- A new multifunctional sensor for sequential recognizing of Zn2+ and PPi in acetonitrile solution and detection of In3+ in DMF solution
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A simple multifunctional sensor, X, was designed and synthesized based on 8-hydroxy-2,3,6,7-tetrahydro-1H,5H-pyrido[3,2,1-ij]quinoline-9-carbaldehyde and imidazo[2,1-b]thiazole, which could sequentially identify Zn2+ and PPi in acetonitrile buffer solution through the presence or absence of fluorescent signals and could detect In3+ in DMF buffer solution with obvious fluorescence enhancement. The detection limit for Zn2+, PPi and In3+ were calculated to be 4.58 × 10?8 M, 1.07 × 10?8 M and 2.9 × 10?8 M, respectively. Moreover, X could quantitatively detect Zn2+, PPi and In3+ in real water samples with the satisfactory recovery rate (90.1 %–97.6 %) and RSD (0.86 %–3.09 %). In addition, the complexation ratio between X and metal ions (Zn2+ and In3+) was 1:1, which was proved by mass spectrometry titration. The binding mode and sensing mechanism of X to metal ions (Zn2+ and In3+) were verified by Gaussian calculation based on B3LYP/6-31 G(d) and B3LYP/LanL2DZ basis set.
- Pei, Meishan,Wang, Hanyu,Xu, Yuankang,Yang, Xiaofeng,Yuan, Shufang,Zhang, Guangyou,Zhang, Yanxia
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- A selective "turn-on" sensor for recognizing In3+ and Zn2+ in respective systems based on imidazo[2,1-: B] thiazole
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A new simple and easily synthesized multitarget sensor, (E)-N′-(4-(diethylamino)-2-hydroxybenzylidene)imidazo[2,1-b]thiazole-6-carbohydrazide (X), was designed and synthesized using imidazo[2,1-b]thiazole-6-carboxylic acid and 4-(diethylamino)-2-hydroxybenzaldehyde. X could be used as a sensor to detect In3+ in DMF-H2O buffer solution and detect Zn2+ in EtOH-H2O buffer solution through fluorescence enhancement with detection limits of 1.02 × 10-9 M and 5.5 × 10-9 M, respectively. X exhibited an efficient "off-on-off" fluorescence behavior by cyclic addition of metal ions (In3+ and Zn2+) and EDTA. The stoichiometry between X and metal ions (In3+ and Zn2+) was 1:1. The binding mode and sensing mechanism of X with metal ions (In3+ and Zn2+) was verified by theoretical calculations using Gaussian 09 based on B3LYP/6-31G(d) and B3LYP/LANL2DZ basis, respectively. Moreover, X could be applied as a potential sensor for the quantitative detection of In3+ and Zn2+ with a satisfactory recovery and relative standard deviation (RSD) in real water samples.
- Xu, Yuankang,Zhao, Songfang,Zhang, Yanxia,Wang, Hanyu,Yang, Xiaofeng,Pei, Meishan,Zhang, Guangyou
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- A simple sensor based on imidazo[2,1-b]thiazole for recognition and differentiation of Al3+, F? and PPi
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Based on imidazo[2,1-b]thiazole and 2,3-dihydroxybenzaldehyde, a simple sensor, (E)-N'-(2,3-dihydroxybenzylidene)imidazo[2,1-b]thiazole-6-carbohydrazide (X), was designed and synthesized and its fluorescence responses to various ions were explored in DMF/
- Consty, Zoualou Arvel,Xu, Yuankang,Zhang, Yanxia
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- A new “off-on-off” sensor for sequential detection of Al3+ and Cu2+ with excellent sensitivity and selectivity based on different sensing mechanisms
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A new simple Schiff base, (E)-N'-(2-hydroxybenzylidene)imidazo[2,1-b]thiazole-6-carbohydrazide (X), was designed and synthesized based on salicylaldehyde and imidazo[2, 1-b]thiazole. X could be used as a sensor to identify Al3+ through a significant fluorescence enhancement because of CHEF and inhibition of PET process and then to detect Cu2+ through a highly efficient quenching behavior due to the paramagnetic quenching. The sensor showed a high selectivity for Al3+ and Cu2+ in methanol solution at pH = 5 and was not disturbed by other competing metal ions. Furthermore, based on the equation 3σ/slope, the detection limits of sensor for Al3+ and Cu2+ were calculated to be 3.1 × 10?10 M and 9.8 × 10-11 M, respectively. Additionally, the association constants of X[Al3+] and X[Cu2+] were also determined to be 2.3 × 104 M-1 and 6.1 × 104 M-1 on basis of Benesi-Hildebrand equation. In addition, the titration experiment of fluorescence and mass spectrometry showed that sensor was combined with Al3+ or Cu2+ both in 1:1 ratio. Moreover, the optimized structure and energy calculations of X, X[Al3+] and X[Cu2+] were obtained by Gaussian software based on the basis set of B3LYP/6?31 G(d) and B3LYP/LANL2DZ. And, the sensor successfully detected Al3+ and Cu2+ in the real water sample with a satisfactory recovery (91.4 % - 107.1 %) and RSD values (0.66 % - 1.91 %).
- Xu, Yuankang,Yang, Lei,Wang, Hanyu,Zhang, Yanxia,Yang, Xiaofeng,Pei, Meishan,Zhang, Guangyou
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- A simple fluorescent schiff base for sequential detection of Zn2+ and PPi based on imidazo[2,1-b]thiazole
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A simple fluorescent schiff base, X, based on imidazo[2,1-b]thiazole-6-carboxylic acid and 3-ethoxy-2-hydroxybenzaldehyde, was designed and synthesized for detection of Zn2+ and PPi. X showed excellent sensitivity and selectivity toward Zn
- Xu, Yuankang,Wang, Hanyu,Zhao, Jinyan,Yang, Xiaofeng,Pei, Meishan,Zhang, Guangyou,Zhang, Yanxia,Lin, Li
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- A dual functional fluorescent sensor for the detection of Al3+ and Zn2+ in different solvents
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(E)-N′-((2-Hydroxynaphthalen-1-yl)methylene)imidazo[2,1-b]thiazole-6-carbohydrazide (X), a new fluorescent sensor, was designed and synthesized based on imidazo[2,1-b]thiazole and 2-hydroxy-1-naphthaldehyde, which could be used to detect Al3+ in methanol buffer solution and detect Zn2+ in ethanol buffer solution with detection limits of 1.45 × 10-7 M and 1.29 × 10-8 M, respectively. X showed high sensitivity and selectivity towards Al3+ and Zn2+ in the presence of other metal ions. The fluorescence intensity of X was reversible even after six cycles with the sequentially alternative addition of metal ions (Al3+ and Zn2+) and PPi, showing an efficient "off-on-off" fluorescence behavior. The complexation ratio of X to Al3+ and Zn2+ was 1:1, which was proved by mass spectrometry and the B-H equation. The binding mode and sensing mechanism of X with metal ions (Al3+ and Zn2+) were verified by DFT/TDDFT calculations using Gaussian 09 based on the B3LYP/6-31G(d) basis set.
- Xu, Yuankang,Wang, Hanyu,Zhao, Jinyan,Yang, Xiaofeng,Pei, Meishan,Zhang, Guangyou,Zhang, Yanxia
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- Imidazole [2, 1-b] thiazole derivative as well as preparation method and application thereof
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The invention belongs to the field of chemical pharmaceuticals, and particularly relates to an imidazole [2, 1-b] thiazole derivative as well as a preparation method and an application thereof. The structure of the imidazole [2, 1-b] thiazole derivative i
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Paragraph 0117; 0118
(2017/01/02)
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- Discovery of imidazo[2,1- b ]thiazole HCV NS4B inhibitors exhibiting synergistic effect with other direct-acting antiviral agents
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The design, synthesis, and SAR studies of novel inhibitors of HCV NS4B based on the imidazo[2,1-b]thiazole scaffold were described. Optimization of potency with respect to genotype 1b resulted in the discovery of two potent leads 26f (EC50 = 16
- Wang, Ning-Yu,Xu, Ying,Zuo, Wei-Qiong,Xiao, Kun-Jie,Liu, Li,Zeng, Xiu-Xiu,You, Xin-Yu,Zhang, Li-Dan,Gao, Chao,Liu, Zhi-Hao,Ye, Ting-Hong,Xia, Yong,Xiong, Ying,Song, Xue-Jiao,Lei, Qian,Peng, Cui-Ting,Tang, Hong,Yang, Sheng-Yong,Wei, Yu-Quan,Yu, Luo-Ting
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p. 2764 - 2778
(2015/04/14)
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- SUBSTITUTED HETEROARYL FUSED DERIVATIVES AS PI3K INHIBITORS
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The present invention provides fused derivatives of Formula (I) that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PBKs including, for example, inflammatory disorders, immune- based disorders, cancer, and other diseases.
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Page/Page column 53
(2011/07/07)
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- Modulators of S1P and Methods of Making And Using
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The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.
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Page/Page column 45
(2010/10/19)
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- DNA binding ligands targeting drug-resistant bacteria: Structure, activity, and pharmacology
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We describe the lead optimization and structure-activity relationship of DNA minor-groove binding ligands, a novel class of antibacterial molecules. These compounds have been shown to target A/T-rich sites within the bacterial genome and, as a result, inhibit DNA replication and RNA transcription. The optimization was focused on N-terminal aromatic heterocycles and C-terminal amines and resulted in compounds with improved in vivo tolerability and excellent in vitro antibacterial potency (MIC ≥ 0.031 μg/mL) against a broad range of Gram-positive pathogens, including drug-resistant strains such as methicillin-resistant Stapylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and vancomycin-resistant Enterococcus faecalis (VRE). In a first proof-of-concept study, a selected compound (35) showed in vivo efficacy in a mouse peritonitis model against methicillin-sensitive S. aureus infection with an ED50 value of 30 mg/kg.
- Kaizerman, Jacob A.,Gross, Matthew I.,Ge, Yigong,White, Sarah,Hu, Wenhao,Duan, Jian-Xin,Baird, Eldon E.,Johnson, Kirk W.,Tanaka, Richard D.,Moser, Heinz E.,Bürli, Roland W.
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p. 3914 - 3929
(2007/10/03)
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