We designed and synthesized conformationally restricted analogues and regioisomers of the nonsteroidal anti-inflammatory drug indomethacin
Indomethacin (IND) is a non-steroidal anti-inflammatory drug (NSAID), used as an analgesic and anti-pyretic
The 1960s saw acetic acid derivatives developed into indomethacin, diclofenac, and sulindac, and propionic derivatives into ibuprofen, naproxen, and ketoprofen
The indomethacin derivatives synthesised during this work are summarised in Figure 2 and can be considered in three distinct groups; compounds Figure 1, Figure 2
Biosynthesis of Indomethacin
53-86-1 indometacin Indocin Indomethacine View More Molecular Weight 357
Non-steroidal anti-inflammatory drugs (NSAIDs) have drawn considerable attention in the field of cancer treatment, yet these drugs display limited potency and selectivity against cancer cells
Indomethacin concentrations reached during therapy have produced in vivo effects
Indomethacin actively inhibits the expression of PTGES2 hence inhibiting the prostaglandin synthesis and reducing pain and inflammation significantly
To address these problems, we designed a peptide-based self-delivery system [Indomethacin-Phe-Phe-Tyr (H 2 PO 3)-Ser-Val, IDM-FFpYSV] that combines an NSAID molecule (indomethacin, or IDM) and a segment of anticancer tripeptide (tyroservatide, or YSV)
In the first step, by the condensation of levulinic acid with p-chlorobenzoyl-p-methoxy-phenyl-hydrazine in homogeneous acidic catalysis an intermediate is formed
This prevents prostaglandin synthesis (prostaglandins elevate body temperature and make nerve endings more sensitive to pain transmission)
Therefore, colon-specific and controlled
In animal studies, administration of prostaglandin synthesis inhibitors such as indomethacin, resulted in increased pre- and post-implantation loss; Prostaglandins also have been shown to have an important role in fetal kidney development; in published animal studies, prostaglandin synthesis inhibitors have been reported to impair kidney Solid complexes have been prepared and characterized by IR, UV-Vis, elemental analysis, and 1H NMR
A human whole-blood COX assay shows the modifications on the 3-acetic acid
Nonsteroidal anti-inflammatory drugs (NSAIDs) exert their pharmacological activities by inhibiting cyclooxygenase (COX)-1 and COX-2
A study about indomethacin in podocytes also showed that inhibition of inflammatory response, which is dependent on TNF-α, triggers the activation of NF-κB
The molecular structure of indomethacin was used as a starting scaffold for the synthesis of 20 novel analogs and to study their effects on the proliferation of three human colon cancer cell lines, HCT-116, HT-29, and Caco-2, by MTT assay
Notably, this new method was applied for the synthesis of key intermediate of indomethacin
To obtain