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  • Open access
  • 168 Reads
Ultrasound-Assisted Facile Synthesis and Anticancer Evaluation of Novel N-(2-substituted phenyl-4-oxathiazolidine-3-carbonothioyl) benzamide

The work reports synthesis of ten novel derivatives of N-(2-substituted phenyl)- 4-oxothiazolidine-3-carbonothioyl benzamide derivatives 6(a-j) were synthesized by cyclization of key compounds N-(benzylidenecarbamothioyl)-benzamide using thioglycolic acid in solvent DMF and catalyst anhydrous ZnCl2 using ultra-sonicator as an eco-friendly synthetic route. The nitrogen and sulphur containing heterocycle such as thiazolidinone has attracted continuing interest because of its varied biological activities. With the coupling of benzamide the anticancer activity of thiazolidinone derivatives is enhanced. Out of the 10 derivatives, 6a and 6c were found to have potential activity against MCF7 cell line whereas 6d and 6h exhibited potential activity against both the cell lines MCF7 and HeLa cell line. As the synthesized derivatives showed good anticancer activity this moiety can be further studied and modified to help in development of anticancer drug. The structures of the synthesized compounds were confirmed by spectral characterization such as IR, 1H NMR, 13CNMR and Mass spectral studies.

  • Open access
  • 141 Reads
A One-pot process for the synthesis of Alkyne-3-tretrazolyl-tetrazolo [1,5-a] quinolines.

An efficient synthesis of alkyne-3-tetrazolyl-Tetrazolo[1,5-a] quinolone via a one-pot process: I-MCR Ugi-azide /SNAr/ ring-chain azido tautomerization under ecofriendly conditions. We report the one-pot synthesis of tris-heterocycles containing the tetrazolo[1,5-a]quinoline bound with 1,5-disubstituted-tetrazole (1,5-DS-T). The synthesis of this compounds can be of high interest for synthetic and medicinal chemistry because all the heterocycles are considered privilegied scaffolds and could lead to the discovery of novel bioactive molecules.

  • Open access
  • 74 Reads
Ultra sound assisted green one pot synthesis of bound type bis-heterocyclic furan-2-yl imidazo [1,2-a] pyridines via GBBR

A series of six new 3-imidazo[1,2-a] pyridine furan bound type tris-heterocycles were synthesized by Ultrasound Irradiation (USI) assisted Groebke-Blackburn-Bienaymé reaction (GBBR), by employing ammonium chloride (10 mol%) as a catalyst in excellent yields (80-93%) under green conditions. This efficient and mild protocol has silent features such as green inexpensive and easily available catalyst and solvent at room temperature.

  • Open access
  • 16 Reads
Alginate-Coated MIL-100-Fe as an Appropriate Drug Delivery System

Metal-organic frameworks (MOFs) are a class of crystalline porous materials which contain metal ions and organic linkers in their structure. These materials are known as molecular cages which can trap a various range of molecules and whereby are highly functional in different fields of chemistry.

In this work, we exerted coated-nanoporous MIL-100-Fe MOF as a drug delivery system (DDS) to encapsulation and release of a model pharmaceutical agent. The MOF has been prepared using solvothermal technique and then coated with Sodium Alginate as a green biodegradable polymer. Herein Metformin is utilized as a model drug to be trapped inside the MOF pores within an aqueous solution in the presence of the MOF nanoparticles. Metformin is an oral antihyperglycemic agent which is used for the treatment of type II diabetes. The successful synthesis of the framework is proved by several techniques including IR, PXRD, and TGA. In vitro studies showed that this framework is a promising DDS for the targeting and controlling release of drug molecules especially the oral one.

By this technique, unwanted effects of the immature release of the loaded drug will be reduced and the drug cargo will be released in a controlled way either which it resulted in the increase of drug bioavailability.

  • Open access
  • 71 Reads
Structural study of three 1,2,4-triazole derivatives prepared by oxidative cyclization of thiosemicarbazides

In the present research, 5,5-dimethyl-4-phenyl-4,5-dihydro-3H-1,2,4-triazole-3-thione was prepared by condensation from N-phenylhydrazinecarbothioamide, while 4-phenyl-5-(pyrazin-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione and 2-((5-(pyridin-2-yl)-4H-1,2,4-triazol-3-yl)thio)acetic acid have been prepared by oxidative cyclization from 2-(amino(pyrazin-2-yl)methylene)-N-phenylhydrazine-1-carbothioamide and 2-(amino(pyridin-2-yl)methylene)hydrazine-1-carbothioamide, respectively. The three compounds have been well characterized and their molecular structures studied by single-crystal X-ray diffraction. The supramolecular assembly of each crystal is also analyzed and discussed.

  • Open access
  • 120 Reads
Effects of three ionic liquids on microbial activity of an organic soil. Microcalorimetric study.

Ionic liquids are considered as a potential green replacement for traditional volatile organic solvents, but their impact on the environment is not studied enough. Despite the increasing number of papers reporting studies trying to determine the toxic effects of different ILs, the knowledge of their toxicity is still an open question.

The effect of different amounts (from 0% to 100%) of three ionic liquids, two based imidazolium, dimethylimidazolium dimethylphosphate ([MMIM][DMP] and 1-butyl-3-methylimidazolium tetrafluoroborate ([BMIM][BF4]), and choline dihydrogen phosphate ([Chol][DHP]) on the microbial activity of an organic soil was determined in this work. For this propose, an isothermal microcalorimeter, TAM III of TA Instruments was used. This apparatus allows estimating the variation of the metabolic activity trough the variation of the heat released after the addition of the ILs to the soil.

The results showed that the most toxic IL is [BMIM][BF4] which presented a large stress effect and subsequent death on soil microorganisms for the highest concentration of the IL. On the contrary, [Chol][DHP] showed stimulation of the microbial activity for all the concentrations.

  • Open access
  • 103 Reads
Hydrothermal Synthesis of a new Cd-MOF

Metal-organic frameworks (MOFs) are porous crystalline materials of one-, two-, or three-dimensional networks constructed from metal ions/clusters and multidentate organic linkers via coordination bonding [1]. Exceptionally high porosity, crystallinity, compositional and structural variability, large surface area and acceptable thermal and mechanical stability of metal-organic frameworks (MOFs) make them ideal materials to satisfy the needs of various applications such as gas and vapour sorption, chemical separation, catalysis, magnetism, luminescence, drug storage and delivery [1,2].

There are many systematic and facile synthetic routes such as hydro/solvothermal technique, microwave, electrochemical and mechanochemical, etc. Hydrothermal method is used more than any other way due to its high speed [3].

For synthesis of [Cd(BDC)0.5(PCA)], three constituents i.e. Cd(NO3)2·4H2O, pyridine-4-carboxylic acid (PCA), and benzene-1,4-dicarboxylic acid (BDC) in DMF−EtOH were reacted by solvothermal technique under autogenous pressure.

The MOF characterized by Fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy. Due to the high intensity of the peaks and a peak that appears in 2Ɵ below 10, we concluded a high porosity of the obtained MOF. The Fourier transform infrared spectroscopy (FT-IR) spectra of MOF are presented. The characteristic C=O vibrations at 1650 cm1 indicate the existence of carboxylate in PCA and BDC.

  • Open access
  • 65 Reads
Pyrrolidinodiones in Enol-Ugi, Enol-Passerini and anomalous enol-Passerini condensations

In continuation with our recent research in the development of novel multicomponent reactions with isocyanides, we have used for the first time enols as the acid components in Ugi and Passerini-type reactions. Thus, electron-poor pyrrolidinodiones react with aldehydes, amines and isocyanides to give the enaminic four-component adducts. Conversely, in the absence of the amine component, careful control of the reaction conditions allows the involvement of one or two molecules of isocyanide to afford selectively, either Passerini-type or pseudo-enol-Ugi-type products. These unprecedented condensations of isocyanides, enols and 4-substituted pyrrolidine-2,3-diones constitute an excellent strategy for the preparation of new biologically relevant pyrrolidinones having peptidic or pseudo-peptidic groups on carbon 3.

  • Open access
  • 96 Reads
Design and Synthesis of Novel chalcone-phenylpyranone derivatives as Estrogen Receptor Modulators

Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor (ER). SERMs are used for treatment and reduction of risk of breast cancer. Herewith we had designed, synthesized and evaluated chalcone-phenylpyran-2-one derivatives bearing N,N-dimethyl ethalamine side chain for their anti-breast cancer activity using MCF-7 and Zr-75-1 cell lines in-vitro. The pharmacological data indicated that most of tested compounds showed moderate to significant cytotoxicity and high selectivity toward estrogen receptor. The SAR analyses indicated that compounds 5f with 2,6 dichloro substitution was more effective. Docking study was performed to predict binding orientation towards the estrogen receptor-α.

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