDE4 selectivity
KW - phosphodiesterases 4
KW - respiratory diseases
KW - structural analysis
UR - http://www.scopus.com/inward/record.url?scp=85166029697&partnerID=8YFLogxK
U2 - 10.3390/ijms241411518
DO - 10.3390/ijms241411518
M3 - Review article
C2 - 37511275
AN - SCOPUS:85166029697
SN - 1661-6596
VL - 24
JO - International Journal of Molecular Sciences
JF - International Journal of Molecular Sciences
IS - 14
M1 - 11518
ER -