1160740-50-0

Upstream product

• 50-01-1 guanidine hydrochloride 
• 123-08-0 4-hydroxy-benzaldehyde 
• 105-56-6 ethyl 2-cyanoacetate 
• 593-85-1 diguanidine carbonate 
• 105-34-0 methyl 2-cyanoacetate 

Relevant academic research and scientific papers

A spectral deciphering the perturbation of model transporter protein (HSA) by antibacterial pyrimidine derivative: Pharmacokinetic and biophysical insights

Steady state fluorescence and UV-vis absorption spectroscopic techniques have been exploited to explore the binding interaction of a antibacterial pyrimidine derivative 2-amino-6-hydroxy-4-(4-hydroxyphenyl)-pyrimidine-5- carbonitrile (AHHPPC) with the model transporter protein, human serum albumin (HSA) under the physiological conditions. It exhibits antibacterial activity against Escherichia coli and Staphylococcus aureus. Analysis of fluorescence quenching data of HSA at different temperatures using Stern-Volmer methods revealed the formation of AHHPPC-HSA complex with binding affinities of the order 104 M-1. The binding site number (n ≈ 1) and corresponding thermodynamic parameters (ΔG), (ΔH) and (ΔS) were calculated, indicated that binding reaction was endothermic and the hydrophobic interactions plays a major role in stabilizing the complex. The binding distance (r = 3.13 nm) between donor (HSA) and acceptor (AHHPPC) was obtained according to FRET. Changes in the albumin secondary structure imparted by the compound was confirmed using synchronous fluorescence, electronic absorption, circular dichroism (CD) and three-dimensional (3D) fluorescence spectroscopy. All these experimental results clarified that AHHPPC could bind to HSA and be effectively transported and eliminated in body, which could be a useful guideline for further drug design.

Fullerene-C60/NH2: A recyclable heterogeneous catalyst for the green synthesis of chromene and pyrimidine derivatives and antibacterial evaluation

An effective procedure for the synthesis of amino-functionalized fullerene with diethylenetriamine (C60-NH2) is described. The obtained material was characterized by Fourier-transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, energy dispersive X-ray spectroscopy, elemental analysis, thermogravimetric measurements, and X-ray photoelectron spectroscopy. The catalytic activity of C60-NH2 was studied in multicomponent reactions for the synthesis of chromene and pyrimidine derivatives. The results revealed that C60-NH2 was very effective and the desired chromene and pyrimidine products were isolated in good to excellent yields 78%–97% and 81%–98%, respectively. Moreover, the C60-NH2 catalyst could be recycled and reused for at least eight runs without substantial loss in its activity, which makes our procedure environmentally benign. Antibacterial behavior of some of the synthesized products was studied against Gram-positive and Gram-negative bacteria using disk and well diffusion methods. The chromene 4g showed a good antibacterial activity against both bacterial strains Staphylococcus aureus and Serratia marcescens. A good antibacterial activity was also detected for chromene 4o and pyrimidine 7j against S. aureus. The chromene 4m, 4n and pyrimidine 7i compounds displayed a good activity against Micrococcus luteus as a Gram-positive bacterium.

Amino-functionalized SBA-15 catalyzed one-step synthesis of 2-amino-5-cyano-4-hydroxy-6-aryl pyrimidines

A simple and efficient approach towards one-step synthesis of 2-amino-5-cyano-4-hydroxy-6-aryl pyrimidines has been developed. It is based on three-component condensation of aliphatic, aromatic or heterocyclic aldehydes, ethyl cyanoacetate and guanidinium carbonate in the presence of amino-functionalized SBA-15 catalyst in ethanol. In this chemical process, the tautomeric interconversion of pyrimidine derivatives has been observed. This efficient technique has the advantage to give 2-amino-pyrimidine derivatives using a heterogeneous catalyst in high yields, to be completed in short reaction times and to offer a simple product isolation procedure.

A novel and efficient one-pot synthesis of 2-aminopyrimidinones and their self-assembly

A three-component reaction of benzaldehyde derivatives, methyl cyanoacetate, and guanidinium carbonate affords 2-amino-4-aryl-1,6-dihydro-6- oxopyrimidine-5-carbonitriles and the four-component reaction of benzaldehyde derivatives, methyl cyanoacetate, and guanidinium hydrochloride in the presence of piperidine leads to piperidinium salts of pyrimidinones. X-ray crystallography data confirm self-assembly and H-bonding in these compounds.

A novel and efficient one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines and their anti-bacterial activity

The first simple and efficient approach towards one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines has been developed by three component condensation of aromatic aldehydes, ethyl cyanoacetate and guanidine hydrochloride in alkaline ethanol