7597-67-3

Upstream product

• 67-56-1 methanol 
• 3216-48-6 2-(benzo[b]thiophen-3-yl)acetonitrile 
• 1131-09-5 benzo[b]thiophene-3-acetic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 77-78-1 dimethyl sulfate 

Downstream Products

• 86738-58-1 N-<2-(3,4-dimethoxyphenyl)ethyl>-3-benzothienylacetamide 
• 1416134-79-6 C₁₇H₁₂O₃S 
• 1416134-91-2 C₁₈H₁₄O₃S 
• 1416134-92-3 C₁₈H₁₄O₄S 
• 1416134-93-4 C₁₉H₁₆O₅S 
• 1416134-80-9 C₁₇H₁₂N₂OS 
• 1416134-97-8 C₁₈H₁₄N₂OS 
• 1416134-98-9 C₁₈H₁₄N₂O₂S 
• 1416134-99-0 C₁₉H₁₆N₂O₃S 
• 87894-73-3 1-phenyl-3H-<1>benzothieno<2,3-c>pyran-3-one 
• 1416134-89-8 C₁₈H₁₂O₂S 
• 1354516-83-8 C₁₈H₁₂O₃S 
• 1354513-57-7 C₁₉H₁₄O₄S 
• 1416134-81-0 C₁₉H₁₆O₃S 

Relevant academic research and scientific papers

New Series of Potent Allosteric Inhibitors of Deoxyhypusine Synthase

Deoxyhypusine synthase (DHPS) is the primary enzyme responsible for the hypusine modification and, thereby, activation of the eukaryotic translation initiation factor 5A (eIF5A), which is key in regulating the protein translation processes associated with tumor proliferation. Although DHPS inhibitors could be a promising therapeutic option for treating cancer, only a few studies reported druglike compounds with this inhibition property. Thus, in this work, we designed and synthesized a new chemical series possessing fused ring scaffolds designed from high-throughput screening hit compounds, discovering a 5,6-dihydrothieno[2,3-c]pyridine derivative (26d) with potent inhibitory activity; furthermore, the X-ray crystallographic analysis of the DHPS complex with 26d demonstrated a distinct allosteric binding mode compared to a previously reported inhibitor. These findings could be significantly useful in the functional analysis of conformational changes in DHPS as well as the structure-based design of allosteric inhibitors.

NOVEL COMPOUNDS AND THEIR USE IN THERAPY

The present invention relates to novel chemical compounds formula (I) (C)n-B-(A)m-B-(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five-and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (-CO-), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.

NOVEL THIOPHENE COMPOUNDS AND METHOD FOR IN VIVO IMAGING

The present invention relates to novel labelled compounds of formula (I) (C)n-B-(A)m-B-(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group ( -CO- ), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1, for use in imaging amyloid deposits and aggregated protein in living patients. The invention further relates to imaging methods using labelled or unlabelled compounds of formual I and the use of unlabelled compounds in such methods.

Access to paullone analogues by intramolecular Heck reaction

The syntheses of paullone (1a) and three paullone derivatives, including a sulfur analogue (2a), a tricyclic derivative (2b), and a ring-enlarged variant (2c), are described, Pd-catalyzed intramolecular Heck reaction being the key step. The kinase-inhibitory properties of the novel paullone analogues were investigated.

Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme

The present invention relates to compounds that are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

PYRANOBENZOTHIOPHENE DERIVATIVES TO TREAT INFECTION WITH HEPATITIS C VIRUS

The invention is directed to a compound of the formula: (I) wherein substitutions at R1, R2 , R3 - R12,and Y are set forth in the specification; pharmaceutical compositions comprising said compound, methods of treating or preventing a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of said compound or pharmaceutical compositions including said compound and methods of inhibiting replication of a Hepatitis C virus comprising contacting the HCV virus with an effective amount of said compound or pharmaceutical compositions including said compound.

IMIDAZO(1,2-a)PYRIDINE DERIVATIVE

A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.

Synthesis and structure-antifungal activity relationships of 3-aryl-5-alkyl-2,5-dihydrofuran-2-ones and their carbanalogues: Further refinement of tentative pharmacophore group

Two series of 3-(substituted phenyl)-5-alkyl-2,5-dihydrofuran-2-ones related to a natural product, (-)incrustoporine, were synthesized and their in vitro antifungal activity evaluated. The compounds with halogen substituents on the phenyl ring exhibited selective antifungal activity against the filamentous strains of Absidia corymbifera and Aspergillus fumigatus. On the other hand, the influence of the lenghth of the alkyl chain at C(5) was marginal. The antifungal effect of the most active compound against the above strains was higher than that of ketoconazole, and close to that of amphotericin B. In order to verify the hypothesis about a possible relationship between the Michael-accepting ability of the compounds and their antifungal activity, a series of simple carbanalogues, 2-(substituted phenyl)cyclopent-2-enones, was prepared and subjected to antifungal activity assay as well.

Synthesis of 5,6,6a,7,7a,12a-Hexahydro-4H-benzobenzothienoquinolines and of 8-Phenyl-2,3,7,8,9,9a-hexahydro-1H-benzoquinolines

Demethylation of 1-(3-benzothienylmethyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline (1; R=H) gives two diastereoisomeric 1,2-dihydroxy-5,6,6a,7,7a,12a-hexahydro-4H-benzobenzothienoquinolines (4; R=H).Desulphurisation of their N-acetyl-di