Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.4.23.5 (cathepsin D)
 4,130 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Gallic acid, one of the most abundant plant phenolic acids, has been modified to cathepsin D protease inhibitors. The strategy of modification was proposed basing on some previously reported structure and activity relationship (SAR) studies. The synthesized naphthophenone fatty acid amide derivatives have been evaluated for in vitro cathepsin D inhibition activity. Two of them have shown significant inhibition activity with IC(50) values of 0.06 and 0.14 microM, respectively, as compared against pepstatin (0.0023 microM), the most potent inhibitor known so far. The study revealed that such attempts on gallic acid based pharmacophores might result in potent inhibitors of cathepsin D.
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PMID:Synthesis of gallic acid based naphthophenone fatty acid amides as cathepsin D inhibitors. 1679 87

The leading cause of several degenerative diseases such as atherosclerosis, cancer, aging, cardiovascular, and inflammatory diseases is oxidative stress, a consequence of overproduction and accumulation of free radicals. Naturally occurring antioxidants polyphenols have unnumbered biological activities such as antibacterial, anticancer, antiviral, antifungal, anticholesterol, and antiulcer. A naturally occurring gallic acid (3,4,5-trihydroxybenzoic acid), is highly antioxidant and may play a protective role in healthy individuals by inhibiting apoptosis. Pharmacological agents containing gallic acid and of diverse therapeutic categories as antioxidants, anticancer, antimicrobial, chondro-protective effect, carbonic anhydrase inhibitors, antidiabetic activity, anti-ulcerogenic, cathepsin D inhibitor, etc. have made this nucleus as an indispensable anchor for designing and development of new pharmacological agents. This review is an update on the latest development of the chemistry and the medicinal impacts of pharmacophores containing gallic acids. In addition, fused gallic acid derivatives and hybrid molecules containing different bioactive moieties in the presence of gallic acid are also presented and discussed.
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PMID:Recent developments of gallic acid derivatives and their hybrids in medicinal chemistry: A review. 3273 Nov 88