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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 benzofuran analogues that showed promising PDE4B inhibitory activity
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Figure 18: Structure of benzofuran analogues that showed promising PDE4B inhibitory activity

Mentions: One-pot synthesis of benzofuran fused N-heterocycles 39 and 40a–g (Figure 18) has been achieved by AlCl3-mediated C–C followed by C–O bond formation between 2,3-dichloropyrazine or its derivatives and phenols. Synthesized compounds were tested in vitro for their PDE4B inhibitory activity [57]. Compound 39 showed significant PDE4B inhibition at 30 µM in comparison to the reference compound rolipram. Compounds possessing a substituent on the benzofuran moiety showed moderate activities and the presence of a smaller substituent was well-tolerated compared to a larger or bulky group in terms of PDE4 inhibition.


Selective Phosphodiesterase 4B Inhibitors: A Review.

Azam MA, Tripuraneni NS - Sci Pharm (2014)

Structure of benzofuran analogues 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 18: Structure of benzofuran analogues that showed promising PDE4B inhibitory activity
Mentions: One-pot synthesis of benzofuran fused N-heterocycles 39 and 40a–g (Figure 18) has been achieved by AlCl3-mediated C–C followed by C–O bond formation between 2,3-dichloropyrazine or its derivatives and phenols. Synthesized compounds were tested in vitro for their PDE4B inhibitory activity [57]. Compound 39 showed significant PDE4B inhibition at 30 µM in comparison to the reference compound rolipram. Compounds possessing a substituent on the benzofuran moiety showed moderate activities and the presence of a smaller substituent was well-tolerated compared to a larger or bulky group in terms of PDE4 inhibition.

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