New therapeutic leads are in global demand against multiple drug-resistant , as presently there is no drug of choice left to treat this pathogen. In the present work, we have designed, synthesized, and in vitro validated dimedone-coupled 2,3-dihydrofuran (DDHF)-based inhibitor scaffolds against Staphylococcal thioredoxin reductase (SaTR), a pivotal drug target enzyme of Gram-positive pathogens. Accordingly, a green multicomponent method that is both efficient and one pot has been optimized to synthesize DDHF derivatives.
View Article and Find Full Text PDFIntroduction: Tooth discoloration is a common issue for oral health practitioners. Whitening treatments remove surface and deep stains using either chemicals or over-the-counter products. Due to harmful chemical effects, organic whitening products are increasingly preferred.
View Article and Find Full Text PDFWe show that the non-canonical nucleobase 2,6-diaminopurine (D) spontaneously base pairs with uracil (U) in water and the solid state without the need to be attached to the ribose-phosphate backbone. Depending on the reaction conditions, D and U assemble in thermodynamically stable hydrated and anhydrated D-U base-paired cocrystals. Under UV irradiation, an aqueous solution of D-U base-pair undergoes photochemical degradation, while a pure aqueous solution of U does not.
View Article and Find Full Text PDFLewis-acid cascade reactions promoted by BF·OEt are reported for the synthesis of highly substituted pyrrolo[1,2-]indoles and congeners of benzofuro[2,3-]indoles. These reactions are highly regio- and diastereoselective towards generating up to five contiguous stereogenic centers, including two vicinal quaternary centers. Furthermore, an established cascade approach and the mechanism proposed herein are well supported by quantum chemistry calculations.
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