53421-88-8Relevant articles and documents
Design, synthesis and biological evaluation of new benzoxazolone/benzothiazolone derivatives as multi-target agents against Alzheimer's disease
Erdogan, Merve,Kilic, Burcu,Sagkan, Rahsan Il?kc?,Aksakal, Fatma,Ercetin, Tugba,Gulcan, Hayrettin O.,Dogruer, Deniz S.
, (2021/01/05)
In this study, four series of compounds with benzoxazolone and benzothiazolone cores were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease (AD). Additionally, in order to shed light on the effect of the carbonyl groups of benzoxazolone/benzothiazolone, benzoxazole/benzothiazole-containing analogues were also synthesized and evaluated. Inhibition potency of all final compounds towards cholinesterase enzymes and their antioxidant activity were tested. Subsequently, the anti-inflammatory activity, cytotoxicity, apoptosis, and Aβ aggregation inhibition tests were also performed for selected compounds. The results indicated that compounds 11c, a pentanamide derivative with benzothiazolone core, and 14b, a keton derivative with benzothiazolone core, were considered as promising multi-functional agents for further investigation against AD. The reversibility, kinetic and molecular docking studies were also performed for the compounds with the highest AChE 14b (eeAChE IC50 = 0.34 μM, huAChE IC50 = 0.46 μM) and BChE 11c (eqBChE IC50 = 2.98 μM, huBChE IC50 = 2.56 μM) inhibitory activities.
Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2- phenylbenzo[d]oxazoles as potential anticonvulsant agents
Wei, Cheng-Xi,Wu, Di,Sun, Zhi-Gang,Chai, Kyu-Yun,Quan, Zhe-Shan
, p. 925 - 935 (2011/12/01)
A series of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d] oxazoles was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (Sc-PTZ), and
Novel anti-inflammatory and analgesic heterocyclic amidines that inhibit nitrogen oxide (NO) production
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Page/Page column 34, (2010/02/13)
Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which:G1 and G2 are hydrogen, halogen, hydroxyl, C1-C4 alkoxy, C1-C4 alkyl, and an amidino substituent of formula Q, provided that, for each compound of formula (I), only one of the two substituents G1 or G2 is an amidino substituent of formula Q: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; andZ is an aryl or heteroaryl group, a linear or branched C1-C6 alkyl or alkenyl chain, a C1-C4 alkyl-aryl group or a C1-C4 alkyl-heteroaryl group.