307538-54-1Relevant articles and documents
UiO-66-NH2as an effective solid support for quinazoline derivatives for antibacterial agents against Gram-negative bacteria
Al Blooshi, Afra G.,Al Neyadi, Shaikha S.,Alnaqbi, Mohamed. A.,Nguyen, Ha L.
, p. 20386 - 20395 (2021/12/02)
Nanomaterials have been widely used as a class of antibacterial drugs. However, the bottlenecks of this class of materials are their significant aggregation and accumulation, as well as toxicity resulting from excessive metal leaching. Metal-organic frameworks (MOFs) have inspired researchers owing to their distinct characteristics of robust architecture and tunable pore structures, which may help overcome the above challenges. We, herein, synthesize UiO-66-NH2 and use it as a solid support for loading quinazoline derivatives that are specifically designed and active against Gram-negative bacteria. The quinazoline derivatives were adsorbed on UiO-66-NH2 nanoparticles to form new UiO-66-NH2-quinazoline formulations which have a large inhibitory zone against Gram-negative bacteria, compared to that of free quinazoline compounds. This work has the potential for increasing antibacterial activity while also broadening the antibacterial range, and thus opens a pathway for new medical applications using MOFs. This journal is
Potent inhibitors of Huntingtin protein aggregation in a cell-based assay
Rinderspacher, Alison,Cremona, Maria Laura,Liu, Yidong,Deng, Shi-Xian,Xie, Yuli,Gong, Gangli,Aulner, Nathalie,Toebben, Udo,Myers, Katherine,Chung, Caty,Andersen, Monique,Vidovic, Dusica,Schuerer, Stephan,Branden, Lars,Yamamoto, Ai,Landry, Donald W.
experimental part, p. 1715 - 1717 (2009/12/03)
A quinazoline that decreases polyglutamine aggregate burden in a cell-based assay was identified from a high-throughput screen of a chemical-compound library, provided by the NIH Molecular Libraries Small Molecule Repository (MLSMR). A structure and activ
NITROGENOUS FUSED?RING COMPOUND HAVING PYRAZOLYL GROUP AS SUBSTITUENT AND MEDICINAL COMPOSITION THEREOF
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Page 340, (2008/06/13)
The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. Inparticular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, X represents a nitrogen-containing condensed aromatic heterocyclic group such as imidazo[1,2-a]pyridine, benzimidazole, quinazoline, quinoline, or 2,1-benzisoxazole and has (R4)n as substituent groups; Y represents a C3-8 cycloalkyl group, C4-8 cycloalkenyl group, 5- to 14-membered non-aromatic heterocyclic group, C6-14 aromatic hydrocarbon cyclic group or 5- to 14-membered aromatic heterocyclic group; n in (R4)n is 0, 1, 2 or 3, and Z groups independently represent (1) hydrogen atom, (2) amino group, (3) halogen atom, (4) hydroxyl group, (5) nitro group, (6) cyano group, (7) azido group, (8) formyl group, (9) hydroxyamino group, (10) sulfamoyl group, (11) guanodino group, (12) oxo group, (13) C2-6 alkenyl group, (14) C1-6 alkoxy group, (15) C1-6 alkylhydroxyamino group, (16) halogenated C1-6 alkyl group, (17) halogenated C2-6 alkenyl group, (18) (i) C3-7cycloalkyl group, (ii) C3-7cycloalkenyl group, (iii) 5- to 14-membered non-aromatic heterocyclic group, each of which may have one or more substituent groups Q, or (19) formula -M1-M2-M3, R1 represents (1) hydrogen atom, (2) halogen atom, (3) hydroxyl group, (4) nitro group, (5) cyano group, (6) halogenated C1-6 alkyl group, (7) C2-6 alkyl group substituted with a hydroxyl or cyano group, (8) C2-6 alkenyl group, or (9) formula -L1-L2-L3, and R2 represents a hydrogen atom or a protecting group; and R3 represents a hydrogen atom, halogen atom, cyano group, amino group, C1-4 alkyl group or halogenated C1-4 alkyl group.