76979-31-2

Upstream product

• 141-84-4 2-thioxo-4-thiazolidinone 
• 591-31-1 3-methoxy-benzaldehyde 

Downstream Products

• 19924-43-7 3-methoxyphenylacetonitrile 
• 91715-52-5 β-(3-methoxyphenyl)-α-mercaptoacryIic acid 
• 7635-28-1 3-methoxyphenylalanine 
• 81154-03-2 morpholine salt of (E,Z)-5-(3-methoxyphenylmethylene)-4-oxo-2-thioxothiazolidine 
• 76979-50-5 5-(3-methoxyphenylmethylene)-2-morpholino-4-oxo-2-thiazoline 
• 76979-48-1 5-(3-Methoxyphenylmethylene)-2-piperidino-2-thiazolin-4-one 
• 76979-39-0 5-(3-Methoxyphenylmethylene)-2-imino-4-thiazolidinone 
• 76979-34-5 5-[1-(3-Methoxy-phenyl)-meth-(E)-ylidene]-2-methylsulfanyl-thiazol-4-one 
• 76979-38-9 5-(3-methoxyphenylmethylene)-3-methyl-4-oxo-2-thioxothiazolidine 
• 91715-53-6 3-(3-methoxy-phenyl)-2-thioxo-propionic acid 

Relevant academic research and scientific papers

Synthesis, molecular modeling, selective aldose reductase inhibition and hypoglycemic activity of novel meglitinides

In the present study, a novel generation of selective aldose reductase ALR2 inhibitors with significant hypoglycemic activities was designed and modulated based on rhodanine scaffold joined to an acetamide linker in between two lipophilic moieties. The synthesis of the novel compounds was accomplished throughout simple chemical pathways. Molecular docking was performed on B-cell membrane protein SUR1, aldehyde reductase ALR1 and aldose reductase ALR2 active sites. Compounds 10B, 11B, 12B, 15C, 16C, 26F and 27F displayed the highest hypoglycemic activities with 80.7, 85.2, 87, 82.3, 83.5, 81.4 and 85.3% reduction in blood glucose levels, respectively. They were more potent than the standard hypoglycemic agent repaglinide with 65.4% reduction in blood glucose level. Compounds 12B and 15C with IC50 0.29 and 0.35 μM were more potent than the standard ALR2 inhibitor epalrestat with IC50 0.40 μM. They were selective towards ALR2 over ALR1 134 and 116 folds, respectively. Molecular docking studies matched with the in-vitro and in-vivo results to elucidate the dual activities of both compounds 12B and 15C as potent antagonists for ALR2 over ALR1 and good agonists for the SUR1 protein.

Introducing broadened antibacterial activity to rhodanine derivatives targeting enoyl-acyl carrier protein reductase

Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50=3.18μM for Mtb InhA; IC50=10nM for DNA Gyrase B) with positive controls. Structure–activity relationship discussion and molecular docking model revealed the significance of rhodanine moiety and derived methoxyl on meta-position, pointing out orientations for future modification.

CHEMILUMINESCENT COMPOSITIONS, METHODS, ASSAYS AND KITS FOR OXIDATIVE ENZYMES

Chemiluminescent compositions, methods, assays and kits for oxidative enzymes are described. Further disclosed are dioxetane compounds of the form: 0-0 ΛR R R T (i) where R can independently be any branched alkyl or cycloalkyl group which provides stabili