10.1016/j.tetasy.2008.01.031
The research focuses on the chemoenzymatic preparation of enantiopure LL-benzofuranyl- and LL-benzo[b]thiophenyl alanines, which are important components in biological and pharmaceutical products. The study combines lipase-mediated dynamic kinetic resolution (DKR) with chemical and enzymatic hydrolytic steps to synthesize the enantiopure amino acids. The experiments involve the use of various commercially available starting materials, such as benzofuran, benzo[b]thiophene, and 1-(2-hydroxyphenyl)ethanone, which are transformed through a series of chemical reactions, including formylation, chloromethylation, and cyclisation, to produce the desired aldehydes and subsequently the racemic amino acids and their derivatives. The enzymatic DKR is then carried out using Novozyme 435 in different alcohols and solvents to achieve high enantioselectivity. The stereoselectivity and conditions of DKR are investigated, and the enantiomeric excess (ee) is determined using HPLC analyses with chiral columns. The research also includes the use of Acylase I for the kinetic resolution of racemic 2-acetamido-3-(heteroaryl)propanoic acids, leading to the final enantiopure products. The analyses used in this study include NMR spectroscopy, mass spectrometry, HPLC, and specific rotation measurements to confirm the configuration and purity of the synthesized amino acids.
10.1080/07391102.2020.1805364
The study focuses on the synthesis and evaluation of 3-hydroxyflavone derivatives as inhibitors of mushroom tyrosinase, an enzyme involved in melanin production. A series of 3-hydroxyflavone scaffolds were synthesized using the Algar-Flynn-Oyamada reaction, and these compounds were screened for their in vitro inhibitory activity against tyrosinase. The chemicals used in the study included o-hydroxyacetophenone, various substituted benzaldehydes, sodium hydroxide, methanol, and hydrogen peroxide. These chemicals served the purpose of reacting together to form the desired 3-hydroxyflavone derivatives, which were then tested for their antimicrobial potential and their ability to inhibit tyrosinase, providing insights into their potential use as therapeutic agents for pigmentation-related disorders and as antimicrobial agents. The study also involved the use of spectroscopic techniques and mass spectrometry for compound characterization, as well as molecular modeling to explore binding interactions with the tyrosinase enzyme.
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