124078-87-1Relevant 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)
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.
Design and synthesis of some new carboxamide and propanamide derivatives bearing phenylpyridazine as a core ring and the investigation of their inhibitory potential on in-vitro acetylcholinesterase and butyrylcholinesterase
Kilic, Burcu,Gulcan, Hayrettin O.,Aksakal, Fatma,Ercetin, Tugba,Oruklu, Nihan,Umit Bagriacik,Dogruer, Deniz S.
, p. 235 - 249 (2018/05/24)
A series of new carboxamide and propanamide derivatives bearing phenylpyridazine as a core ring were designed, synthesized and evaluated for their ability to inhibit both cholinesterase enzymes. In addition, a series of carboxamide and propanamide derivat
Novel quinazolinone derivatives as 5-HT7 receptor ligands
Na, Yong Ho,Hong, Sung Ho,Lee, Jung Hyang,Park, Woo-Kyu,Baek, Du-Jong,Koh, Hun Yeong,Cho, Yong Seo,Choo, Hyunah,Pae, Ae Nim
, p. 2570 - 2578 (2008/09/21)
5-HT7 receptor antagonists generated antidepressant-like effects in animal model and the involvement of the 5-HT7 receptor in other pathophysiological mechanisms such as thermoregulation, learning and memory, and sleep has been highl
1,2-DIHYDRO-1-OXOPHTHALAZINYL DERIVATIVES HAVING BIOLOGICAL ACTIVITY ON SEROTONIN RECEPTORS 5-HT2A AND 5-HT2C, AND PREPARATION THEREOF
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Page/Page column 23, (2008/12/07)
The present invention relates to a novel 1,2-dihydro-1-oxophthalazinyl piperazine compound having biological activity as serotonin receptor antagonist, a preparation method of the compound and a pharmaceutical composition for the treatment and prevention of central nervous system diseases comprising the compound.
Nitrogen-based camptothecin derivatives
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, (2008/06/13)
(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.
Nitrogen-based camptothecin derivatives
-
, (2008/06/13)
(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.
NITROGEN-BASED HOMO-CAMPTOTHECIN DERIVATIVES
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Page 46-48, (2008/06/13)
(20) esters of camptothecin analogs are provided. The compounds are (20) esters of an aminoalkanoic acid or an imidoalkanoic acid and homocamptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the homocamptothecin ring. The
Nitrogen-based camptothecin derivatives
-
, (2008/06/13)
(20S) esters of camptothecin analogs are provided. The compounds are (20S) esters of an aminoalkanoic acid or an imidoalkanoic acid and camptothecin, which is optionally substituted at the 7, 9, 10, 11, and 12 positions of the camptothecin ring. The compounds are useful for treating cancer.