220504-68-7

Upstream product

• 204568-74-1 methyl 3-acetyloxy-4-methylbenzoate 
• 586-30-1 3-hydroxy-4-methylbenzoic acid 
• 3556-86-3 methyl 4-methyl-3-hydroxybenzoate 

Downstream Products

• 220504-70-1 diethyl (2-acetoxy-4-(methoxycarbonyl)benzyl)benzamidomalonate 
• 336111-37-6 Methyl 2-{[2-acetoxy-4-(methoxycarbonyl)benzyl]sulfanyl}-4-methoxybenzoate 
• 791838-00-1 3-acetoxy-4-(2-benzylcarbamoyl-2-methoxycarbonyl-ethyl)-benzoic acid methyl ester 
• 791838-08-9 3-(N-benzylcarbamoyl)-7-carboxy-3,4-dihydro-2H-1-benzopyran-2-one 
• 791838-06-7 3-benzylcarbamoyl-2-oxo-chroman-7-carboxylic acid benzyl ester 
• 336111-41-2 Methyl 2-hydroxy-4-(3-hydroxy-6-methoxy[1]benzothiophen-2-yl)benzoate 
• 336111-38-7 Methyl 2-{[2-hydroxy-4-(methoxycarbonyl)benzyl]sulfanyl}-4-methoxybenzoate 
• 220504-74-5 7-carboxy-3-benzamido-3,4-dihydroxy-2H-1-benzopyran-2-one 
• 220504-72-3 rac-N-benzoyl-4-carboxy-2-hydroxyphenylalanine 

Relevant academic research and scientific papers

NITROGEN-CONTAINING TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE

A nitrogen-containing tricyclic compound which acts as modulator of FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the use of the compoun

Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents

Malaria is a major health problem in poverty-stricken regions where new antiparasitic drugs are urgently required at an affordable price. We report herein the design, synthesis, and biological investigation of novel antimalarial agents with low potential to develop resistance and structurally based on a highly conjugated scaffold. Starting from a new hit, the designed modifications were performed hypothesizing a specific interaction with free heme and generation of radical intermediates. This approach provided antimalarials with improved potency against chloroquine-resistant plasmodia over known drugs. A number of structure-activity relationship (SAR) trends were identified and among the analogues synthesized, the pyrrolidinylmethylarylidene and the imidazole derivatives 5r, 5t, and 8b were found as the most potent antimalarial agents of the new series. The mechanism of action of the novel compounds was investigated and their in vivo activity was assessed.

QUINOLIN-4-YLHYDRAZINE DERIVATIVES AS ANTIMALARIAL AGENT

Novel quinolyl and acridinylhydrazone compounds of formula (I), which present remarkable biological activity especially against the choloroquine-resistant Plasmodium falciparum strains, useful for the treatment and prevention of malaria infection are described herein.

A novel synthesis of [1]benzothieno[3,2-b][1]benzofuran

A new synthesis of the title compound based on the formation of the furan ring in the key step was elaborated. Methyl 2-methoxy[1]benzothieno[3,2-b][1]benzofuran-7-carboxylate (15) was prepared by this methodology as a new type of a core for liquid crystal synthesis.

Synthesis and reactivity with β-lactamases of 'penicillin-like' cyclic depsipeptides

Several 7-carboxy-3-amido-3,4-dihydro-2H-1-benzopyran-2-ones have been synthesized as potential β-lactamase substrates and/or mechanism-based inhibitors. Substituted o-tyrosine precursors were prepared by the Sorensen method and then heated in vacuo to give the lactones. These compounds are cyclic analogues of aryl phenaceturates which are known to be β-lactamase substrates. The goal of incorporating the scissile ester group into a lactone was to retain the leaving group tethered to the acyl moiety at the acyl- enzyme stage of turnover by serine β-lactamases, in a manner similar to that during penicillin turnover. Further, in two cases, a functionalized methylene group para to the leaving group phenoxide oxygen was incorporated. These molecules possess a latent p-quinone methide electrophile which could, in principle, be unmasked during enzymic turnover and react with an active site nucleophile. All of these compounds were found to be substrates of class A and C β-lactamases, the first δ-lactones with such activity. Generally, k(cat) values were smaller than for the analogous acyclic depsipeptides, which suggests that the tethered leaving group may obstruct the attack of water on the acyl-enzymes. Further exploration of this structural theme might lead to quite inert acyl-enzymes and thus to significant inhibitors. Despite the apparent advantage offered by the longer-lived acyl-enzymes, the functionalized compounds were no better as irreversible inhibitors than comparable acyclic compounds [Cabaret, D.; Liu, J.; Wakselman, M.; Pratt, R. F.; Xu, Y. Bioorg. Med. Chem. 1994, 2, 757-771]. Thus, even tethered quinone methides, at least when placed as dictated by the structures of the present compounds, were unable to efficiently trap a nucleophile at serine β- lactamase active sites.