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Spacer/Linker based synthesis and biological evaluation of mutual prodrugs as antiinflammatory agents.

Velingkar VS, Jain DR, Ahire DC - Indian J Pharm Sci (2010)

Bottom Line: All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma.Biological activity of title compounds was studied by carrageenan-induced paw edema method.From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Jote Joy Building, Rambhau Salgaonkar Marg, Cuffe parade, Mumbai-400 005, India.

ABSTRACT
Mutual prodrugs of some antiinflammatory agents were synthesized with the aim of improving the therapeutic index through prevention of gastrointestinal complications and to check the efficiency of release of the parent drug in presence of spacer. These mutual prodrugs were synthesized by direct condensation method using dicyclohexyl carbodiimide as a coupling agent and glycine as a spacer. The title compounds were characterized by spectral techniques and the release of the parent drug from mutual prodrug was studied in two different non-enzymatic buffer solutions at pH 1.2, pH 7.4 and in 80% human plasma. All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma. Biological activity of title compounds was studied by carrageenan-induced paw edema method. From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

No MeSH data available.


Related in: MedlinePlus

Naproxen, ibuprofen and ketoprofen mutual prodrugs with paracetamol using glycine as spacer.P= Protecting group, Y= Spacer, TFA= Trifl uoro acetic acid and DCC= Dicyclohexyl carbodimid
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Related In: Results  -  Collection

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Figure 2: Naproxen, ibuprofen and ketoprofen mutual prodrugs with paracetamol using glycine as spacer.P= Protecting group, Y= Spacer, TFA= Trifl uoro acetic acid and DCC= Dicyclohexyl carbodimid


Spacer/Linker based synthesis and biological evaluation of mutual prodrugs as antiinflammatory agents.

Velingkar VS, Jain DR, Ahire DC - Indian J Pharm Sci (2010)

Naproxen, ibuprofen and ketoprofen mutual prodrugs with paracetamol using glycine as spacer.P= Protecting group, Y= Spacer, TFA= Trifl uoro acetic acid and DCC= Dicyclohexyl carbodimid
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC3116311&req=5

Figure 2: Naproxen, ibuprofen and ketoprofen mutual prodrugs with paracetamol using glycine as spacer.P= Protecting group, Y= Spacer, TFA= Trifl uoro acetic acid and DCC= Dicyclohexyl carbodimid
Bottom Line: All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma.Biological activity of title compounds was studied by carrageenan-induced paw edema method.From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Chemistry, Prin. K. M. Kundnani College of Pharmacy, Jote Joy Building, Rambhau Salgaonkar Marg, Cuffe parade, Mumbai-400 005, India.

ABSTRACT
Mutual prodrugs of some antiinflammatory agents were synthesized with the aim of improving the therapeutic index through prevention of gastrointestinal complications and to check the efficiency of release of the parent drug in presence of spacer. These mutual prodrugs were synthesized by direct condensation method using dicyclohexyl carbodiimide as a coupling agent and glycine as a spacer. The title compounds were characterized by spectral techniques and the release of the parent drug from mutual prodrug was studied in two different non-enzymatic buffer solutions at pH 1.2, pH 7.4 and in 80% human plasma. All mutual prodrugs exhibited encouraging hydrolysis profile in 80% human plasma. Biological activity of title compounds was studied by carrageenan-induced paw edema method. From the results obtained, it was concluded that these compounds retain the antiinflammatory action.

No MeSH data available.


Related in: MedlinePlus