58778-45-3

Upstream product

• 2554-82-7 2-acetoxy-3-methoxybenzoic acid 
• 877-22-5 3-methoxysalicylic acid 

Downstream Products

• 218923-45-6 2'-deoxy-2'-(3-methoxy-2-acetoxybenzamido)-3',5'-O-(1,1,3,3-tetraisopropyldisiloxane-1,3-diyl)adenosine 
• 156806-81-4 methyl 6-[N-(2-hydroxy-3-methoxybenzoyl)amino] hexanoate 
• 1313886-74-6 (2-hydroxy-3-methoxyphenyl)(2-(4-methoxyphenyl)-5-methylbenzofuran-3-yl)methanone 
• 1053263-61-8 N-[(2R,3R,3aS,9aR)-2-(6-Amino-purin-9-yl)-5,5,7,7-tetraisopropyl-tetrahydro-1,4,6,8-tetraoxa-5,7-disila-cyclopentacycloocten-3-yl]-2-hydroxy-3-methoxy-benzamide 
• 367526-60-1 ethyl [(2-acetoxy-3-methoxyphenyl)hydroxymethylidene]ethoxycarbonylacetate 
• 30674-62-5 (2-hydroxy-3-methoxyphenyl)(morpholino)methanone 
• 46984-64-9 2-hydroxy-3-methoxy-benzoic acid-(2-diethylamino-ethyl ester) 

Relevant academic research and scientific papers

Thiazole compound as well as preparation method and application thereof

The invention relates to thiazole compounds as well as a preparation method and application thereof, and belongs to the field of medicinal chemistry. The compound has a structural general formula described in the specifications of the invention; the compound or the prodrug thereof or pharmaceutically acceptable salts of the compound not only can significantly improve the biological activity, but also can effectively reduce the loss of biological activity due to glycosylation, significantly improve the exposure of effective drugs, and can be used for preparing medicines for preventing or treating hepatic fibrosis, medicines for preventing or treating viral influenza, medicines for treating Alzheimer's disease and Parkinson's disease and the like, and the clinical application of the compound is expanded.

Synthesis and antimicrobial evaluation of new benzofuran derivatives

Thirteen compounds, based on benzofuran skeleton bearing aryl substituents at its C-3 position through methanone linker, were synthesized and screened for their antibacterial and antifungal activities against four bacteria Escherichia coli, Staphylococcus aureus, Methicillin-resistant S. aureus, Bacillus subtilis, and a fungus Candida albicans. Four hydrophobic benzofuran analogs were found to exhibit favorable antibacterial activities (MIC80 = 0.39-3.12 μg/mL), which were better than the control drugs.

A highly practical route to 2-methylchromones from 2-acetoxybenzoic acids

2-Methylchromones were accessed via a keto ester condensation on 2-acetoxybenzoyl chloride, followed by cyclization and decarboxylation. No column chromatography was required in the process.

Selective tight binding inhibitors of trypanosomal glyceraldehyde-3- phosphate dehydrogenase via structure-based drug design

Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) from the sleeping sickness parasite Trypanosoma brucei is a rational target for anti- trypanosomatid drug design because glycolysis provides virtually all of the energy for the bloodstream form of this parasite. Glycolysis is also an important source of energy for other pathogenic parasites including Trypanosoma cruzi and Leishmania mexicana. The current study is a continuation of our efforts to use the X-ray structures of T. brucei and L. mexicana GAPDHs containing bound NAD+ to design adenosine analogues that bind tightly to the enzyme pocket that accommodates the adenosyl moiety of NAD+. The goal was to improve the affinity, selectivity, and solubility of previously reported 2'-deoxy-2'-(3-methoxybenzamido)adenosine (1). It was found that introduction of hydroxyl functions on the benzamido ring increases solubility without significantly affecting enzyme inhibition. Modifications at the previously unexploited N6-position of the purine not only lead to a substantial increase in inhibitor potency but are also compatible with the 2'-benzamido moiety of the sugar. For N6-substituted adenosines, two successive rounds of modeling and screening provided a 330-fold gain in affinity versus that of adenosine. The combination of N6- and 2'- substitutions produced significantly improved inhibitors. N6-Benzyl (9a) and N6-2-methylbenzyl (9b) derivatives of 1 display IC50 values against L. mexicana GAPDH of 16 and 4 μM, respectively (3100- and 12500-fold more potent than adenosine). The adenosine analogues did not inhibit human GAPDH. These studies underscore the usefulness of structure-based drug design for generating potent and species-selective enzyme inhibitors of medicinal importance starting from a weakly binding lead compound.

Substituted 2-amino chromones and process for the preparation thereof

This invention relates to substituted 2-amino chromones of the general structure I: SPC1 wherein R1, R2, R3, and R4 may be hydrogen, hydroxy, lower alkyl or lower alkoxy of 1-6 carbon atoms, halogen such as chloro or bromo, or aryl such as phenyl, and X may be cyano or carboxamido. Two novel procedures for preparing substituted 2-amino chromones having the Formula I, starting with salicylic acid or substituted salicylic acid, are described. The compounds of this invention are active in the prevention of allergic and asthmatic reactions in mammals.