13188-55-1

Upstream product

• 120-61-6 1,4-benzenedicarboxylic acid dimethyl ester 
• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 
• 1679-64-7 Monomethyl terephthalate 
• 108724-76-1 (carbonic acid ethyl ester)-(terephthalic acid methyl ester)-anhydride 
• 100-21-0 terephthalic acid 

Downstream Products

• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 
• 24852-49-1 N-(4-methyl-2-thioxo-thiazol-3-yl)-terephthalamic acid methyl ester 
• 24000-79-1 bis(4-methoxycarbonylbenzoyl)hydrazine 
• 22816-03-1 4-(1,3,4-oxadiazol-2-yl)benzoic acid methyl ester 
• 1609113-38-3 C₂₄H₂₃N₃O₆ 
• 1609112-76-6 C₂₂H₁₇N₃O₅ 
• 1609113-39-4 C₂₄H₂₁N₃O₅ 

Relevant academic research and scientific papers

Two polymorphic forms of 2,5-bis-(4-methoxycarbonylphenyl)-1,3,4-oxadiazole

The title compound [systematic name: dimethyl 4,4′-(1,3,4-oxadiazole-2,5-diyl)diphenylenedicarboxylate], C18H14N2O5, crystallizes under similar conditions in two different orthorhombic crystalline forms. In both

AROMATIC RING OR HETEROAROMATIC RING COMPOUNDS, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF

The present invention relates to aromatic ring or heteroaromatic ring compounds, a preparation method therefor and a medical use thereof. Particularly, the present invention relates to a compound as shown in general formula (I) and a preparation method th

Discovery of Novel Small-Molecule Inhibitors of NF-κB Signaling with Antiinflammatory and Anticancer Properties

Excessive NF-κB activation contributes to the pathogenesis of numerous diseases. Small-molecule inhibitors of NF-κB signaling have significant therapeutic potential especially in treating inflammatory diseases and cancers. In this study, we performed a ce

Antifungal benzo[b]thiophene 1,1-dioxide IMPDH inhibitors exhibit pan-assay interference (PAINS) profiles

Fungi cause serious life-threatening infections in immunocompromised individuals and current treatments are now complicated by toxicity issues and the emergence of drug resistant strains. Consequently, there is a need for development of new antifungal drugs. Inosine monophosphate dehydrogenase (IMPDH), a key component of the de novo purine biosynthetic pathway, is essential for growth and virulence of fungi and is a potential drug target. In this study, a high-throughput screen of 114,000 drug-like compounds against Cryptococcus neoformans IMPDH was performed. We identified three 3-((5-substituted)-1,3,4-oxadiazol-2-yl)thio benzo[b]thiophene 1,1-dioxides that inhibited Cryptococcus IMPDH and also possessed whole cell antifungal activity. Analogs were synthesized to explore the SAR of these hits. Modification of the fifth substituent on the 1,3,4-oxadiazole ring yielded compounds with nanomolar in vitro activity, but with associated cytotoxicity. In contrast, two analogs generated by substituting the 1,3,4-oxadiazole ring with imidazole and 1,2,4-triazole gave reduced IMPDH inhibition in vitro, but were not cytotoxic. During enzyme kinetic studies in the presence of DTT, nucleophilic attack of a free thiol occurred with the benzo[b]thiophene 1,1-dioxide. Two representative compounds with substitution at the 5 position of the 1,3,4-oxadiazole ring, showed mixed inhibition in the absence of DTT. Incubation of these compounds with Cryptococcus IMPDH followed by mass spectrometry analysis showed non-specific and covalent binding with IMPDH at multiple cysteine residues. These results support recent reports that the benzo[b]thiophene 1,1-dioxides moiety as PAINS (pan-assay interference compounds) contributor.

Discovery of highly selective and potent monoamine oxidase B inhibitors: Contribution of additional phenyl rings introduced into?2-aryl-1,3,4-oxadiazin-5(6H)-one

Monoamine oxidase B (MAO-B) is a flavin adenine dinucleotide (FAD)-containing enzyme that plays a major role in the oxidative deamination of biogenic amines and neurotransmitters. Inhibiting MAO-B activity is a promising approach in the treatment of neuro

PYRROL-1 -YL BENZOIC ACID DERIVATES USEFUL AS MYC INHIBITORS

The present invention provides compounds of Formula (I-A), (I-B), and (I-C), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting Myc (e.g., c-Myc) activity. The p

IMIDAZO-OXADIAZOLE AND IMIDAZO-THIADIAZOLE DERIVATIVES

The present invention provides compounds of Formula (I) used as Amyloid beta lowering agent for the treatment of neurodegenerative diseases.

Substituted Benzo-Pyrido-Triazolo-Diazepine Compounds

The present invention relates to substituted benzo-pyrido-triazolo-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-pyrido-triazolo-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.

Discovery of histone deacetylase 8 selective inhibitors

We have developed an efficient method for synthesizing candidate histone deacetylase (HDAC) inhibitors in 96-well plates, which are used directly in high-throughput screening. We selected building blocks having hydrazide, aldehyde and hydroxamic acid functionalities. The hydrazides were coupled with different aldehydes in DMSO. The resulting products have the previously identified 'cap/linker/biasing element' structure known to favor inhibition of HDACs. These compounds were assayed without further purification. HDAC8-selective inhibitors were discovered from this novel collection of compounds.

1,2,4-TRIAZOLE CARBOXYLIC ACID DERIVATIVES AS MODULATORS OF MGLUR5

The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.