Validation of Inhibitory Activity of Thiazolidine-4-carboxylic Acid Derivatives against Novel Influenza Neuraminidase Enzyme

Abstract

Background: Neuraminidase enzymes are a large family found in a range of organisms. The best-known neuraminidase is viral neuraminidase, a drug target for the prevention of the spread of influenza infection. The viral neuraminidases are frequently used as antigenic determinants found on the surface of the influenza virus. Objective: Thiazolidine derivatives have been synthesized and explored previously, and further compounds have been designed on the basis of leading compounds. This research aimed to validate those previously synthesized compounds and a new series of compounds. Methods: A series of 28 compounds of thiazolidine-4-carboxylic acid derivatives were studied and evaluated for their ability to inhibit the neuraminidase (NA) of the influenza A virus. Twenty-eight compounds were differentiated into a training set of 21 compounds and a test set of 07 compounds. Results: The validated compounds demonstrated moderate inhibitory activity against influenza A neuraminidase. The most potent compound was acetaminophen mercapturate (C13H16N2O5S) (MW: 312.34). S-(5-acetamido-2-hydroxyphenyl)-N-acetyl-L-cysteine is an S-substituted N-acetyl-Lcysteine in which the S-substituent is specified as 5-acetamido-2-hydroxyphenyl. It acts as a drug metabolite, a human urinary metabolite, and a rat metabolite. It is a member of acetamides, an organic sulphide, a member of phenols and an S-substituted N-acetyl-L-cysteine. It derives from “paracetamol”. Conclusion: Validation of inhibitory activity of thiazolidine-4-carboxylic acid derivatives as novel influenza NA shows drug discovery of a more potent and reliable drug for the influenza virus.