Synthesis and characterization of novel 2, 2'-bipyrimidine fluorescent derivative for protein binding

<p>Abstract</p> <p>Background</p> <p>Fluorescent dyes with biocompatible functional group and good fluorescence behavior are used as biosensor for monitoring different biological processes as well as detection of protein assay. All reported fluorophore used as sensors are having high selectivity and sensitivity but till there is more demand to synthesized new fluorophore which have improved fluorescence properties and good biocompatibility.</p> <p>Results</p> <p>Novel 4, 4'-(1, 1'-(5-(2-methoxyphenoxy)-[2, 2'-bipyrimidine]-4, 6-diyl)bis(1<it>H</it>-pyrazol-3, 1-diyl)) dianiline fluorescent dye was synthesized by multistep synthesis from 2-phenylacetonitrile, 2-chloropyrimidine and 2-methoxyphenol. This dye has absorption at 379 nm with intense single emission at 497 nm having fairly good quantum yield (0.375) and Stokes shift. The intermediates and dye were characterized by FT-IR, ¹H NMR, ¹³C NMR and Mass spectral analysis. The pyrazole bipyrimidine based fluorescent dye possessing two amino groups suitable for binding with protein is reported. Its utility as a biocompatible conjugate was explained by conjugation with bovine serum albumin. The method is based on direct fluorescence detection of fluorophore-labelled protein before and after conjugation. Purified fluorescent conjugate was subsequently analyzed by fluorimetry. The analysis showed that the tested conjugation reaction yielded fluorescent conjugates of the dye through carbodiimide chemistry.</p> <p>Conclusion</p> <p>In summery synthesized fluorophore pyrazole-bipyrimidine has very good interaction towards protein bovine serum albumin and it acts as good candidate for protein assay.</p

Synthesis of novel dipodal-benzimidazole, benzoxazole and benzothiazole from cyanuric chloride: Structural, photophysical and antimicrobial studies

AbstractIn the present study, new benzimidazole, benzoxazole and benzothiazole derivatives were prepared and screened for antimicrobial activity. The structure of 4,4′-((6-(4-(diethylamino)phenyl)-1,3,5-triazine-2,4-diyl)bis(oxy))dibenzaldehyde (DIPOD) 5 was established from p-hydroxy benzaldehyde 4 and 4-(4,6-dichloro-1,3,5-triazin-2-yl)-N,N-diethylaniline 3. The reaction of DIPOD 5 with different o-phenylenediamine or o-amino phenol or o-amino thiophenol in ethanol gave benzimidazole, benzoxazole and benzothiazole 7. Novel heterocycles showed excellent broad-spectrum antimicrobial activity against bacterial strain (Escherichia coli, Staphylococcus aureus) and fungal strain (Candida albicans, Aspergillus niger) cultures. Activity data was compared with standard Streptomycin and Fluconazole drug. Photophysical and thermal properties of synthesized compounds were also studied

IBX promoted one-pot condensation of β-naphthol, aldehydes, and 1,3-dicarbonyl compounds

Abstract An efficient and mild protocol has been developed for one-pot condensation of β-naphthol, aldehydes, and 1,3-dicarbolyl compounds in presence of o-iodoxybenzoic acid has been found to be an excellent catalyst for the synthesis of tetrahydrobenzo[a]xanthen-one, 1H-benzo[f]chromen-2-yl)-one via one-pot three-component condensation of β-naphthol, aldehydes, and 1,3-dicarbonyl compounds. Short reaction time, ambient conditions, simple workup, and high yield with selective manner are some of the striking features of the present protocol

Synthesis and characterization of novel 4-(1-(4-(4-(4-aminophenyl)-1H-pyrazol-1-yl)-6-(4-(diethylamino)phenyl)-1,3,5-triazin-2-yl)-1H-pyrazol-4-yl)benzenamine fluorescent dye for protein binding

Novel 4-(1-(4-(4-(4-aminophenyl)-1H-pyrazol-1-yl)-6-(4-(diethylamino)phenyl)-1,3,5-triazin-2-yl)-1H-pyrazol-4-yl)benzenamine fluorescent dye was synthesized by multistep synthesis from cyanuric chloride and phenyl acetonitrile. It has absorption at 360 nm with single emission at 497 nm having fairly good quantum yield (0.379). The intermediates and the dye were characterized by FT-IR, 1H NMR, 13C NMR and Mass spectral analysis. Its utility as biocompatible fluorescent dye was explained by conjugation with bovine serum albumin. The method is based on direct fluorescence detection of fluorophore labelled protein before and after conjugation. Purified fluorescent conjugates were subsequently analyzed by fluorimetry. The analysis showed that the tested conjugation reaction yielded fluorescent conjugates of the dye through carbodiimide chemistry

Synthesis of triazine based dialdehyde Schiff's base – new templates for Molecular Imprinting and study of their structural and photophysical properties

Triazine based dialdehyde (DIPOD) and its Schiff's base derivatives were designed and synthesized from cyanuric chloride as template for Molecular Imprinting. Density functional theory calculation results revealed that the distance between two aldehyde groups is 1.3 nm. Synthesized structurally the rigid template having 1,3,5-triazine as core moiety, has been used as template to introduce two appropriately spaced amino groups for substrate binding on the solid surface of silica. The structures of the synthesized DIPOD and its Schiff's base were characterized by FT-IR, 1H NMR, 13C NMR, and UV–Vis spectral analysis. Thermogravimetric analysis showed that the compound has thermal stabilities above 300 °C

Synthesis and antimicrobial activity of novel 2-substituted benzimidazole, benzoxazole and benzothiazole derivatives

In an endeavor to find a new class of antimicrobial agents, a series of 2-(1H-benzimidazol-2-yl)-5-(diethylamino)phenol, 2-(1,3-benzoxazol-2-yl)-5-(diethylamino)phenol, 2-(1,3-benzothiazol-2-yl)-5-(diethylamino)phenol and their derivatives were synthesized starting from p-N,N-diethyl amino salicylaldehyde with different substituted o-phenylenediamine or o-aminophenol or o-aminothiophenol. The newly synthesized compounds were characterized by FT-IR, 1H NMR and LC–MS analysis. All compounds were evaluated for in vitro antibacterial activities against Escherichia coli and Staphylococcus aureus strains and in vitro antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. The antibacterial activities were expressed as the minimum inhibitory concentration (MIC) in μg/mL

Synthesis, photophysical properties of novel fluorescent metal complexes from 3-(1,3-benzoxazol-2-yl)naphthalen-2-ol, and their antimicrobial activities

A series of novel metal complexes containing metal atoms such as Zn, Co, Cu, Cd, Ni, Mg and Sn have been synthesized from 3-(1,3-benzoxazol-2-yl)naphthalen-2-ol. The synthesized ligand was well characterized by IR, 1H-NMR and mass spectrometry. The electrochemical properties were studied by cyclic voltammetric analysis. The synthesized complexes are fluorescent and absorb in the range of 317 to 323 nm while emit in the range of 371 to 416 nm with good quantum yield. All metal complexes show significant in vitro antibacterial activity against E. coli and S. aureus strains and in vitro antifungal activity against C. albicans and A. niger strains by using serial dilution method. The antibacterial activities were expressed as the minimum inhibitory concentration (MIC) in μg/mL