{"title":"Validation of Inhibitory Activity of Thiazolidine-4-carboxylic Acid Derivatives against Novel Influenza Neuraminidase Enzyme","authors":"Aakanksha Yadav, N. Jain, Anita k","doi":"10.2174/2211544712666230406123325","DOIUrl":null,"url":null,"abstract":"\n\nNeuraminidase 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.\n\n\n\nStudied on a 28 series compound and came with the most potent drug towards Influenza\n\n\n\nThiazolidine 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.\n\n\n\nTo make the most potent drug with enhanced biological activity.\n\n\n\nA 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.\n\n\n\nA series of 28 compounds of thiazolidine-4-carboxylic acid derivatives was studied and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus. Compound was drawn on ChemSketch and further evaluated.\n\n\n\nThe 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-L-cysteine 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”.\n\n\n\nThe most potent compound is Acetaminophen mercapturate (C13H16N2O5S) (MW: 312.34) S-(5-acetamido-2-hydroxyphenyl)-N-acetyl-L-cysteine is an S-substituted N-acetyl-L-cysteine in which the S-substituent is specified as 5-acetamido-2-hydroxyphenyl.\n\n\n\nValidation 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.\n\n\n\nAll the studies and evaluation carried out in this paper is only to get the most potent compound or drug with enhanced biological activity.\n\n\n\nAs to it, 10 predicted compounds also being proposed in the given paper\n","PeriodicalId":10862,"journal":{"name":"Current Catalysis","volume":"7 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-04-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Catalysis","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/2211544712666230406123325","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0
Abstract
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.
Studied on a 28 series compound and came with the most potent drug towards Influenza
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.
To make the most potent drug with enhanced biological activity.
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.
A series of 28 compounds of thiazolidine-4-carboxylic acid derivatives was studied and evaluated for their ability to inhibit neuraminidase (NA) of influenza A virus. Compound was drawn on ChemSketch and further evaluated.
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-L-cysteine 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”.
The most potent compound is Acetaminophen mercapturate (C13H16N2O5S) (MW: 312.34) S-(5-acetamido-2-hydroxyphenyl)-N-acetyl-L-cysteine is an S-substituted N-acetyl-L-cysteine in which the S-substituent is specified as 5-acetamido-2-hydroxyphenyl.
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.
All the studies and evaluation carried out in this paper is only to get the most potent compound or drug with enhanced biological activity.
As to it, 10 predicted compounds also being proposed in the given paper