35357-56-3

Usage

Synthesis Reference(s)

Journal of Heterocyclic Chemistry, 21, p. 215, 1984 DOI: 10.1002/jhet.5570210143Synthesis, p. 143, 1985

Upstream product

• 35355-52-3 ethyl 2-azido-3-(thiophen-3-yl)acrylate 
• 335030-68-7 ethyl (Z)-2-azido-3-(3-thienyl)prop-2-enoate 
• 498-62-4 3-thiophene carboxaldehyde 
• 637-81-0 ethyl-2-azidoacetate 

Downstream Products

• 51856-25-8 6H-thieno[2,3-b]pyrrole-5-carboxylic acid 
• 332099-01-1 2-Chloro-6H-thieno[2,3-b]pyrrole-5-carboxylic acid ethyl ester 
• 1007387-91-8 ethyl 2-(4-chlorobenzoyl)-6H-thieno[2,3-b]pyrrole-5-carboxylate 
• 250-79-3 6H-thieno[2,3-b]pyrrole 

Relevant academic research and scientific papers

INDOLE AND AZAINDOLE COMPOUNDS WITH SUBSTITUTED 6-MEMBERED ARYL AND HETEROARYL RINGS AS AGROCHEMICAL FUNGICIDES

The present invention relates to heteroaryl compounds of formula (Ia) or a compound in the form of a stereoisomer, an agriculturally acceptable salt, a tautomer,an isotopic form, a N-oxide or a S-oxide thereof. The present invention further relates to the use of a compound of formula (I) or an agriculturally acceptable salt, a stereoisomer, a tautomer, an isotopic form, a derivative or mixture thereof, as fungicide.

New tetracyclic compound

The invention relates to a new tetracyclic compound. The tetracyclic compound has a structure shown in the formula (III) and can be used as a bromine domain and additional terminal (BET) inhibitor. The invention further relates to synthesis and application of the compounds in disease treatment. More specifically, the invention relates to a fused heterocyclic derivative used as a BET inhibitor, a method for the preparation of these compounds, and a disease and symptom treatment method conductive to inhibition of one or more BET bromine domains.

Peptidylarginine deiminase inhibitor and application thereof

The invention belongs to the technical field of medicine, and particularly relates to a peptidylarginine deiminase PAD4 inhibitor compound shown in a formula (I) or pharmaceutically acceptable salts,stereoisomers and tautomers thereof, as well as pharmaceutical compositions, pharmaceutical preparations and application thereof. X, Y, R1, R2, R3, R4, R5, R7, R8, R9, ring B and m are as defined in the specification. The compound has inhibitory effect on peptidylarginine deiminase PAD4, and can be used for treating various diseases, such as rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, multiple sclerosis, cystic fibrosis, cancer, cutaneous lupus erythematosus, asthma and psoriasis.

Thieno[3,2-b]pyrrole-5-carboxamides as New Reversible Inhibitors of Histone Lysine Demethylase KDM1A/LSD1. Part 1: High-Throughput Screening and Preliminary Exploration

Lysine specific demethylase 1 KDM1A (LSD1) regulates histone methylation and it is increasingly recognized as a potential therapeutic target in oncology. We report on a high-throughput screening campaign performed on KDM1A/CoREST, using a time-resolved fluorescence resonance energy transfer (TR-FRET) technology, to identify reversible inhibitors. The screening led to 115 hits for which we determined biochemical IC50, thus identifying four chemical series. After data analysis, we have prioritized the chemical series of N-phenyl-4H-thieno[3, 2-b]pyrrole-5-carboxamide for which we obtained X-ray structures of the most potent hit (compound 19, IC50 = 2.9 μM) in complex with the enzyme. Initial expansion of this chemical class, both modifying core structure and decorating benzamide moiety, was directed toward the definition of the moieties responsible for the interaction with the enzyme. Preliminary optimization led to compound 90, which inhibited the enzyme with a submicromolar IC50 (0.162 μM), capable of inhibiting the target in cells.

Structural Optimizations of Thieno[3,2-b]pyrrole Derivatives for the Development of Metabolically Stable Inhibitors of Chikungunya Virus

Chikungunya virus (CHIKV) is a re-emerging vector-borne alphavirus, and there is no approved effective antiviral treatment currently available for CHIKV. We previously reported the discovery of thieno[3,2-b]pyrrole 1b that displayed good antiviral activit

FLUORESCENT COMPOUND AND LABELING AGENT COMPRISING THE SAME

A novel fluorescent compound having a high light fastness, high fluorescence quantum yield and sharp absorption spectrum, which emits fluorescence having a wavelength in long wavelength region, as well as its use as a labeling agent, is disclosed. In Form

FLUORO-SUBSTITUTED INHIBITORS OF D-AMINO ACID OXIDASE

This invention provides novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CR1 and N. X and Y are members independently selected from O, S, CR2, N and NH. R1, R2 and R4 are members independently selected from H and F, provided that at least one member selected from R1, R2 and R4 is F. R6 is a member selected from O?X+ and OH, wherein X+ is a positive ion, which is a member selected from inorganic positive ions and organic positive ions.

The discovery of fused pyrrole carboxylic acids as novel, potent d-amino acid oxidase (DAO) inhibitors

The 'NMDA hypofunction hypothesis of schizophrenia' can be tested in a number of ways. DAO is the enzyme primarily responsible for the metabolism of d-serine, a co-agonist for the NMDA receptor. We identified novel DAO inhibitors, in particular, acid 1, which demonstrated moderate potency for DAO in vitro and ex vivo, and raised plasma d-serine levels after dosing ip to rats. In parallel, analogues were prepared to survey the SARs of 1.

Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: Potent human histamine H4 antagonists

Three series of H4 receptor ligands,- derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H 4 receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [3H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H4 antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.

FAB I INHIBITORS

Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.