1196532-71-4

Upstream product

• 2657-25-2 (E)-1-(4-hydroxyphenyl)-3-phenylprop-2-en-1-one 
• 106-96-7 propargyl bromide 
• 100-52-7 benzaldehyde 
• 85699-00-9 1-[4-(methoxymethoxy)phenyl]-1-ethanone 
• 34264-14-7 4-(2-propynyloxy)acetophenone 
• 99-93-4 4-Hydroxyacetophenone 

Downstream Products

• 1196532-69-0 C₇₇H₆₄N₁₂O₈ 
• 1196532-66-7 C₆₆H₅₇N₉O₆ 

Relevant academic research and scientific papers

Click reaction based synthesis, antimicrobial, and cytotoxic activities of new 1,2,3-triazoles

Three-motif pharmacophoric models 20a-e and 21-25 were prepared in good yields by CuAAC of two azido substrates 2 and 11 with seven terminal acetylenic derivatives including chalcones 17a-e, theophylline 18 and cholesterol 19. The structure of these compounds was elucidated by NMR, MS, IR spectroscopy and micro analyses. This series was screened as antimicrobial and cytotoxic agents in vitro. Most derivatives showed appreciable antibacterial activity, but they displayed weak cytotoxic, and antifungal activities. Notably, conjugate 25 (cream of the crop) was found to be more active than Ampicillin against Escherichia coli and Staphylococcus aureus and showed appreciable antifungal and cytotoxic activities as well.

Polymethine-Based Semiconducting Polymer Dots with Narrow-Band Emission and Absorption/Emission Maxima at NIR-II for Bioimaging

Deep-penetration fluorescence imaging in the second near-infrared (NIR-II) window heralds a new era of clinical surgery, in which high-resolution vascular/lymphatic anatomy and detailed cancerous tissues can be visualized in real time. Described here is a series of polymethine-based semiconducting polymers with intrinsic emission maxima in the NIR-IIa (1300–1400 nm) window and absorption maxima ranging from 1082 to 1290 nm. These polymers were prepared as semiconducting polymer dots (Pdots) in aqueous solutions with fluorescence quantum yields of 0.05–0.18 %, and they demonstrate promising applications in noninvasive through-skull brain imaging in live mice with remarkable spatial resolution as well as signal-to-background contrast. This study offers a platform for future design of NIR-IIa or even NIR-IIb emitting Pdots.

Synthesis, Biological Evaluation and Molecular Modeling Studies of Propargyl-Containing 2,4,6-Trisubstituted Pyrimidine Derivatives as Potential Anti-Parkinson Agents

Monoamine oxidase B (MAO-B) inhibitors are potential drug candidates for the treatment of various neurological disorders including Parkinson's disease. A total of 20 new propargyl-containing 2,4,6-trisubstituted pyrimidine derivatives were synthesized and

A Ratiometric Acoustogenic Probe for in Vivo Imaging of Endogenous Nitric Oxide

Photoacoustic (PA) imaging is an emerging imaging modality that utilizes optical excitation and acoustic detection to enable high resolution at centimeter depths. The development of activatable PA probes can expand the utility of this technology to allow for detection of specific stimuli within live-animal models. Herein, we report the design, development, and evaluation of a series of Acoustogenic Probe(s) for Nitric Oxide (APNO) for the ratiometric, analyte-specific detection of nitric oxide (NO) in vivo. The best probe in the series, APNO-5, rapidly responds to NO to form an N-nitroso product with a concomitant 91 nm hypsochromic shift. This property enables ratiometric PA imaging upon selective irradiation of APNO-5 and the corresponding product, tAPNO-5. Moreover, APNO-5 displays the requisite photophysical characteristics for in vivo PA imaging (e.g., high absorptivity, low quantum yield) as well as high biocompatibility, stability, and selectivity for NO over a variety of biologically relevant analytes. APNO-5 was successfully applied to the detection of endogenous NO in a murine lipopolysaccharide-induced inflammation model. Our studies show a 1.9-fold increase in PA signal at 680 nm and a 1.3-fold ratiometric turn-on relative to a saline control.

Synthesis and bioactivity of new chalcone derivatives as potential tyrosinase activator based on the click chemistry

A new series of (E)-1-(4-((1-benzyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-3-phenylprop-2-en-1-one 1a(4-((1-benzyl-1H-1,2,3-triazol-4-yl) methoxy)phenyl)-1-phenylprop-2-en-1-one 1b-15b were designed, synthesized based on click chemistry, and biologically evaluated for their activity on tyrosinase. The result showed that most of prepared compounds 1a-15a have potent activating effect on tyrosinase, especially for 3a, 8a-10a and 14a-15a. Among them, compounds 10a and 14a demonstrated the best activity with EC50=1.71 and 5.60 μmol·L-1 respectively, even better than the positive control 8-MOP (EC50=14.8 μmol·L-1). Conversely, compounds 3b, 5b-6b, 9b-10b, and 15b induced enzymatic inhibition on tyrosinase.

Design, synthesis and anticancer activity of matrine-1H-1,2,3-triazole-chalcone conjugates

Abstract A series of novel matrine-1H-1,2,3-triazole-chalcone conjugates was synthesized and their anticancer activity against A549, Bel-7402, Hela, and MCF-7 cancer cells was evaluated. Most of the conjugates displayed higher potency than their component

Design, synthesis and biological evaluation of chalconyl blended triazole allied organosilatranes as giardicidal and trichomonacidal agents

A series of chalconyl blended triazole allied silatranes (7a-g/8a-g/9a-g) were synthesized in good yields using a simple, economical and biocompatible synthetic route. The blend of three different pharmacologically active moieties into a single scaffold r

Synthetic investigations and photo-physical properties of 1,2,3-triazole encapped chalconyl substituted organotriethoxysilanes

Organotriethoxysilanes (OTES) play an impressive role in the designing of organic-inorganic hybrid materials. The highly efficient copper catalysed 'Click Silylation' is followed for the functionalization of 3-azidopropyltriethoxysilane (AzPTES) with a se

Synthesis and characterization of some novel dendritic architectures bearing chalcone at the periphery through click approach

Synthesis of 1,2,3-triazole-based dendritic architectures bearing a chalcone unit at the surface group has been achieved through a click reaction by the convergent synthetic strategy, in which tri-and tetra-azide were used as core units. Copyright Taylor