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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

Novel series of N-alkylated pyridazinones that have shown selective PDE4B inhibitory activity
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Figure 20: Novel series of N-alkylated pyridazinones that have shown selective PDE4B inhibitory activity

Mentions: Yet in another publication [59], authors explored the effect of N-alkylation of the pyridazinone ring in compound 18 (Figure 8) on PDE4B inhibition and selectivity. N-alkylation of the pyridazinone ring resulted in a marked enhancement of potency against PDE4, but suppressed PDE3 inhibition. Addition of a 6-aryl-4,5-dihydropyridazin-3(2H)-one extension to the N-alkyl group in derivatives 42a–f (Figure 20) facilitated both the enhancement of PDE4-inhibitory activity and the restoration of potent PDE3 inhibition. These modifications of structural changes afforded potent dual PDE3/4 inhibitors and most of the synthesized compound suppressed histamine-induced bronchoconstriction in vivo and exhibited promising anti-inflammatory activity via intratracheal administration.


Selective Phosphodiesterase 4B Inhibitors: A Review.

Azam MA, Tripuraneni NS - Sci Pharm (2014)

Novel series of N-alkylated pyridazinones that have shown selective PDE4B inhibitory activity
© Copyright Policy - open-access
Related In: Results  -  Collection

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

Figure 20: Novel series of N-alkylated pyridazinones that have shown selective PDE4B inhibitory activity
Mentions: Yet in another publication [59], authors explored the effect of N-alkylation of the pyridazinone ring in compound 18 (Figure 8) on PDE4B inhibition and selectivity. N-alkylation of the pyridazinone ring resulted in a marked enhancement of potency against PDE4, but suppressed PDE3 inhibition. Addition of a 6-aryl-4,5-dihydropyridazin-3(2H)-one extension to the N-alkyl group in derivatives 42a–f (Figure 20) facilitated both the enhancement of PDE4-inhibitory activity and the restoration of potent PDE3 inhibition. These modifications of structural changes afforded potent dual PDE3/4 inhibitors and most of the synthesized compound suppressed histamine-induced bronchoconstriction in vivo and exhibited promising anti-inflammatory activity via intratracheal administration.

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