Synthesis and evaluation of NS5A inhibitors containing diverse heteroaromatic cores

Imidazoles and Oxazoles from Lapachones and Phenanthrene‐9,10‐dione: A Journey through their Synthesis, Biological Studies, and Optical Applications

“…Imidazoles are present in several natural products, for instance, the hormone histamine (5). [1] Furthermore, some commercial drugs contain an imidazole ring, such as the antifungal miconazole (6), [2] antibiotic metronidazole (7), [3] and the sedative midazolam (8). [4] Ahmat and co-workers have described a series of 2,5disubstituted 1,3,4-oxadiazoles (9) as potent β-glucuronidase inhibitors (Figure 1).…”

“…[7] Some examples of oxazole fused with benzene, producing benzoxazole (4) derivatives, with interesting applicability, are well described in the literature, such as the bis-benzoxazole 12, which exhibits activity against the hepatitis C virus variant genotype 1b. [8] The substitution of benzoxazole by benzimidazole resulted in compounds with activity against both genotype 1b and 1a replicons. Another example of benzoxazole is tafamidis (13), described as a potent transthyretin kinetic stabilizer that inhibits the amyloid cascade (Figure 1).…”

An efficient one-pot conversion of carboxylic acids into benzimidazoles via an HBTU-promoted methodology

“…In recent years, alpha-aminobenzimidazoles (3 and 4) have emerged as potent drug leads for infections, cancer and autoimmune diseases, [15][16][17] as well as metal-binding motifs. 5 Due to the limited synthetic utility of existing methods, we envisioned developing a mild, functional group tolerant method for accessing a diverse class of benzimidazole synthons (Scheme 2).…”

“…5 Due to the limited synthetic utility of existing methods, we envisioned developing a mild, functional group tolerant method for accessing a diverse class of benzimidazole synthons ( Scheme 2 ). Such a methodology would greatly benefit our research group and others who are interested in developing benzimidazole-containing peptides as drug leads, 16 and chiral benzimidazoles as ligands. The reported study explores a simple, yet reliable approach to access a structurally diverse library of benzimidazoles that includes amino acid derived alpha-aminobenzimidazoles, alkyl benzimidazoles and indole benzimidazoles.…”

Bio-Analytical Method Development and Validation for Simultaneous Determination of Ledipasvir and Sofosbuvir Drugs in Human Plasma by Rp-HPLC Method

“…It acts against HCV and is categorized as a direct-acting antiviral agent (DAA). It is an inhibitor of the Hepatitis C Virus (HCV) NS5A protein which is required for viral RNA replication and assembly of HCV virions [9]. Sofosbuvir, IUPAC name is Isopropyl-…”