Volume 1 | Issue 1 | 1 of 6 Chem Pharm Res, 2018 Synthesis, α-Glucosidase Enzymatic Inhibition and Docking Studies of some Fused Heterocycles 1 Departamento de Ciencias Básicas, Unidad Profesional Interdisciplinaria de Biotecnología del Instituto Politécnico Nacional (UPIBI-IPN) Avenida Acueducto s/n La Laguna Ticomán Ciudad de México, México. 2 Departamento de Química Centro de Investigación y Estudios Avanzados (Cinvestav-IPN) Avenida Instituto Politécnico Nacional 2508 San Pedro Zacatenco Ciudad de México México. * Correspondence: Marco Brito-Arias, Departamento de Ciencias Básicas, Unidad Profesional Interdisciplinaria de Biotecnología del Instituto Politécnico Nacional (UPIBI-IPN), México, E-mail: mbrito@ ipn.mx. Received: 27 December 2018; Accepted: 02 February 2019 Marco Brito-Arias 1* , Paola L. Ramírez-Hernández 1 , Esmeralda C. García-Barrera 1 , Mario Perez- Venegas 2 , Christian Montiel-Valenciana 1 and Leonor P. Rodríguez-Pascual 1 Chemical & Pharmaceutical Research Research Article Citation: Marco Brito-Arias, Paola L. Ramírez-Hernández, Esmeralda C. García-Barrera, et al. Synthesis, α-Glucosidase Enzymatic Inhibition and Docking Studies of some Fused Heterocycles. Chem Pharm Res. 2019; 1(1): 1-6. ABSTRACT In the search of heterocyclic ring systems potentially useful as α-glucosidase inhibitors we have synthesized a set of heterocycles bearing hydroacridone 4-5, hydroxanthone 6, quinazolone 8, benzoyl phtalimide 9 and isoquinolone 10-11. These compounds under study were subjected to enzyme inhibition and compared against reference inhibitor acarbose observing potent inhibition for benzoyl phtalimide 9, and isoquinolone dione 11. Based on their inhibition activity, both candidates were selected for docking analysis to determine their best posing, and the interactions involved between the ligand and the residues. A comparative analysis was established to determine the potential correlation between the interactions found, the inhibition observed for the candidates and the interactions observed for the reference inhibitor acarbose. Keywords Fused heterocycles, α-Glucosidase, Enzymatic inhibition, Molecular docking. Introduction The glycaemic control is considered a crucial step in the prevention and management of diabetes mellitus, and the search of inhibitors targeting the enzymes α-amylase and α-glucosidase responsible for the hydrolysis of starch and oligosaccharides present in the diet an important strategy in the modulation of the glycaemic profle. It is well known that α-glucosidase inhibitors slow down the process of digestion and absorption of carbohydrates by competitively blocking its activity, leading to the reduction of the glucose concentrations in blood [1]. In the search of active compounds useful as α-glucosidase inhibitors an intensive screening has been undertaken particularly from natural resources including microorganisms and medicinal plants. For instance a recent review reported the evaluation of 61 terpenes, 37 alkaloids, 49 quinones, 7 xanthones, 103 favonoids and 37 phenols either with or without glycosidic moieties, providing important information about structural diversity which can be applied in drug discovery and lead modifcation [1-3]. On the other hand, progress in the search of synthetic α-glucosidase inhibitors specially having heterocyclic rings [4] such as pyrazole [5], coumarins [6], fused pyrimidines [7], benzo[d]oxazol [8], bisbenzimidazoles [9], oxadiazole [10], xanthones [11], 4-quinazolones [12-14], and quinoxaline [15] derivatives has been also described. With the aim of looking for heterocyclic rings within the wide range of structural diversity in either natural or synthetic compounds displaying α-glucosidase inhibition we proceed to synthesize diferent fused heterocycles bearing quinolone, isoquinoline, xanthone, phtalimide and quinazolinone ring systems and those presenting α-glucosidase inhibition used as lead molecules for a structure-activity relationship program. Results and Discussion Chemistry The heterocyclic rings used for the screening analysis were