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JSIR Vol.64(08) [August 2005] >


Title: Synthesis, anti-fungal, anti-tumor and anti-inflammatory activities of some new 5-(N-substitutedarylidenehydrazono)-2-(4-chloroaryl)-3-oxo-1,2,4-thiadiazolidines
Authors: Manna, Paresh
Narang, and K K
Keywords: 1,2,4-Thiadiazolidines
Synthesis
Characterization
Anti-fungal
Anti-tumor
Anti-inflammatory
Issue Date: Aug-2005
Publisher: CSIR
IPC CodeC10J1/20
Abstract: 5-(N-Substitutedarylidenehydrazono)-2-(4-chloroaryl)-3-oxo-1,2,4-thiadiazolidines (IVa-e) have been synthesized by oxidative debenzylation and cyclization with bromine in chloroform from the corresponding 5-(4-chloroaryl)-1-(substitutedarylideneamino)-2-S-benzyliso-4-biurets (IIIa-e) or by the oxidation of corresponding 1-(substituted¬≠arylideneamino)-5-(4-chloroaryl)-2,4-thiobiurets (Va-e), obtained from IIIa-e by reductive debenzylation with hydrogen sulphide in a mixture of pyridine and triethylamine. 2-S-Benzyliso-4-biurets (IIIa-e), in turn, were prepared by the condensation of 2-S-benzyliso-1-substitutedarylthiosemi-carbazone (IIa-e) with 4-chlorophenylisocyanate. Thiadiazolidines (IVa-e) have been characterized by their element analyses, IR, 1H-NMR and 13C-NMR. Anti-fungal screening of these compounds against ten fungi has been done by glass slides methods. The compound (1000 mg/ml) containing dichlorogroup (IVe) showed maximum inhibitory effect (99.6 %) against Fusarium udum. The compound possessing dichloro group (IVe) have potent anti-inflammatory and anti-tumor properties as they down regulate NF-kB transcription factor.
Page(s): 585-593
ISSN: 0975-1084 (Online); 0022-4456 (Print)
Source:JSIR Vol.64(08) [August 2005]

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