3084-04-6Relevant articles and documents
Based on isoxazole substitution of benzamide derivatives and anti-prostate cancer drug applications
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Paragraph 0065; 0073-0074, (2022/01/10)
The present invention discloses a class (I), formula (II) structure based on isoxazole substituted benzamide derivatives and antiprostate cancer drug applications, such isoxazole substituted benzamide derivatives, can effectively inhibit the activity of a
Potential of aryl-urea-benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease
Kurt, Belma Zengin,Gazioglu, Isil,Basile, Livia,Sonmez, Fatih,Ginex, Tiziana,Kucukislamoglu, Mustafa,Guccione, Salvatore
, p. 80 - 92 (2015/08/11)
New benzofuranylthiazole derivatives containing the aryl-urea moiety were synthesized and evaluated in vitro as dual acetylcholinesterase (AChE)-butyrylcholinesterase (BuChE) inhibitors. In addition, the cupric reducing antioxidant capacities (CUPRAC) and ABTS cation radical scavenging abilities of the synthesized compounds were assayed. The result showed that all the synthesized compounds exhibited inhibitory activity on both AChE and BuChE with 1-(4-(5-bromobenzofuran-2-yl)thiazol-2-yl)-3-(2-fluorophenyl)urea (e25, IC50 value of 3.85 1/4M) and 1-(4-iodophenyl)-3-(4-(5-nitrobenzofuran-2-yl)thiazol-2-yl)urea (e38, IC50 value of 2.03 1/4M) as the strongest inhibitors against AChE and BuChE, respectively. Compound e38 was 8.5-fold more potent than galanthamine. The selectivity index of e25 and e38 was 2.40 and 0.37 against AChE and BuChE, respectively. Compound e2, e4 and e11 (IC50 Combining double low line 0.2, 0.5 and 1.13 1/4M, respectively) showed a better ABTS cation radical scavenging ability than the standard quercetin (IC50 Combining double low line 1.18 1/4M). Best poses of compounds e38 on BuChE and e25 on AChE indicate that the thiazole ring and the amidic moiety are important sites of interaction with both ChEs. In addition, the benzofuran ring and phenyl ring are anchored to the side chains of both enzymes by €-€(pi-pi) interactions.
Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA
Annadurai, Sivakumar,Martinez, Rogelio,Canney, Daniel J.,Eidem, Tess,Dunman, Paul M.,Abou-Gharbia, Magid
supporting information, p. 7719 - 7725 (2013/02/21)
Privileged structure-based libraries have been shown to provide high affinity lead compounds for a variety of important biological targets. The present study describes the synthesis and screening of a 2-aminothiazole based compound library to determine th