102609-56-3Relevant academic research and scientific papers
Hyperbolic mixed-type inhibition of acetylcholinesterase by tetracyclic thienopyrimidines
Gonzalez Tanarro,Guetschow
scheme or table, p. 350 - 358 (2012/02/14)
A series of tetracyclic thienopyrimidines (7-14) was prepared and investigated as inhibitors of acetylcholinesterase from Electrophorus electricus acetylcholinesterase (EeAChE), as well as human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). A new synthetic procedure was employed for the synthesis of the angularly fused heterocycles 7-10. Among them, the presence of a tetrahydropyrido ring with a benzyl rest at the basic nitrogen was required for EeAChE inhibition. A detailed kinetic analysis of the hyperbolic mixed-type inhibition of EeAChE by 9-14 was performed. These heterocyclic compounds inhibited EeAChE with Ki values of less than 3 μM. Most α values were relatively close to 1, indicating a similar affinity of the inhibitor to the free enzyme and the enzyme-substrate complex. Inhibitor 10 displayed a rather uncompetitive pattern of inhibition (α=0.47) and a relatively high residual activity of a postulated ternary enzyme-substrate- inhibitor complex (β=0.24).
Synthesis, characterization and biological studies of some novel thieno[2,3-d]pyrimidines
Al-Taisan, Khulud M.,Al-Hazimi, Hassan M. A.,Al-Shihry, Shar S.
experimental part, p. 3932 - 3957 (2010/09/18)
Several 2-unsubstituted thieno[2,3-d]pyrimidines have been prepared from 2-aminothiophene-3-carboxylic acid esters and their carbonitrile analogs. Some triazolothienopyrimidine and 2-thioxothienopyrimidine representatives have also been synthesized using
Synthesis of tricyclic 1,3-oxazin-4-ones and kinetic analysis of cholesterol esterase and acetylcholinesterase inhibition
Pietsch, Markus,Gütschow, Michael
, p. 8270 - 8288 (2007/10/03)
A series of thieno[1,3]oxazin-4-ones and thieno[1,3]thiazin-4-ones were synthesized and investigated as inhibitors of the α/β hydrolases cholesterol esterase (CEase) and acetylcholinesterase (AChE). The introduction of a cycloaliphatic five- or six-member
The Facile Synthesis of 2-Aminothienothiazin-4-ones, in Some Cases 5,6-Anelated
Leistner, Siegfried,Guetschow, Michael,Wagner, Guenther
, p. 466 - 470 (2007/10/02)
The cyclization of ethyl 2-thioureidothiophene-3-carboxylates is known to give 2-thioxothienopyrimidin-4-ones not only under basic conditions but also upon treatment with ethanolic hydrochloric acid.On the other hand, we have found that ethyl 2-thi
