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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

Structure of spirooxindole that showed promising PDE4B inhibitory activity
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Figure 17: Structure of spirooxindole that showed promising PDE4B inhibitory activity

Mentions: A novel series of spirooxindoles have been synthesized in the one-pot efficient methodology using Cu-mediated 1,3-dipolar cycloaddition of azomethineylides with dipolarophiles and evaluated for in vitro inhibition of PDE4B [56] using rolipram as a reference compound. The structure-activity relationship study revealed compound 38 (Figure 17) as a potent PDE4B inhibitor with >40% inhibition at 30 µM. In the in silico docking result, compound 38 C=O function showed two hydrogens bonding with His278 and Met347 residues of the active site. Additionally, hydrophobic interactions with the hydrophobic clamp residue of the Q-pocket were also observed.


Selective Phosphodiesterase 4B Inhibitors: A Review.

Azam MA, Tripuraneni NS - Sci Pharm (2014)

Structure of spirooxindole that showed promising PDE4B inhibitory activity
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 17: Structure of spirooxindole that showed promising PDE4B inhibitory activity
Mentions: A novel series of spirooxindoles have been synthesized in the one-pot efficient methodology using Cu-mediated 1,3-dipolar cycloaddition of azomethineylides with dipolarophiles and evaluated for in vitro inhibition of PDE4B [56] using rolipram as a reference compound. The structure-activity relationship study revealed compound 38 (Figure 17) as a potent PDE4B inhibitor with >40% inhibition at 30 µM. In the in silico docking result, compound 38 C=O function showed two hydrogens bonding with His278 and Met347 residues of the active site. Additionally, hydrophobic interactions with the hydrophobic clamp residue of the Q-pocket were also observed.

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