20886-87-7Relevant academic research and scientific papers
Novel thiazole-thiophene conjugates as adenosine receptor antagonists: Synthesis, biological evaluation and docking studies
Pandya, Dhaivat H.,Sharma, Jayesh A.,Jalani, Hitesh B.,Pandya, Amit N.,Sudarsanam,Kachler, Sonja,Klotz, Karl Norbert,Vasu, Kamala K.
, p. 1306 - 1309 (2015)
Here we report novel thiazole-thiophene conjugates as adenosine receptor antagonists. All the molecules were evaluated for their binding affinity for adenosine receptors. Most of the molecules were found to interact with the A1, A2A and A3 adenosine receptor subtypes with good affinity values. The most potent and selective compound 8n showed an A3 Ki value of 0.33 μM with selectivity ratios of >90 versus the A1 and >30 versus the A2 subtypes. For compound 8n docking studies into the binding site of the A3 adenosine receptor are provided to visualize its binding mode.
PROTEASOME ACTIVITY MODULATING COMPOUNDS
-
Page/Page column 64, (2013/08/15)
The present invention is directed to compounds having the Formula (I), (la) or (Ib), compositions thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis.
Synthesis and biological evaluation of thiophene derivatives as acetylcholinesterase inhibitors
Ismail, Mohamed M.,Kamel, Mona M.,Mohamed, Lamia W.,Faggal, Samar I.,Galal, Mai A.
, p. 7217 - 7231 (2012/09/22)
A series of new thiophene derivatives has been synthesized using the Gewald protocol. The acetylcholinesterase inhibition activity was assayed according to Ellman's method using donepezil as reference. Some of the compounds were found to be more potent inhibitors than the reference. 2-(2-(4-(4-Methoxyphenyl) piperazin-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide (IIId) showed 60% inhibition, compared to only 40% inhibition by donepezil.
Synthesis and antimicrobial evaluation of some new thiophene derivatives
Khalil,Berghot,Abd El-Ghani, Ghada E.,Gouda
scheme or table, p. 1658 - 1669 (2010/08/03)
2-(2-Cyano-acetylamino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3- carboxamide(3) was used as starting material for synthesis of 4-thiazolidinone, thiazolidine, and thiophene derivatives 6, 7a, b, and 8a, b, respectively. Thiocarbomyl derivative 5, 4-thizolidinone 9, and thioxothiazolidine 10 were obtained from reaction of 3 with thioglycolic acid and phenyl isothiocyanate/sulfur, respectively. Condensation of 3 with selected cyclic ketones and aromatic aldehydes yielded the arylidine derivatives 11a, b and 13, respectively. Refluxing of 11a, b with sulfur and morpholine yielded the thiophene derivatives 12a, b, respectively. Diazocoupling of compound 3 withp-tolyl diazonium chloride yielded the hydrazone derivative 14. The newly synthesized compounds were characterized by infrared, 1H NMR, and mass spectral studies. Representative compounds of the synthesized product were tested and evaluated as antimicrobial agents. Compound 12b gives very high antimicrobial activity against Ampicillin. Copyright
2-(3,4-dihydro-4-oxothieno[2,3-d]pyrimidin-2-ylthio) acetamides as a new class of falcipain-2 inhibitors. 3. design, synthesis and biological evaluation
Zhu, Jin,Chen, Tong,Liu, Jie,Ruoqun, Ma.,Lu, Weiqiang,Huang, Jin,Li, Honglin,Li, Jian,Jiang, Hualiang
experimental part, p. 785 - 797 (2009/05/27)
The cysteine protease falcipain-2 (FP-2) of Plasmodium falciparum is a principal cysteine protease and an essential hemoglobinase of erythrocytic P. falciparum trophozoites, making it become an attractive target enzyme for developing anti-malarial drugs.
Thienopyrimidines as hetryl moiety in 2-azetidinones: Synthesis of 4-hetryl-2-azetidinones
Kanwar, Seema,Sharma
, p. 2367 - 2371 (2007/10/03)
A Facile and efficient method for the synthesis of 4-hetryl substituted β-lactams 1 have been reported from substituted thienopyrimidinone 2b, which in turn was prepared from appropriately substituted 2-amino-3-carboxamido thiophene 10. The structures of
