Design, synthesis and in silico molecular docking evaluation of novel 1,2,3-triazole derivatives as potent antimicrobial agents.

Chalcone and triazole scaffolds have demonstrated a crucial role in the advancement of science and technology. Due to their significance, research has proceeded on the design and development of novel benzooxepine connected to 1,2,3-triazolyl chalcone structures. The new chalcone derivatives produced by benzooxepine triazole methyl ketone and different aromatic carbonyl compounds are discussed in this paper.

Development and validation of a novel stability-indicating reverse phase HPLC method for the determination of sacubitril-valsartan premix stereoisomers: Cellulose tris(4-methyl benzoate) stationary phase.

A new stability indicating reverse phase HPLC method has been developed and validated as per International Conference on Harmonization guidelines for the determination of sacubitril-valsartan premix stereoisomers, namely, (2R)-valsartan, (2S,4S)-sacubitril, (2R,4S)-sacubitril, and (2R,4R)-sacubitril. Primarily, stability indicating separation study was done on reverse phase LC conditions; it was described by peak homogeneity of sacubitril-valsartan and its stereoisomers. Cellulose tris(4-methylbenzoate) packing column Chiralcel OJ-RH(150 mm × 4.

Synthesis of Isomeric and Potent Impurities of the Triazole-Based Antifungal Drug Voriconazole.

We describe the synthesis of two positional isomers and a desfluoro impurity of Voriconazole starting with Friedel-Crafts acylation of mono- and difluorobenzene. These isomers are the crucial components in determining the quality of Voriconazole during its manufacturing from the key raw material, 1-(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethan-1-one. All the prepared impurities were characterized by IR, (1)H-NMR, (13)C-NMR, and mass spectral data.

An Alternative Approach to Isoganciclovir: A Prominent Impurity in the Antiviral Drug Ganciclovir.

A simple and efficient process for the preparation of (±)-9-[(2,3-dihydroxypropoxy)methyl]guanine (isoganciclovir) is described. The synthesis features the preparation of a kinetically and thermodynamically controlled acyclic side chain using masked glycerol and methoxymethyl acetate. The unwanted regioisomers were separated through selective crystallization, which upon deprotection yielded isoganciclovir in good yield.