Hdl Handle:
http://hdl.handle.net/10675.2/621307
Title:
Design & Synthesis of Pyrazinamide Hybrid Conjugates as Potential Anti-tubercular Agents
Authors:
Torkian,Behrad; Panda, Siva S.
Abstract:
Tuberculosis (TB) is a bacterial pathogen caused by Mycobacterium tuberculosis, which generally causes pulmonary infection and is extremely pervasive within the lungs and between subjects. Pyrazinamide (PZA) is a first-line prodrug used synergistically with two or more chemotherapies to eradicate TB. PZA is hydrolyzed to its active constituent, pyrazinoic acid, intracellularly in M. tuberculosis via pyrazinamidase. With prolonged administration of the recommended dose, harmful side effects have been reported: hepatitis, acute hypertension, thrombocytopenia, and gastrointestinal discomfort Drug-amino acid conjugates are used because of increased tissue delivery, in which the amino acids act as effective carriers of these agents while maintaining, and even amplifying, their bioactive integrity. Amino acid conjugates can increase bioavailability and quantitatively decrease the required amount of active drug thus preventing toxic side effects. We have synthesized several pyrazinamide conjugates with secondary amines via amino acid linkers with retention of chiral integrity of the desired products. Secondary amines are known for enhancing biological properties of various potential molecules. All the synthesized compounds were characterized by NMR and X-ray studies. The synthesized conjugates are expected to have better anti-tubercular properties with less side effects.
Affiliation:
Department of Chemistry & Physics
Issue Date:
Mar-2017
URI:
http://hdl.handle.net/10675.2/621307
Type:
Presentation
Language:
en
Description:
Presentation given at the 18th Annual Phi Kappa Phi Student Research and Fine Arts Conference
Appears in Collections:
Department of Chemistry and Physics: Student Research and Presentations; 18th Annual PKP Student Research and Fine Arts Conference: Oral Symposia II

Full metadata record

DC FieldValue Language
dc.contributor.authorTorkian,Behraden
dc.contributor.authorPanda, Siva S.en
dc.date.accessioned2017-03-06T19:45:11Z-
dc.date.available2017-03-06T19:45:11Z-
dc.date.issued2017-03-
dc.identifier.urihttp://hdl.handle.net/10675.2/621307-
dc.descriptionPresentation given at the 18th Annual Phi Kappa Phi Student Research and Fine Arts Conferenceen
dc.description.abstractTuberculosis (TB) is a bacterial pathogen caused by Mycobacterium tuberculosis, which generally causes pulmonary infection and is extremely pervasive within the lungs and between subjects. Pyrazinamide (PZA) is a first-line prodrug used synergistically with two or more chemotherapies to eradicate TB. PZA is hydrolyzed to its active constituent, pyrazinoic acid, intracellularly in M. tuberculosis via pyrazinamidase. With prolonged administration of the recommended dose, harmful side effects have been reported: hepatitis, acute hypertension, thrombocytopenia, and gastrointestinal discomfort Drug-amino acid conjugates are used because of increased tissue delivery, in which the amino acids act as effective carriers of these agents while maintaining, and even amplifying, their bioactive integrity. Amino acid conjugates can increase bioavailability and quantitatively decrease the required amount of active drug thus preventing toxic side effects. We have synthesized several pyrazinamide conjugates with secondary amines via amino acid linkers with retention of chiral integrity of the desired products. Secondary amines are known for enhancing biological properties of various potential molecules. All the synthesized compounds were characterized by NMR and X-ray studies. The synthesized conjugates are expected to have better anti-tubercular properties with less side effects.en
dc.language.isoenen
dc.subjectTuberculosisen
dc.subjectPyrazinamideen
dc.subjectAmino Acidsen
dc.titleDesign & Synthesis of Pyrazinamide Hybrid Conjugates as Potential Anti-tubercular Agentsen
dc.typePresentationen
dc.contributor.departmentDepartment of Chemistry & Physicsen
All Items in Scholarly Commons are protected by copyright, with all rights reserved, unless otherwise indicated.