Mebastin (mebhydrolin) / Incepta Pharma - LARVOL DELTA

Photo-driven bifunctional iron-catalyzed one-pot assembling of indoles from arylamines and alkanes/carboxylic acids. (PubMed, Nat Commun) - "The protocol demonstrates broad substrate scope (152 examples), excellent functional group tolerance, and high yields (up to 95%), facilitating the direct construction of diverse indole scaffolds without pre-functionalization. Notably, the methodology can be successfully applied to the concise and scale-up total synthesis of several pharmacologically relevant indole derivatives, including Iprindole, Mebhydrolin, Melatonin, and A-FABP inhibitor, underscoring its practicality and potential for industrial application in pharmaceutical manufacturing."

Journal • FABP4

Pd/NBE-Catalyzed One-Pot Modular Synthesis of Tetrahydro-γ-carbolines. (PubMed, J Org Chem) - "Here, using commercially available NBE derivatives (NBEs), we report an efficient protocol for the one-pot modular synthesis of 4-substituted tetrahydro-γ-carbolines via Catellani/aza-Michael addition cascade from easily available 3-iodo-1-tosyl-1H-indole, aziridines and olefins. This approach exhibits a wide substrate scope, good yields, scalability, and potential extension toward the synthesis of Mebhydroline analogues."

Journal

Repurposing of the antihistamine mebhydrolin napadisylate for treatment of Zika virus infection. (PubMed, Bioorg Chem) - "Our data together suggest that MHL suppresses ZIKV infection through the inhibition of ZIKV NS5 RdRp activity. This study highlights that MHL might be a promising clinical anti-ZIKV therapeutic."

Journal • CNS Disorders • Infectious Disease

Antiallergic drug Mebhydrolin ameliorates glucose homeostasis in type 2 diabetic mice by functioning as a selective FXR antagonist. (PubMed, Metabolism) - "Our work has revealed a novel mode for the regulation of FXR against glucose metabolism in T2DM mice and highlighted the potential of Mebhydrolin in the treatment of T2DM."

Journal • Preclinical • Diabetes • Dyslipidemia • Metabolic Disorders • Type 2 Diabetes Mellitus • FOXO1 • GSK3B