151392-10-8Relevant articles and documents
Synthesis and antibacterial activity of a series 1-aryl-2-mercapto-5--1,3,4-triazoles, thiadiazoles and 2--3,4,5-trisubstituted pyrazoles
Nagrund, L. V. G.,Reddy, G. R. N.,Hariprasad, V.
, p. 499 - 502 (2007/10/03)
A series of new 1-aryl-2-mercapto-5--1,3,4-triazoles, 2-arylamino-5--1,3,4-thiadiazoles, p-acetamido(phenoxy)acetyl thio-semicarbazides and 2--3-amino-4-carboxamido-5-methylthiopyrazole have been prepared and evaluated for comparative antibacterial activity.The antibacterial activity of the target compounds and their relevant reference agent have been determined in vitro using serial 2-fold dilution technique on an assortment of Gram negative and Gram positive organisms.It has been observed that the in vitro antibacterial activity of cyclized 1,3,4-triazoles and 1,3,4-thiadiazoles are significantly greater than thiosemicarbazides.The derivatives 4b, 5b have better in vitro antibacterial activity.
Anti-inflammatory activity of substituted 1,3,4-oxadiazoles
Nargund,Reddy,Hariprasad
, p. 246 - 248 (2007/10/02)
Various 5-[[(acetamidophen-4-yl)oxy]methyl]-2-(p-substituted phenylamino)- 1,3,4-oxadiazoles (4a-4d) were synthesized by cyclization of the corresponding N1-[[(acetamidophen-4-yl)oxy]acetyl]-N4-(p-substituted phenylamino)-3-thiosemicarbazides (3a-3d). All four of the thiosemicarbazides [250 mg/kg, orally (p.o.)] and the corresponding oxadiazoles (250 mg, p.o.) possessed anti-inflammatory activity. In the Carrageenan-induced edema test in rat paw, the activity ranged from 28 to 47% for 3a-3d and 44 to 63% for 4a-4d, with indomethacin (10 mg/kg, p.o.), used as the standard reference drug, showing 88.5% protection. The compounds (1 mM) were also tested for the inhibition of bovine serum albumin denaturation, and this activity ranged from 27 to 68%. No correlation was seen between the anti-inflammatory activity of 3a-4d and the inhibition of denaturation of bovine serum albumin. The low toxicity of these compounds was reflected by their high approximate 50% lethal dose (LD50) values, ranging from 2000 to 2500 mg/kg.