Herein we report a direct and efficient method for the synthesis of four new carboxylate-isostere analogs of daptomycin. The side chain carboxylic acid moieties of the aspartic acids (Asp-3, Asp-7 and Asp-9) and β-methyl glutamic acid (MeGlu-12) were all converted into the corresponding carboxylate isosteres using direct synthetic procedures. The present study also describes an esterification p...

To evaluate the impact of chalcogen atom type, we performed a comparative study antioxidant capacity and antiproliferative activity focused library three pyridine-based hydrazonyl-1,3-selenazoles their sulfur isosteres in five assays six human solid tumor cell lines, respectively. In-silico calculations were further used to check pharmacokinetic profiles investigated compounds such as drug-like...

We demonstrated previously that the aqueous root extract of Cryptolepis sanguinolenta (cryptolepis), with cryptolepine as the major constituent adversely affect reproduction and foetal development in mice. However, very little is known on the effect of prenatal exposure of cryptolepis on the post-natal life of surviving animals. Using murine models, we report here, the effects of prenatal expos...

This communication describes a general synthetic route to bicyclic amino acid-carbohydrate-conjugates, which would be useful as conformationally restricted hydroxyethylamine (HEA) transition-state isosteres. The synthesis was achieved in 12 steps starting from D-glucose. The striking features of this system are the bicyclic rigid core displaying an α-amino acid side chain and hydroxyethylamine ...

New 1-benzhydryl-3-phenylurea derivatives and their 1-benzhydryl-3-phenylthiourea isosteres were synthesized and evaluated for their human CB1 and CB2 cannabinoid receptor affinity. These compounds proved to be selective CB1 cannabinoid receptor ligands, acting as inverse agonists in a [35S]-GTPgammaS assay. The affinity of 3,5,5'-triphenylimidazolidine-2,4-dione and 3,5,5'-triphenyl-2-thioxoim...

Abstract The Stimulator of Interferon Genes (STING) plays an important role in innate immunity by inducing type I interferons response to sensing viral or bacterial cytosolic DNA. Cyclic dinucleotides (CDNs) are known activate STING. Here, we describe the synthesis and biological evaluation two new 3’,3’‐CDN, which internucleotide linkages were replaced, respectively, a 1,2,3‐triazole moiety (a...