3084-04-6Relevant academic research and scientific papers
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
SUBSTITUTED AMINOTHIAZOLES AS INHIBITORS OF NUCLEASES
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Page/Page column 14-15; 40; 47, (2019/11/12)
The invention provides compounds represented by the structural formula (1): wherein R1, R2, R3, R4, R5, R6 are as defined in the claims. The compounds are inhibitors of nucleases, and are useful in particular in a method of treatment and/or prevention of proliferative diseases, neurodegenerative diseases, and other genomic instability associated diseases.
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.
Novel benzofuran derivatives: Synthesis and antitumor activity
Othman, Dina I.,Abdelal, Ali M.M.,El-Sayed, Magda A.,El Bialy, Serry A.A.
, p. 29 - 35 (2013/05/23)
A series of new benzofuran derivatives 3a-f, 5a-e containing a heterocyclic substituent linked to benzofuran nucleus at C-2 were synthesized as potential antitumor agents. These products were synthesized starting with 2-bromoacetylbenzofuran 1. The structures of all compounds were established on the basis of analytical and spectral data. The synthesized compounds were tested against human liver carcinoma cell line (HEPG2) and all were more potent than the comparative standard (5-flurouracil). Compound 3f was the most active (IC50 = 12.4μg/mL).
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
Synthesis of 3-[4-(1-benzofuran-2-yl)-1,3-thiazol-2-yl]-2-(4-aryl)-1,3- thiazolidin-4-one derivatives as biological agents
Venkatesh, Bhovi K.,Bodke, Yadav D.,Biradar
scheme or table, p. 1926 - 1931 (2010/11/18)
A protocol for the synthesis of 3-[4-(1-benzofuran-2-yl)-1,3-thiazol-2-yl]- 2-(4-aryl)-1,3-thiazolidin-4-one derivatives (5a-e) has been developed from 1-(1-benzofuran-2-yl)-2-bromoethanone (2),which served as a key intermediate for the synthesis of the title compounds. The reaction of compound 2 with thiourea furnished 4-(1-benzofuran-2-yl)-1,3-thiazol-2-amine 3, which upon further reaction with various aromatic aldehydes, gave Schiff bases 4a-e. These Schiff bases, when treated with thioacetic acid in the presence of catalytic amount of anhydrous ZnCl2, yielded thiazolidinone derivatives 5a-e. All the newly synthesized compounds have been characterized by analytical and spectral data and screened for their antimicrobial and analgesic activity. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. Copyright
MODULATORS OF GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-κB ACTIVITY AND USE THEREOF
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Page/Page column 77, (2008/12/05)
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and immune diseases, obesity and diabetes having the structure o
