Prodrugs of NSAIDs: A Review

نویسندگان

  • Kamal Shah
  • Jeetendra K. Gupta
  • Nagendra S. Chauhan
  • Neeraj Upmanyu
  • Sushant K. Shrivastava
  • Pradeep Mishra
چکیده

Intoroduction Prodrug approach deals with chemical biotransformation or enzymatic conversion or involves inactive or less active bio-reversible derivatives of active drug molecules. They have to pass through enzymatic or chemical biotransformation before eliciting their pharmacological action. Methods & Materials The two different pharmacophores combine to give synergistic activity or may help in targeting the active drug to its target. Prodrug super seeds the problems of prodrug designing, for example solubility enhancement, bioavailability enhancement, chemical stability improvement, presystemic metabolism, site specific delivery, toxicity masking, improving patient acceptance, or eradicating undesirable adverse effects. Results As an outcome the search for a prodrug or mutual prodrug with reduced toxicity has continued during recent years. This present review emphasizes the common help to revamp physiochemical, pharmaceutical and therapeutic effectiveness of drugs. Conclusion This gives the researcher a common platform where they can find prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation, ulcergenocity and bleeding).

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Prodrugs of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs), More Than Meets the Eye: A Critical Review

The design and the synthesis of prodrugs for nonsteroidal anti-inflammatory drugs (NSAIDs) have been given much attention by medicinal chemists, especially in the last decade. As a therapeutic group, NSAIDs are among the most widely used prescribed and over the counter (OTC) medications. The rich literature about potential NSAID prodrugs clearly shows a shift from alkyl, aryalkyl or aryl esters...

متن کامل

Design, synthesis and evaluation of diclofenac-antioxidant mutual prodrugs as safer NSAIDs

Diclofenac has been conjugated with different antioxidants having antiulcerogenic activity with the objective of obtaining diclofenac-antioxidant mutual prodrugs as safer NSAIDs devoid of ulcerogenic side-effects. The synthesized derivatives are screened for their antiinflammatory, analgesic and antiulcer activity. The mutual prodrugs show retention of antiinflammatory activity with reduced ulc...

متن کامل

Design, Synthesis, and Biological Evaluation of Mutual Prodrugs of Some Selected NSAIDs

Non-steroidal Anti-inflammatory drugs (Aceclofenac, Mefenamic acid) have conjugated with different antioxidants such as Thymol, Menthol which having antiulcerogenic activity with the NSAIDsantioxidant mutual prodrug gastro sparing NSAIDs devoid of Ulcerogenic side effects. Two mutual Prodrugs have synthesized in which NSAIDs have been conjugated with different antioxidants by a glycolic acid sp...

متن کامل

NO-NSAIDs. Part 3: nitric oxide-releasing prodrugs of non-steroidal anti-inflammatory drugs.

In continuation of our efforts to discover novel nitric oxide-releasing non-steroidal anti-inflammatory drugs (NO-NSAIDs) as potentially "Safe NSAIDs," we report herein the design, synthesis and evaluation of 21 new NO-NSAIDs of commonly used NSAIDs such as aspirin, diclofenac, naproxen, flurbiprofen, ketoprofen, sulindac, ibuprofen and indomethacin. These prodrugs have NO-releasing disulfide l...

متن کامل

Amide prodrugs of NSAIDs: Synthesis and biological evaluation with a hydrolysis study

The aim of the present study was to synthesize prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation and bleeding) associated with their use. A total of six amide-based prodrugs (Ia-f) of aceclofenac, diclofenac, fenbufen, indomethacin, mefenamic acid and 4-biphenyl acetic acid were synthesized through one-pot method (single step synthesis). The structures of th...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:

دوره 11  شماره 

صفحات  -

تاریخ انتشار 2017