613-94-5Relevant articles and documents
Highly selective colorimetric fluorescent sensor for Pb2+
Goswami, Shyamaprosad,Chakrabarty, Rinku
, p. 3791 - 3795 (2010)
Phenanthroline-based colorimetric sensors 1 and 2 have been designed, synthesized, and compared with phenanthrene-based receptor 3 for sensing of Pb2+ by color change. Receptor 1 imparts color change (from yellow to red) selectively with Pb2+ in acetonitrile/water (9:1) as well as in methanol/water (9:1) when in the presence of other metal ions studied (Li +, Na+, K+, Ca2+, Mg2+, Ba2+, Fe3+, Co2+, Ni2+, Cu 2+, Zn2+, Cd2+, Hg2+, and Mn 2+ as their Perchlorate salts). Receptor 1 also shows fluorescence enhancement upon addition of lead Perchlorate in acetonitrile/water (9:1) solvent possibly due to the chelation enhanced fluorescence (CHEF) effect. However, the binding behavior of 2 with Pb2+ is found to be less effective compared to that of receptor 1.
Synthesis, characterization, thermal degradation and urease inhibitory studies of the new hydrazide based Schiff base ligand 2-(2-hydroxyphenyl)-3-{[(E)-(2-hydroxyphenyl)methylidene]amino}-2,3-dihydroquinazolin-4(1H)-one
Ikram, Muhammad,Rehman, Sadia,Subhan, Fazle,Akhtar, Muhammad Nadeem,Sinnokrot, Mutasem Omar
, p. 308 - 319 (2017)
The novel Schiff base ligand 2-(2-hydroxyphenyl)-3-{[(E)-(2-hydroxyphenyl)methylidene]amino}-2,3-dihydroquinazolin-4(1H)-one (H-HHAQ) derived from 2-aminobenzhydrazide was synthesized and characterized by elemental analyses, ES+-MS, 1/sup
A new strategy for fluorometric detection of ascorbic acid based on hydrolysis and redox reaction
Zhao, Yirong,Li, Yinhui,Wang, Yijun,Zheng, Jing,Yang, Ronghua
, p. 35112 - 35115 (2014)
In this study, a near-infrared, indole-cyanine probe, i.e. Cy5-HD, was designed for the detection of ascorbic acid for the first time. The probe has a hydrazone moiety that can be hydrolyzed by Cu2+ to induce the fluorescence quenching of Cy5-H
Protein-Metal-Ion Interactions Studied by Mass Spectrometry-Based Footprinting with Isotope-Encoded Benzhydrazide
Guo, Chunyang,Cheng, Ming,Gross, Michael L.
, p. 1416 - 1423 (2019)
Metal ions, usually bound by various amino-acid side chains in proteins, play multiple roles in protein folding, conformational change, cellular communication, and catalysis. Ca(II) and Mg(II), abundant among biologically relevant cations, execute their c
Exploration of synthesis, structural aspects, DFT studies and bio-efficacy of some new DHA-benzohydrazide based copper(II) complexes
Richa,Kumar, Sunil,Sindhu, Jayant,Choudhary, Poonam,Jaglan, Sundeep,Zangrando, Ennio,Kumar, Rakesh,Sahoo, Subash C.,Kumar, Vinod,Mehta, Surinder K.,Kataria, Ramesh
, (2021)
A copper (II) complex with ligand obtained by the dehydrative condensation of 3-acetyl-6-methyl-2H-pyran-2,4(3H)?dione (DHA) and benzohydrazide has been synthesized (4). This species was additionally coordinated by various solvent molecules, namely ethano
Carbazole-based semicarbazones and hydrazones as multifunctional anti-Alzheimer agents
Chaudhary, Bharat N.,Gandhi, Bhumi,Kanhed, Ashish M.,Patel, Dushyant V.,Patel, Kirti V.,Patel, Kishan B.,Patel, Nirav R.,Prajapati, Navnit K.,Shah, Bhavik S.,Teli, Divya M.,Yadav, Mange Ram
, (2021/07/14)
With the aim to combat a multi-faceted neurodegenerative Alzheimer’s disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and biometal chelating activity. Among them, (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(pyridin-2-yl)hydrazinecarbothioamide (62) and (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(5-chloropyridin-2-yl)hydrazinecarbothioamide (63) emerged as the premier candidates with good ChE inhibitory activities (IC50 values of 1.37 μM and 1.18 μM for hAChE, IC50 values of 2.69 μM and 3.31 μM for EqBuChE, respectively). All the test compounds displayed excellent antioxidant activity (reduction percentage of DPPH values for compounds (62) and (63) were 85.67% and 84.49%, respectively at 100 μM concentration). Compounds (62) and (63) conferred specific copper ion chelating property in metal chelation study. Molecular docking studies of compounds (62) and (63) indicate strong interactions within the active sites of both the ChE enzymes. Besides that, these compounds also exhibited significant in silico drug-like pharmacokinetic properties. Thus, taken together, they can serve as a starting point in the designing of multifunctional ligands in pursuit of potential anti-AD agents that might further prevent the progression of ADs. Communicated by Ramaswamy H. Sarma.
Design, synthesis and pharmacological evaluation of tricyclic derivatives as selective RXFP4 agonists
Lin, Lin,Lin, Guangyao,Zhou, Qingtong,Bathgate, Ross A.D.,Gong, Grace Qun,Yang, Dehua,Liu, Qing,Wang, Ming-Wei
supporting information, (2021/03/16)
Relaxin family peptide receptors (RXFPs) are the potential therapeutic targets for neurological, cardiovascular, and metabolic indications. Among them, RXFP3 and RXFP4 (formerly known as GPR100 or GPCR142) are homologous class A G protein-coupled receptors with short N-terminal domain. Ligands of RXFP3 or RXFP4 are only limited to endogenous peptides and their analogues, and no natural product or synthetic agonists have been reported to date except for a scaffold of indole-containing derivatives as dual agonists of RXFP3 and RXFP4. In this study, a new scaffold of tricyclic derivatives represented by compound 7a was disclosed as a selective RXFP4 agonist after a high-throughput screening campaign against a diverse library of 52,000 synthetic and natural compounds. Two rounds of structural modification around this scaffold were performed focusing on three parts: 2-chlorophenyl group, 4-hydroxylphenyl group and its skeleton including cyclohexane-1,3-dione and 1,2,4-triazole group. Compound 14b with a new skeleton of 7,9-dihydro-4H-thiopyrano[3,4-d][1,2,4]triazolo[1,5-a]pyrimidin-8(5H)-one was thus obtained. The enantiomers of 7a and 14b were also resolved with their 9-(S)-conformer favoring RXFP4 agonism. Compared with 7a, compound 9-(S)-14b exhibited 2.3-fold higher efficacy and better selectivity for RXFP4 (selective ratio of RXFP4 vs. RXFP3 for 9-(S)-14b and 7a were 26.9 and 13.9, respectively).