83806-32-0Relevant academic research and scientific papers
Exploration of benzofuran-based compounds as potent and selective Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) inhibitors
Moolman, Chantalle,van der Sluis, Rencia,Beteck, Richard M.,Legoabe, Lesetja J.
, (2021/04/09)
Plasmodium falciparum glycogen synthase kinase-3 (PfGSK-3) has been identified as a potential target for the development of novel drugs against multi-drug resistant malaria. A series of benzofuran-based compounds was synthesised and evaluated as inhibitors of recombinantly expressed and purified PfGSK-3 and human glycogen synthase kinase-3 beta (HsGSK-3β). Of this series, five compounds (5k, 5m, 5p, 5r, 5s) preferentially inhibited PfGSK-3, with four of these compounds exhibiting IC50 values in the sub-micromolar range (0.00048–0.440 μM). Evaluation of the structure-activity relationships required for PfGSK-3 selective inhibition indicated that a C6-OCH3 substitution on ring A is preferred, while the effect of the ring B substituent on activity, in decreasing order is: C4′-CN > C4′-F > C3′-OCH3 > C3′,4′-diCl. To date, development of PfGSK-3 inhibitors has been limited to the 4-phenylthieno[2,3-b]pyridine class. Chalcone-based scaffolds, such as the benzofurans described herein, are promising new hits which can be explored for future design of PfGSK-3 selective inhibitors.
Potent α-amylase inhibitors and radical (DPPH and ABTS) scavengers based on benzofuran-2-yl(phenyl)methanone derivatives: Syntheses, in vitro, kinetics, and in silico studies
Ali, Basharat,Ali, Irfan,Chigurupati, Sridevi,Iqbal, Muhammad Shahid,Ji, Xingyue,Khan, Khalid Mohammed,Perveen, Shahnaz,Rafique, Rafaila,Rehman, Ashfaq Ur,Salar, Uzma,Taha, Muhammad,Wadood, Abdul
, (2020/09/11)
Thirty benzofuran-2-yl(phenyl)methanones 1–30 were synthesized and characterized their structures by spectroscopic techniques. Substituted phenacyl bromide and different derivatives of 2-hydroxy-benzaldehyde treated in the presence of anhydrous K2/s
Synthesis and anticandidal activities of some aryl (5-chloro-benzofuran-2-yl) ketoximes
Karaburun, Ahmet Cagri
, p. 427 - 436 (2019/06/18)
Background: In this study, some aryl (5-chloro-benzofuran-2-yl) ketoximes and their ethers were synthesised to evaluate their antifungal activity against C. albicans, C. glabrata, C. krusei, and C. parapsilosis. Methods: The structure elucidation of the c
DABCO-promoted efficient and convenient synthesis of benzofurans
Meshram,Reddy, B. Chennakesava,Prasad,Goud, P. Ramesh,Kumar, G. Santosh,Kumar, R. Naveen
experimental part, p. 1669 - 1676 (2012/05/04)
An efficient and convenient synthesis of benzofurans has been described from phenacyl halides and o-hydroxy benzaldehyde in the presence of DABCO. The procedure is applicable for a variety of phenacyl halides and provide a variety of benzofurans. DABCO ac
Solid state synthesis of 2-aroylbenzo[b]furans, 1,3-thiazoles and 3-aryl-5,6-dihydroimidazo[2,1-b][1,3]thiazoles from α-tosyloxyketones using microwave irradiation
Varma, Rajender S.,Kumar, Dalip,Liesen, Per J.
, p. 4093 - 4096 (2007/10/03)
The expeditious solventless syntheses of 2-aroylbenzo[e]furans, 1,3-thiazoles and 3-aryl-5,6-dihydroimidazo[2,1-b]-[1,3]thiazoles are described from readily accessible α-tosyloxyketones and mineral oxides in processes that are accelerated by exposure to m
