- Triazole-naphthalene based fluorescent chemosensor for highly selective naked eye detection of carbonate ion and real sample analyses
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Herein, the design and synthesis of triazole-naphthalene hybrid for selective colorimetric and fluorometric sensing of carbonate ion has been reported. The probe has been thoroughly characterized by 1H and 13C NMR and HRMS spectroscopy. CK exhibits an excellent selectivity and sensitivity towards carbonate ions over other anions by changes in both UV–Vis absorption spectra and emission spectra. The limit of detection of carbonate ion in absorbance and emission spectra has 7.2 nM and 1.8 μM respectively. The plausible sensing was confirmed with the help of the Job's plot, FTIR, NMR titration and theoretical studies. Also, naked eye detection method of carbonate from colorless to yellow color is the most conspicuous application of probe CK. The receptor CK providing valuable practical sensor for environmental analyses of carbonate ion. Further, we mimic new logic gate circuit by using the sensing performance of carbonate ion with probe.
- Ayyanar, Siva,Chinnadurai, Chithiraikumar,Chinnamadhaiyan, Muniyappan,Muniyasamy, Harikrishnan,Nelson, Malini
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- Novel Human Urate Transporter 1 Inhibitors as Hypouricemic Drug Candidates with Favorable Druggability
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Lesinurad, a human urate transporter 1 (URAT1) inhibitor approved as a medication for the treatment of hyperuricemia associated with gout in 2015, can cause liver and renal toxicity. Here, we modified all three structural components of lesinurad by applying scaffold hopping, bioisosterism, and substituent-decorating strategies. In a mouse model of acute hyperuricemia, 21 of the synthesized compounds showed increased serum uric acid (SUA)-reducing activity; SUA was about 4-fold lower in animals treated with 44, 54, and 83 compared with lesinurad or benzbromarone. In the URAT1 inhibition assay, 44 was over 8-fold more potent than lesinurad (IC50: 1.57 μM vs 13.21 μM). Notably, 83 also displayed potent inhibitory activity (IC50 = 31.73 μM) against GLUT9. Furthermore, we also preliminarily explored the effect of chirality on the potency of the promising derivatives 44 and 54. Compounds 44, 54, and 83 showed favorable drug-like pharmacokinetics and appear to be promising candidates for the treatment of hyperuricemia and gout.
- Zhao, Tong,Meng, Qing,Sun, Zhuosen,Chen, Yanyu,Ai, Wei,Zhao, Zean,Kang, Dongwei,Dong, Yue,Liang, Ruipeng,Wu, Ting,Pang, Jianxin,Liu, Xinyong,Zhan, Peng
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p. 10829 - 10854
(2020/11/09)
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- Preparing method of triazole thioglycolic acid compound for curing metabolic arthritis
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The invention discloses a preparing method of a triazole thioglycolic acid compound for curing metabolic arthritis. According to the method, compound II and compound III are utilized as initial materials and are generated into intermediate compound IV through Suzuki reaction; then nucleophilic substitution happens between the intermediate compound IV and 1,1minute-thiocarbonyl polypyridobisinudazole to generate intermediate compound V; the compound V generates intermediate compound VI through cyclization reaction, and then nucleophilic substitution happens between the compound VI and methyl chloroacetate to generate intermediate compound VII; the intermediate compound VII generates intermediate compound VIII through bromination reaction; and a target product 2-((5-bromine-4-(4-cyclopropyl naphthalene-1-yl)-4H-1,2,4-triazole-3-yl)sulfenyl) acetic acid (I) is generated through hydrolysis reaction. The preparing method is high in selectivity and simple to operate and avoids poisonous reagents and rigorous reacting conditions. Compared with an original synthetic method, the reacting time of the preparing method is shortened, the energy consumption is reduced, and the reaction yield is improved.
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Paragraph 0069; 0070; 0071
(2016/10/09)
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- MANUFACTURE OF 2- (5- BROMO-4 (-CYCLOPROPYLNAPHTHALEN-1-YL) -4H-1,2,4-TRIAZOL-3-YLTHIO) ACETIC ACID
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Described herein are certain processes for the synthesis of compounds of Formula (I):
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- POLYMORPHIC, CRYSTALLINE AND MESOPHASE FORMS OF SODIUM 2-(5-BROMO-4-(4-CYCLOPROPYLNAPHTHALEN-1-YL)-4H-1,2,4-TRIAZOL-3-YLTHIO)ACETATE, AND USES THEREOF
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Crystalline polymorphs and solid mesophase forms of sodium 2-(5-bromo-4- (4-cyclopropylnaphthalen-l-yl)-4H-l,2,4-triazol-3-ylthio)acetate are described. In addition, pharmaceutical compositions and uses of such compositions for the treatment of a variety of diseases and conditions are provided.
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Page/Page column 38
(2011/08/03)
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- NOVEL COMPOUNDS AND COMPOSITIONS AND METHODS OF USE
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Described herein are compounds useful in the modulation of blood uric, acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders relafed to aberrant levels of uric acid
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Page/Page column 89-91
(2009/07/03)
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- S-TRIAZOLYL α-MERCAPTOACETANILDES AS INHIBITORS OF HIV REVERSE TRANSCRIPTASE
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A series of S-triazolyl α-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
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Page/Page column 23
(2010/10/20)
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