Abstract:
:The present works deals with simple and efficient method of improving therapeutic efficacy of racemic ibuprofen by retarding gastrointestinal side effects through masking of carboxylic group chemically. This is achieved by synthesis and evaluation of ester derivatives of ibuprofen as mutual prodrugs with naturally occurring phenolic and alcoholic compounds. Promoieties like menthol; thymol and eugenol were selected with the aim of getting synergistic effect as these are natural analgesic having traditional medicinal values. Prodrugs are found to be highly lipophilic as compared to parent drug. All the prodrugs are found to be highly stable at acidic pH while undergoes hydrolysis at neutral and alkaline pH as indicated by their t(1/2) values. Synthesized prodrugs derivatives show increased anti-inflammatory activity that might be attributed to synergistic effect as ibuprofen conjugates to natural analgesics. Ulcer index shows much reduction in gastric ulceration compared to ibuprofen concluding the successful masking of acidic group.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Redasani VK,Bari SBdoi
10.1016/j.ejmech.2012.08.030subject
Has Abstractpub_date
2012-10-01 00:00:00pages
134-8eissn
0223-5234issn
1768-3254pii
S0223-5234(12)00521-1journal_volume
56pub_type
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