39827-12-8Relevant articles and documents
Synthesis and pharmacological activity of benzo[b]thiophene-3-carboxylic acid derivatives
Shafiee,Hedayati,Salimi,Faghihi
, p. 198 - 202 (1983)
Several dialkylaminoethyl benzo[b]thiophene-3-carboxylates, N-(2-dialkylaminoethyl)benzo[b]thiophene-3-carboxamides, 2-dialkylaminoethyl benzo[b]thiophene-3-carbamates, and substituted ureas with benzo[b]thiophene moiety, were prepared and tested for local anesthetic, anticholinergic, and antihistaminic activities. Several of the compoundds showed significant activity.
Development of a Library of Thiophene-Based Drug-Like Lego Molecules: Evaluation of Their Anion Binding, Transport Properties, and Cytotoxicity
Vieira, Paulo,Miranda, Margarida Q.,Marques, Igor,Carvalho, Sílvia,Chen, Li-Jun,Howe, Ethan N. W.,Zhen, Carl,Leung, Claudia Y.,Spooner, Michael J.,Morgado, Bárbara,da Cruz e Silva, Odete A. B.,Moiteiro, Cristina,Gale, Philip A.,Félix, Vítor
, p. 888 - 899 (2020)
The anion-binding and transport properties of an extensive library of thiophene-based molecules are reported. Seventeen bis-urea positional isomers, with different binding conformations and lipophilicities, have been synthesized by appending α- or β-thiophene or α-, β-, or γ-benzo[b]thiophene moieties to an ortho-phenylenediamine central core, yielding six subsets of positional isomers. Through 1H NMR, X-ray crystallography, molecular modelling, and anion efflux studies, it is demonstrated that the most active transporters adopt a pre-organized binding conformation capable of promoting the recognition of chloride, using urea and C?H binding groups in a cooperative fashion. Additional large unilamellar vesicle-based assays, carried out under electroneutral and electrogenic conditions, together with N-methyl-d-glucamine chloride assays, have indicated that anion efflux occurs mainly through an H+/Cl? symport mechanism. On the other hand, the most efficient anion transporter displays cytotoxicity against tumor cell lines, while having no effects on a cystic fibrosis cell line.
Heterocyclic compound and preparation and application thereof
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Paragraph 0297-0299, (2020/07/24)
The invention relates to bromodomain inhibitors, and provides a compound represented by a general formula I, a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method thereof, a pharmaceutical composition containing the same, and applicationthereof in pharmacy.
