303091-99-8Relevant academic research and scientific papers
E-N-(2-acetyl-phenyl)-3-phenyl-acrylamide targets abrin and ricin toxicity: Hitting two toxins with one stone
Chauhan, Vinita,Dhaked, Ram Kumar,Pathak, Uma,Phatak, Pooja,Saxena, Nandita
, (2021/09/04)
The efficacy of small molecule inhibitors (SMIs) against the enzymatic activity of Shiga toxin prompted the evaluation of their efficacy on related toxins viz. ricin and abrin. Ricin, like Shiga toxin, is listed as a category B bioweapon and belongs to th
Synthesis and biological evaluation of asymmetric indole curcumin analogs as potential anti-inflammatory and antioxidant agents
Bandgar, Babasaheb P.,Kinkar, Santosh N.,Chavan, Hemant V.,Jalde, Shivkumar S.,Shaikh, Rafik U.,Gacche, Rajesh N.
, p. 7 - 11 (2014/03/21)
A series of asymmetric indole curcumin analogs were synthesized and evaluated as possible inhibiters of pro-inflammatory enzymes such as COX-2, pro-inflammatory cytokines as TNF-α and IL-6, trypsin and β-glucuronidase. They were also tested for antioxidant activities. The results showed that compounds 5e and 5h were found to be the most potent inhibitors of COX-2 (83.33%, 82.50%) and β-glucuronidase (67.80%, 64.12%). All the synthesized compounds exhibited promising activity against IL-6 in a range of 71-100% at 10 μM concentration. Compounds 5f, 5h, 5e, 5c and 5d showed significant inhibition against TNF-α (28-51%) and IL-6 (87-98%) with low toxicity (45-51%) against CCK-8 cells. With few exceptions, all other compounds were found to be good to excellent inhibitors of IL-6 and moderate inhibitors of TNF-α; however, the toxicity profiles of these compounds need to be ameliorated in further optimization studies. Amongst the tested compounds, 5c, 5b, 5j and 5g were found to possess excellent reducing activity and 5b, 5c and 5h were moderate DPPH (1,1-diphenyl-2-picryl hydrazine) radical scavengers.
Synthesis and antioxidant, cytotoxicity and antimicrobial activities of novel curcumin mimics
Bandgar, Babasaheb P.,Jalde, Shivkumar S.,Korbad, Balaji L.,Patil, Sachin A.,Chavan, Hemant V.,Kinkar, Santosh N.,Adsul, Laxman K.,Shringare, Sadanand N.,Nile, Shivraj H.
scheme or table, p. 267 - 274 (2012/07/13)
Claisen-Schmidt condensation of 3-(1,2,3,6-tetrahydro-1-methylpyridin-4-yl) -2,4,5-trimethoxybenzaldehyde 3 and various aromatic, heterocyclic and alicyclic amides of 3-aminoacetophenone 6(as) afforded novel curcumin mimics. All the synthesized compounds
Synthesis, biological evaluation, and molecular docking of N-{3-[3-(9-methyl-9H-carbazol-3-yl)-acryloyl]-phenyl}-benzamide/amide derivatives as xanthine oxidase and tyrosinase inhibitors
Bandgar, Babasaheb P.,Adsul, Laxman K.,Chavan, Hemant V.,Shringare, Sadanand N.,Korbad, Balaji L.,Jalde, Shivkumar S.,Lonikar, Shrikant V.,Nile, Shivraj H.,Shirfule, Amol L.
, p. 5649 - 5657 (2012/10/29)
Claisen-Schmidt condensation of 3-formyl-9-methylcarbazole with various amides of 3-aminoacetophenone afforded N-{3-[3-(9-methyl-9H-carbazol-3-yl)- acryloyl]-phenyl}-benzamide/amide derivatives. All compounds were investigated for their in vitro xanthine oxidase (XO), tyrosinase and melanin production inhibitory activity. Most of the target compounds had more potent XO inhibitory activity than the standard drug (IC50 = 4.3-5.6 μM). Interestingly, compound 7q bearing cyclopropyl ring was found to be the most potent inhibitor of XO (IC50 = 4.3 μM). Molecular modelling study gave an insight into its binding modes with XO. Compounds 7a, 7d, 7e, 7g, and 7k were found to be potent inhibitors of tyrosinase (IC50 = 14.01-17.52 μM). These results suggest the possible use of these compounds for the design and development of novel XO and tyrosinase inhibitors.
Synthesis and biological evaluation of novel curcumin analogues as anti-inflammatory, anti-cancer and anti-oxidant agents
Bandgar, Babasaheb P.,Hote, Baliram S.,Jalde, Shivkumar S.,Gacche, Rajesh N.
, p. 3006 - 3014 (2012/10/29)
A series of novel curcumin analogues 5a- m were synthesized by Claisen-Schmidt condensation of various aromatic and heteroaromatic amides of 3-aminoactophenones 4a-m with 3-bromo-2,4,6-trimethoxybenzaldehyde and characterized by IR, 1H NMR and mass spectroscopic analysis and were evaluated for anti-inflammatory, anti-cancer and anti-oxidant activity. Out of the 13 synthesized compounds, compounds 5f, 5j and 5m were excellent inhibitors of TNF-α and IL-6. Compounds 5c, 5e, 5b and 5d showed potent COX-2 inhibition, compounds 5d and 5f have shown good trypsin inhibition and compounds 5e, 5g and 5c exhibited excellent β-glucuronidase inhibition. Compounds 5l and 5m showed potent anti-cancer activity against selected five human cancer cell lines. All the compounds exhibited moderate free radical scavenging activity, while compounds 5a and 5m were excellent OH radical scavengers. Springer Science+Business Media, LLC 2011.
