ABSTRACT
A series of novel 2, 5-disubstituted 1, 3, 4-Oxadiazole derivatives as a potential anti-inflammatory, and anti-oxidant agent were synthesized via cyclisation. Hydrazide molecule treated with substituted acids in the presence of phosphorus oxychloride (POCl3) as an efficient reagent as well as solvent by conventional method with shorter reaction time and excellent yield. The newly synthesized 1, 3, 4- oxadiazole derivatives exhibited excellent to good anti-inflammatory and anti-oxidant activities compaired to the standard drugs. Molecular docking study on the crucial anti-inflammatory target-cyclooxygenase-2 (COX-2) revealed the ability of the scaffold to correctly recognize the active site and achieve significant bonded and non-bonded interactions with key residues therein. This study could identify potential compounds which can be pertinent starting points for structure-based drug design to obtain newer anti-inflammatory agents.
Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Antioxidants/pharmacology , Biphenyl Compounds/antagonists & inhibitors , Cyclooxygenase 2 Inhibitors/pharmacology , Molecular Docking Simulation , Oxadiazoles/pharmacology , Picrates/antagonists & inhibitors , Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Antioxidants/chemical synthesis , Antioxidants/chemistry , Cyclooxygenase 2/metabolism , Cyclooxygenase 2 Inhibitors/chemical synthesis , Cyclooxygenase 2 Inhibitors/chemistry , Dose-Response Relationship, Drug , Humans , Molecular Structure , Oxadiazoles/chemical synthesis , Oxadiazoles/chemistry , Structure-Activity RelationshipABSTRACT
An unknown impurity was observed during stability studies of Gabapentin capsules. This impurity has been identified, synthesized, isolated and characterized using modern analytical tool. The novel impurity was confirmed as adduct of Gabapentin and lactose; an excipient used in formulation. The elucidated impurity was further confirmed by its synthesis, which was formed due to Maillard reaction and Amadori rearrangement.
Subject(s)
Amines/chemistry , Cyclohexanecarboxylic Acids/chemistry , gamma-Aminobutyric Acid/chemistry , Chemistry, Pharmaceutical/methods , Drug Contamination , Excipients/chemistry , Gabapentin , Lactose/chemistry , Maillard ReactionABSTRACT
A new unknown impurity was observed in accelerated stability studies of Metoprolol tartrate tablets. This impurity has been identified, synthesized and characterized through different spectral studies and confirmed as an adduct of lactose and Metoprolol formed by Maillard reaction.
