Excess glucocorticoids promote visceral obesity and insulin resistance. The main regulator of intracellular glucocorticoid levels are 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1), which converts inactive glucocorticoid into bioactive glucocorticoid such as cortisol in humans and corticosterone in rodents; therefore, the inhibition of 11β-HSD1 has considerable therapeutic potential for met...

OBJECTIVES Hybridization of bioactive natural and synthetic compounds is one of the most promising novel approaches for the design of hit and lead compounds with new molecular structures. In this investigation, a series of novel hybrid structures bearing quinazolinone, benzofuran and imidazolium moieties were designed and synthesized. MATERIALS AND METHODS Novel hybrid compounds were prepared...

has long been used as a Chinese folk medicine in the treatment of edema and scrofula. The constituents of L. stenocephala have been previously investigated and shown to contain benzofuran derivatives. Here, we report the isolation and structural elucidation of three new dimeric benzofuran derivatives, ligulacephalins A (1), B (2) and C (3), together with three known compounds from the roots of ...

In the present study, the oxidation of 3-(4-chloro-1H-imidazol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1ones with mercuric(II) acetate in in polyethylene glycol (PEG-400) gave the corresponding 2-((4-chloro-1Himidazol-5-yl)methylene)benzofuran-3(2H)-ones. Newly synthesized compounds were tested for their in vitro antimicrobial activity.

A series of heterocyclic quinones based on benzofuran, benzothiophene, indazole and benzisoxazole has been synthesized, and evaluated for their ability to function as substrates for recombinant human NAD(P)H:quinone oxidoreductase (NQO1), a two-electron reductase upregulated in tumor cells. Overall, the quinones are excellent substrates for NQO1, approaching the reduction rates observed for men...

A new approach to the synthesis of cyclopenta[b]benzofuran derivatives via reaction of 1,3-dicarbonyl compounds with α,β,γ,δ-unsaturated aldehydes is described. The constitution and configuration of the new products have been firmly established by means of residual dipolar couplings (RDCs) and ab initio (13)C NMR chemical shift predictions.

The novel 3H-spiro[1-benzofuran-2-cyclopentan]-3-one skeleton has been made accessible by different routes. One- and two-step protocols lead to tricyclic and tetracyclic benzofuranones 2 and 3, respectively. A four-step synthesis to spirocompound 4 is described. The novel spirocyclic benzofuranones display modest to no inhibition of the human peptidyl prolyl cis/trans isomerase Pin1.