628330-16-5

Upstream product

• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 50773-56-3 3-benzyloxy-4-hydroxybenzaldehyde 
• 107-30-2 chloromethyl methyl ether 
• 100-39-0 benzyl bromide 
• 65299-00-5 3-hydroxy-4-(methoxymethoxy)benzaldehyde 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 114688-53-8 3-(benzyloxy)-4-(methoxymethoxy)benzaldehyde 

Downstream Products

• 628330-17-6 ethyl 3-[3-benzyloxy-4-(methoxymethoxy)phenyl]propionate 
• 628330-18-7 ethyl 3-(3-benzyloxy-4-hydroxyphenyl)propionate 
• 628334-57-6 ethyl 3-[3-benzyloxy-4-(3-{3-ethoxy-1-[5-(trifluoromethyl)-2-pyridyl]-1H-pyrazol-4-yl}propoxy)phenyl]propanoate 
• 628334-51-0 ethyl 3-[4-(3-{3-ethoxy-1-[5-(trifluoromethyl)-2-pyridyl]-1H-pyrazol-4-yl}propoxy)-3-hydroxyphenyl]propanoate 

Relevant academic research and scientific papers

Synthesis of non-prenyl analogues of baccharin as selective and potent inhibitors for aldo-keto reductase 1C3

Inhibitors of a human member (AKR1C3) of the aldo-keto reductase superfamily are regarded as promising therapeutics for the treatment of prostatic and breast cancers. Baccharin [3-prenyl-4-(dihydrocinnamoyloxy)cinnamic acid], a component of propolis, was shown to be both potent (Ki56 nM) and highly isoform-selective inhibitor of AKR1C3. In this study, a series of derivatives of baccharin were synthesized by replacing the 3-prenyl moiety with aryl and alkyl ether moieties, and their inhibitory activities for the enzyme were evaluated. Among them, two benzyl ether derivatives, 6m and 6n, showed an equivalent inhibitory potency to baccharin. The molecular docking of 6m in AKR1C3 has allowed the design and synthesis of (E)-3-{3-[(3-hydroxybenzyl)oxy]-4-[(3-phenylpropanoyl)oxy]phenyl}acrylic acid (14) with improved potency (Ki6.4 nM) and selectivity comparable to baccharin. Additionally, 14 significantly decreased the cellular metabolism of androsterone and cytotoxic 4-oxo-2-nonenal by AKR1C3 at much lower concentrations than baccharin.

1,2-AZOLE DERIVATIVES WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY

A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, - O -, - S - and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents -OR4 (R4 is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.