|
NISCAIR ONLINE PERIODICALS REPOSITORY (NOPR) >
NISCAIR PUBLICATIONS >
Research Journals >
Indian Journal of Chemistry -Section B (IJC-B) >
IJC-B Vol.45B [2006] >
IJC-B Vol.45B(04) [April 2006] >
| Title: | Synthesis, biological evaluation and kinetic studies of glyceride prodrugs of biphenyl acetic acid |
| Authors: | Khan, M S Y
Akhter, Mymoona
Husain, A |
| Keywords: | Glyceride derivatives
biphenyl acetic acid
gastrointestinal toxicity
biological evaluation
kinetic study |
| Issue Date: | Apr-2006 |
| Publisher: | NISCAIR-CSIR, India |
| IPC Code: | Int.Cl.7 C 07 C |
| Abstract: | Glyceride derivatives (3a and 3b) of
biphenyl acetic acid have been synthesized to reduce the gastrointestinal
toxicity associated with it and are tested for their ulcerogenicity, anti-inflammatory
and analgesic activity and hydrolytic behaviour. The prodrugs have been
prepared by reacting 1,2,3-trihydroxypropane-1,3-dipalmitate/stearate 1 with
the acid chloride of biphenyl acetic acid. The prodrugs are significantly less
irritating to the mucosa as indicated by scores of 0.75 and 0.82 by 3a and 3b compared to 2.3 of biphenyl acetic
acid. The prodrugs show better anti-inflammatory and analgesic activity than
the parent drug. The hydrolysis studies of prodrugs show that the prodrugs are
resistant to hydrolysis at pH 3, 4, 5 than at pH 7.4. The peak plasma
concentration (Cmax) 28.63  g/mL of biphenyl acetic acid is attained in 2 hr
whereas in case of 3a and 3b treated animals Cmax 33.5 and 34.6 g/mL is
attained in 3 hr respectively. All these studies indicate that the glyceride
prodrugs of biphenyl acetic acid might be considered as potential biolabile
prodrugs of biphenyl acetic acid. |
| Page(s): | 1014-1019 |
| CC License: |  CC Attribution-Noncommercial-No Derivative Works 2.5 India |
| ISSN: | 0975-0983(Online); 0376-4699(Print) |
| Source: | IJC-B Vol.45B(04) [April 2006]
|
|
