DESIGN AND SYNTHESIS OF 1, 3, 4-THIADIAZOLES AS ANTIINFLAMMATORY CANDIDATE Authors: Kadam Satwashila S , KHADE HARSHAD P, JADHAV PANKAJ A AND LADE RUPALI P
ABSTRACT
The N-substituted chloroacetamides (A), 2-chloropropionamides (B) and 3-
chloropropionamides (C) were synthesized by acetylating respective amine using
chloroacetylchloride, 2-chloropropanoyl chloride and 3-chloropropanoyl chloride
respectively. These compounds were characterized by TLC, melting point and IR spectra.
The N –substituted 2-{ [5 - (pyridine-4-yl) - 1, 3, 4 – thiadiazol – 2 -yl]sulfanyl }
acetamide (4a-c), N-substituted-2-{[5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl]sulfanyl}
propanamide (5a-c) and N-substituted-3-{[5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl]sulfanyl}
propanamide (6a-c) derivatives were prepared by condensing sodium salt of 5-(4-pyridyl)-2-
mercapto-1,3,4-thiadiazole (3) and N-substituted chloroacetamides (A), N-substituted ?chloropropionamides (B) and N-substituted ?-chloropropionamides (C) respectively.
Structure of all synthesized compound was confirmed by IR, and 1H NMR. All synthesized
compounds were screened for their anti-inflammatory activity by carrageenan induced rat paw
edema model compared to the standard drug diclofenac. The synthesized compounds showed
anti-inflammatory activity ranging from 26.97% to 59.99%; whereas standard drug
Diclofenac sodium showed 63.70% inhibition after 4 hr.
Keywords: NSAID’s, Anti-inflammatory, Acetamide, Propanamide, 1, 3, 4-Thiadiazoles
Publication date: 15/12/2021 https://ijbpas.com/pdf/2021/December/MS_IJBPAS_2021_DEC_SPCL_1019.pdfDownload PDFhttps://doi.org/10.31032/IJBPAS/2021/10.12.1019