329221-38-7Relevant academic research and scientific papers
New method for the synthesis of 2-acylamino-1-benzothiophene-3-carboxamide derivatives from the corresponding esters
Banhegyi, Peter,Waczek, Frigyes,Szekelyhidi, Zsolt,Hegymegi-Barakonyi, Balint,Keri, Gyoergy,Orfi, Laszlo
, p. 3270 - 3276 (2008)
An unusual chemical method has been applied for the preparation of 1-benzothiophene-3-carboxamide derivatives from esters by reaction with lithium amide in tetrahydrofurane. Copyright Taylor & Francis Group, LLC.
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis
Samala, Ganesh,Brindha Devi, Parthiban,Saxena, Shalini,Gunda, Saritha,Yogeeswari, Perumal,Sriram, Dharmarajan
, p. 5556 - 5564 (2016/10/24)
Thirty three derivatives of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues were synthesized by molecular modification of a reported antimycobacterial molecule (GSK163574A). Compounds were evaluated in vitro against actively replicative and nutrient starved non-replicative Mycobacterium tuberculosis (MTB), enzymatic screening and cytotoxicity against RAW 264.7 cell line. Among the compounds, 2-ethyl-N-phenethyl-5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine (5c) was found to be the most active compound against non-replicative MTB with 2.7 log reduction of bacteria at 10?μg/mL and was more potent than isoniazid (1.2 log reduction) and rifampicin (2.0 log reduction) at same dose level. Compound 5c also showed activity against MTB alanine dehydrogenase enzyme with IC50of 1.82?±?0.42?μM and showed 25% cytotoxicity against RAW 264.7 cell line at 50?μg/mL.
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3
Patch, Raymond J.,Baumann, Christian A.,Liu, Jian,Gibbs, Alan C.,Ott, Heidi,Lattanze, Jennifer,Player, Mark R.
, p. 3282 - 3286 (2007/10/03)
A series of 2-acylaminothiophene-3-carboxamides has been identified which exhibit potent inhibitory activity against the FLT3 tyrosine kinase. Compound 44 inhibits the isolated enzyme (IC50 = 0.027 μM) and blocks the proliferation of MV4-11 cel
HETEROBICYCLIC COMPOUNDS AS PHARMACEUTICALLY ACTIVE AGENTS
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Page/Page column 113, (2010/02/11)
Described are heterobicyclic compounds such as 4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran- 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene
