99584-10-8Relevant articles and documents
NOVEL HYDRAZONE DERIVATIVE WITH ARYL OR HETEROARYL GROUP SUBSTITUTED AT TERMINAL AMINE GROUP THEREOF AND USE THEREOF
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Paragraph 0362-0363; 0370-0371, (2021/11/04)
The present invention relates to novel hydrazone derivatives in which a terminal amine group is substituted with an aryl group or a heteroaryl group, and uses thereof.
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.
Novel hydrazone derivatives comprising aryl or heteroaryl group substituted at terminal amine and use thereof
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Paragraph 1702; 1708; 1709; 1740; 1746-1748, (2020/08/28)
The present invention relates to novel hydrazone derivatives with an aryl or heteroaryl group substituted at a terminal amine group thereof and a use thereof.
Comparative study of conventional and microwave-assisted synthesis of novel 6-(arylideneamino)benzo[d]oxazol-2(3H)-ones with potential antibacterial activity
Adjeroud, Yasmina,Chabane, Hanane,Liacha, Messaoud
, p. 111 - 117 (2016/07/15)
(Formula presented) The synthesis and characterization of novel class of Schiff bases derivatives 6-(Benzylideneamino)benzo[d]oxazol-2(3H)-ones (5a-d and 6a-d), derived from the condensation reactions of different aromatic aldehydes with 6-amino-2(3H)-benzoxazolone and 3-methyl-6-amino-2(3H)-benzoxazolone, using conventional and microwave irradiation methods was described. The structure of all newly synthesized compounds has been proven by using various spectral methods such as IR, 1H-NMR and 13C-NMR. The results confirmed that benzoxazolinonic amino group reacted with aromatic aldehydes to form the desired Schiff bases.
Experimental and theoretical investigation of the intramolecular cyclisation of N-(benzoxazolinon-6-Yl) Maleimide derivatives
Yahia, Wassila,Nacereddine, Abdelmalek Khorief,Seddiki, Khemissi,Liacha, Messaoud,Nippert
, p. 853 - 859 (2015/11/24)
A new N-H and N-CH3 2(3H)-benzoxazolones substituted at the C6 position in the aromatic ring by imide group (maleimides) has been synthesized in good yields. The regioselectivity of the cyclisation step has been investigated through DFT calculations at the B3LYP/6-31G (d,p) level of theory. The obtained results indicate that the maleimide is favored both kinetically and thermodynamically as observed experimentally.
Synthesis of some new urea and thiourea derivatives and evaluation of their antimicrobial activities
Guelkok, Yildiz,Bicer, Tuba,Onurdag, Fatma Kaynak,Oezgen, Selda,Sahin, Mustafa Fethi,Dogruer, Deniz Songuel
experimental part, p. 279 - 291 (2012/06/16)
In the present study, 18 new compounds were synthesized, 9 of which were urea (9a-e, 10a-d) while the others were thiourea (11a-e, 12a-d) derivatives. These derivatives were prepared by the reaction of 6-amino-5-nonsubstituted/ chloro-3-methyl-2(3H) -benzoxazolones used as key intermediates with the appropriate isocyanates and isothiocyanates. The chemical structures of new compounds were confirmed by 1H-NMR, mass, and elemental analysis. The synthesized compounds were screened for their antibacterial and antifungal activities against some pathogenic strains. Compounds 9a, 9b, 9e, 10a, and 10c, urea derivatives, and compounds 12a and 12d, thiourea derivatives, exhibited a relatively good inhibitory profile against E. coli, with a MIC value of 32 ig/mL when compared with the other target compounds.
2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Page 54, (2008/06/13)
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
N-ARYL-2-OXAZOLIDINONE-5-CARBOXAMIDES AND THEIR DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
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Page/Page column 115, (2010/02/07)
Compounds of formula B-C-A-CO-NH-R1, wherein A is structure i, ii or iii: formulae (I), (II), (III). C is optionally substituted aryl or heteroaryl, and B is a specified cyclic moiety, or C and B together are a heterobicyclic moiety, are useful as antibacterial agents.
