18330-76-2Relevant articles and documents
Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents
Andreotti, Elisa,Baldisserotto, Anna,Balzarini, Jan,Buzzi, Raissa,Dissette, Valeria,Djuidje, Ernestine Nicaise,Liekens, Sandra,Manfredini, Stefano,Sciabica, Sabrina,Serra, Elena,Vertuani, Silvia
, (2020/06/22)
Oxidative stress is the product or aetiology of various multifactorial diseases; on the other hand, the development of multifunctional compounds is a recognized strategy for the control of complex diseases. To this end, a series of benzothiazole derivatives was synthesized and evaluated for their multifunctional effectiveness as antioxidant, sunscreen (filter), antifungal and antiproliferative agents. Compounds were easily synthesized via condensation reaction between 2-aminothiophenols and different benzaldehydes. SAR study, particularly in position 2 and 6 of benzothiazoles, led to the identification of 4g and 4k as very interesting potential compounds for the design of multifunctional drugs. In particular, compound 4g is the best blocker of hERG potassium channels expressed in HEK 293 cells exhibiting 60.32percent inhibition with IC50 = 4.79 μM.
Synthesis and evaluation of18F-labeled 2-phenylbenzothiazoles as positron emission tomography imaging agents for amyloid plaques in alzheimer's disease
Serdons, Kim,Terwinghe, Christelle,Vermaelen, Peter,Van Laere, Koen,Kung, Hank,Mortelmans, Luc,Bormans, Guy,Verbruggen, Alfons
experimental part, p. 1428 - 1437 (2009/12/26)
Imaging agents targeting amyloid β(Aβ) may be useful for early diagnosis and follow-up of treatment of patients with Alzheimer's disease (AD). Three of five tested 2-(4′-fluorophenyl)-1,3-benzothiazoles displayed high binding affinities for Aβ plaques in
Optimization of a coagulation factor VIIa inhibitor found in factor Xa inhibitor library
Sagi, Kazuyuki,Fujita, Koichi,Sugiki, Masayuki,Takahashi, Mitsuo,Takehana, Shunji,Tashiro, Kazumi,Kayahara, Takashi,Yamanashi, Masahiro,Fukuda, Yumiko,Oono, Seiji,Okajima, Akiko,Iwata, Seinosuke,Shoji, Masataka,Sakurai, Kuniya
, p. 1487 - 1496 (2007/10/03)
An inhibitor of the complex of factor VIIa and tissue factor (fVIIa/TF), 2-substituted-4-amidinophenylpyruvic acid 1a, was structurally modified with the aim of increasing its potency and selectivity. The lead compound 1a was originally found in our factor Xa (fXa) inhibitor library on the basis of structural similarity of the primary binding sites of fVIIa and fXa. The design was based on computational docking studies using the extracted active site of fVIIa. Compound 1j was found to inhibit factor VIIa/TF at nanomolar concentration with improved selectivity versus fXa and thrombin and it preferentially prolonged the clotting time in the TF-dependent extrinsic pathway.