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Selective Phosphodiesterase 4B Inhibitors: A Review.

Azam MA, Tripuraneni NS - Sci Pharm (2014)

Bottom Line: Phosphodiesterase 4B has constituted an interesting target for drug development.In recent years, a number of PDE4B inhibitors have been developed for their use as therapeutic agents.In this review, an up-to-date status of the inhibitors investigated for the inhibition of PDE4B has been given so that this rich source of structural information of presently known PDE4B inhibitors could be helpful in generating a selective and potent inhibitor of PDE4B.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, J. S. S. College of Pharmacy, Ootacamund-643001, Tamil Nadu, India.

ABSTRACT
Phosphodiesterase 4B (PDE4B) is a member of the phosphodiesterase family of proteins that plays a critical role in regulating intracellular levels of cyclic adenosine monophosphate (cAMP) by controlling its rate of degradation. It has been demonstrated that this isoform is involved in the orchestra of events which includes inflammation, schizophrenia, cancers, chronic obstructive pulmonary disease, contractility of the myocardium, and psoriatic arthritis. Phosphodiesterase 4B has constituted an interesting target for drug development. In recent years, a number of PDE4B inhibitors have been developed for their use as therapeutic agents. In this review, an up-to-date status of the inhibitors investigated for the inhibition of PDE4B has been given so that this rich source of structural information of presently known PDE4B inhibitors could be helpful in generating a selective and potent inhibitor of PDE4B.

No MeSH data available.


Related in: MedlinePlus

Analogues of 3,5-disubstituted-1,2,4-oxadiazole with promising PDE4B2 inhibitory activity
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Figure 9: Analogues of 3,5-disubstituted-1,2,4-oxadiazole with promising PDE4B2 inhibitory activity

Mentions: A novel series of 3,5-disubstituted-1,2,4-oxadiazoles 20a-g (Figure 9) has been prepared and evaluated for PDE4B2 inhibitory activity [47]. Among the synthesized compounds, 20a exhibited maximum PDE4B2 inhibition (IC50 5.28 lM). A structure-activity relationship study revealed that the substituents 3-cyclopentyloxy-4-methoxyphenyl group at third position and the cyclic ring bearing heteroatoms at fifth position of the 1,2,4-oxadiazole ring are important for activity. The molecular modeling study showed similar interactions of the 3-cyclopentyloxy-4-methoxyphenyl group compared to the piclamilast. However, the heteroatom ring was found to be slightly deviated compared to piclamilast. Compound 20a exhibited significant analgesic and anti-inflammatory activities in the formalin-induced pain in mice and carrageenan-induced paw edema model in rats.


Selective Phosphodiesterase 4B Inhibitors: A Review.

Azam MA, Tripuraneni NS - Sci Pharm (2014)

Analogues of 3,5-disubstituted-1,2,4-oxadiazole with promising PDE4B2 inhibitory activity
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4318138&req=5

Figure 9: Analogues of 3,5-disubstituted-1,2,4-oxadiazole with promising PDE4B2 inhibitory activity
Mentions: A novel series of 3,5-disubstituted-1,2,4-oxadiazoles 20a-g (Figure 9) has been prepared and evaluated for PDE4B2 inhibitory activity [47]. Among the synthesized compounds, 20a exhibited maximum PDE4B2 inhibition (IC50 5.28 lM). A structure-activity relationship study revealed that the substituents 3-cyclopentyloxy-4-methoxyphenyl group at third position and the cyclic ring bearing heteroatoms at fifth position of the 1,2,4-oxadiazole ring are important for activity. The molecular modeling study showed similar interactions of the 3-cyclopentyloxy-4-methoxyphenyl group compared to the piclamilast. However, the heteroatom ring was found to be slightly deviated compared to piclamilast. Compound 20a exhibited significant analgesic and anti-inflammatory activities in the formalin-induced pain in mice and carrageenan-induced paw edema model in rats.

Bottom Line: Phosphodiesterase 4B has constituted an interesting target for drug development.In recent years, a number of PDE4B inhibitors have been developed for their use as therapeutic agents.In this review, an up-to-date status of the inhibitors investigated for the inhibition of PDE4B has been given so that this rich source of structural information of presently known PDE4B inhibitors could be helpful in generating a selective and potent inhibitor of PDE4B.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, J. S. S. College of Pharmacy, Ootacamund-643001, Tamil Nadu, India.

ABSTRACT
Phosphodiesterase 4B (PDE4B) is a member of the phosphodiesterase family of proteins that plays a critical role in regulating intracellular levels of cyclic adenosine monophosphate (cAMP) by controlling its rate of degradation. It has been demonstrated that this isoform is involved in the orchestra of events which includes inflammation, schizophrenia, cancers, chronic obstructive pulmonary disease, contractility of the myocardium, and psoriatic arthritis. Phosphodiesterase 4B has constituted an interesting target for drug development. In recent years, a number of PDE4B inhibitors have been developed for their use as therapeutic agents. In this review, an up-to-date status of the inhibitors investigated for the inhibition of PDE4B has been given so that this rich source of structural information of presently known PDE4B inhibitors could be helpful in generating a selective and potent inhibitor of PDE4B.

No MeSH data available.


Related in: MedlinePlus