Enzymatic Synthesis of a Diastereomer of Neoabyssomicin Derivative Using the Diels-Alderase AbyU

Main observation and conclusion The enzyme AbyU catalyses a Diels-Alder (DA) reaction during abyssomicin C biosynthesis.In this study,AbyU is shown to convert t...     

Fabrication of Gene Carrier via Self-assembly of Poly[(dimethylamino)ethyl Methacrylate] and Poly(aspartic acid)-grafted-Poly(ethylene glycol)

A biocompatible complex has been prepared as gene carrier via electrostatic interaction, which is composed of a polycation, that is, poly[(dimethylamino)ethyl methacrylate] end-capped with cholesterol moiety (Chol-PDMAEMA₃₀), along with a polyanion named poly(aspartic acid)-grafted-poly(ethylene glycol) (PASP-g-PEG). The complexes have less cytotoxicity compared to the case of alone Chol-PDMAEMA₃₀ or branched polyethylenimine (PEI) system.

In the present study, biocompatible complexes have been prepared as gene carrier via electrostatic interaction, which is composed of a polycation, that is, poly[(dimethylamino)ethyl methacrylate] end-capped with cholesterol moiety (Chol-PDMAEMA₃₀), along with a polyanion named poly(aspartic acid)-grafted-poly(ethylene glycol) (PASP-g-PEG). We first synthesized polysuccinimide (PSI) via condensation polymerization of aspartic acid, and then used PEG-NH₂ to react with the partial pentacyclic rings of PSI to yield a kind of graft copolymer polysuccinimide-grafted-poly(ethylene glycol) (PSI-g-PEG). After hydrolysis of the residual succinimide units, a new biodegradable and biocompatible graft copolymer PASP-g-PEG was prepared successfully. Chol-PDMAEMA₃₀ was synthesized via oxyanion-initiated polymerization, as reported in our previous literature. We investigated the interactions between every pair among calf thymus DNA, Chol-PDMAEMA₃₀, and PASP-g-PEG by agarose gel retardation assay. The results indicate that the prepared complexes could completely bind DNA and may become more stable during systemic circulation. The complexes have less cytotoxicity compared to the case of alone Chol-PDMAEMA₃₀ or branched polyethylenimine (PEI) system. Furthermore, the physicochemical properties of the complexes were also investigated by zeta potential, transmission electron microscopy (TEM) and dynamic light scattering (DLS) measurements. These biodegradable and biocompatible polymeric carriers have potential applications in gene delivery.     

Multicomponent Domino [4+1+1] Carbocyclization Providing an Efficient and Regioselective Strategy to Fluoren-9-ones

Concise and efficient three‐component domino [4+1+1] carbocyclization to highly substituted fluoren‐9‐one derivatives promoted by K₂CO₃ has been developed under microwave irradiation conditions. The direct bis‐cyanation and aryl amination residing in fluoren‐9‐one framework were achieved in a one‐pot operation. The reaction proceeds at fast rates and can be finished within 30 min, which makes workup convenient to give good to excellent chemical yields.     

Microwave‐assisted Aqueous Multicomponent Reaction: Facile Synthesis of Polyfunctionalized Indoline‐spiro Fused Pyran Derivatives

A green and highly efficient method for the synthesis of polyfunctionalized indoline‐spiro fused pyran derivatives has been established. This reaction was conducted by reacting readily available and inexpensive starting materials, such as isatins, cyclic‐1,3‐dicarbonyl compounds, and malononitrile in aqueous media without any catalysts under microwave irradiation. The present green synthesis shows fascinating properties such as the use of water as the reaction solution, concise one‐pot conditions, short reaction periods (8–14 min), and easy purifications. The synthesis could also set a good example to GAP (Group‐Assistant‐Purification) chemistry in which purification via chromatography can be avoided and the pure products can be easily acquired only by washing the crude products with 95% EtOH.     

Highly Efficient Synthesis of Tricyclic Perimidines under Microwave Heating

A new and efficient access to (Z)‐N‐(2‐argio‐1‐(1H‐perimidin‐2‐yl)vinyl)benzamide derivatives from readily available substrates in HOAc is described with aid of microwave irradiation. The results of our study provide a simple, straightforward synthetic route to these interesting classes of 2‐substituted perimidines analogs in excellent yields.     

Efficient Green Procedure for the Synthesis of Coumarin Derivatives by a One‐Pot,Three‐Component Reaction under Solvent‐Free Conditions

A simple, efficient, and general method has been developed for the synthesis of coumarin derivatives through a one‐pot reaction of aromatic aldehydes, 2,2‐dimethyl‐1,3‐dioxane‐4,6‐dione and 5,5‐dimethyl‐1,3‐cyclohexanedione, in the presence of TEBA under solvent‐free conditions using grinding methods. The mild reaction conditions, simple protocol, high yields, and cleaner reaction make this protocol practical and economically attractive.     

Analytical application of the poly(1H-1,2,4-triazole-3-thiol) modified gold electrode for high-sensitive voltammetric determination of catechol in tap and lake water samples

ABSTRACT

In this work, a simple, sensitive and rapid method for the determination of trace amounts of catechol (CT) in aqueous media has been suggested. For this purpose, poly(1H-1,2,4-triazole-3-thiol) film was electrochemically deposited successfully at the gold electrode (Au/T3T). The electrochemical behaviour of CT was studied on the Au/T3T electrode by the cyclic voltammetry and differential pulse voltammetry techniques. The anodic peak current value and the concentration of CT showed a good linear relationship in the range of 0.015–2.8 µM. The limit of detection was found as 1.88 nM (S/N = 3). Besides, the reproducibility, repeatability, stability and interference measurements were also assayed. This sensor was applied successfully for the detection of CT in synthetic and real samples.     

New formal (3+3) cycloaddition of enaminones for forming tetracyclic indolo[2,3-b]quinolines under microwave irradiation

Concise and efficient base-promoted domino formal (3+3) cycloaddition has been established for the formation of tetracyclic indolo[2,3-b]quinoline derivatives under microwave heating. The present methodology shows attractive properties, such as the maximum efficiency of a process, short reaction periods, and operational simplicity, and it can avoid time-consuming and costly syntheses, tedious work-up and isolation of intermediate. This chemistry provides a facile and promising synthetic strategy to construction of tetracyclic indolo[2,3-b]quinoline skeleton.     

Dopamine derivatives from the insect Polyrhachis dives as inhibitors of ROCK1/2 and stimulators of neural stem cell proliferation

Polyrhachis dives is consumed as an insect food in some regions of China. In this study, new dopamine derivatives, (+)-polyrhadopamine A (1a) and (−)-polyrhadopamine A (1b), (+)-polyrhadopamine B (2a) and (−)-polyrhadopamine B (2b), and polyrhadopamines C–E (3–5), were isolated from this species. The structures and stereochemistry of these substances were assigned by using spectroscopic and computational methods. Compounds 1a, 1b, 2a, and 2b are dimeric N-acetyldopamine derivatives, 3 is a dopamine analog containing an unusual sulfone group, and 4 and 5 possess a rare benzo[d]thiazole moiety. The functions of these substances as ROCK1/2 inhibitors, neural stem cell (NSCs) proliferation stimulators, immunosuppressive, and anti-inflammatory agents were determined.