ABSTRACT
The synthesis of 2-furyl-5-(substituted)-1,3,4-oxadiazoles was carried out by microwave irradiation of 2-furoic acid and ethanol followed by subsequent hydrazinolysis with hydrazine hydrate. Finally furan-2-acid hydrazide was treated with appropriate carboxylic acid in the presence of phosphorous oxychloride to produce title compounds. The structures of the newly synthesized compounds were established on the basis of spectral analysis such as IR, H1NMR and Mass spectral data. The synthesized compounds were screened for their anti-tubercular activity.
ABSTRACT
Background: Tuberculosis holds one of the top places on the list of the main cause of death in India. At times the patients fail to respond to treatment with anti tubercular drugs, drug resistance being one of the reasons. The increasing incidence of MDR- and XDR-TB worldwide highlight the urgent need to search for newer anti-tubercular drugs. Objectives: The present study was carried out to assess the antitubercular activity of Lawsonia inermis, and if any, to compare it with ethambutol by "in vitro" method. Materials and Methods: From sputum samples of patients of pulmonary tuberculosis, who had not received any antitubercular drug earlier, the acid-fast bacilli were cultured and identified. Resistance ratio method was followed. For each isolate, (originally from the sputum samples) two sets of L-J slants containing ethambutol, in serially doubling concentration ranging from 1mcg/ml to 16 mcg/ml and L-J slants containing L.inermis leaves aqueous extract (2%) in serial doubling concentration ranging from 3 mcg/ml to 48 mcg/ml were prepared. One set for inoculating with test strain and the other with standard H37Rv strain. Each set had a drug/extract free L-J slant (control). All the L-J slants were labeled with appropriate drug concentrations and incubated at 37° C for 8 weeks for growth. Result & Conclusion: The MIC for ethambutol for both test as well as standard H37Rv strain was 4 mcg/ml by Resistance ratio method. The number of colonies (test and standard H37Rv) on all the L-J slants containing L.inermis extract were more than 100. Thus the aqueous extract of L.inermis leaves used, did not show antitubercular activity in the concentrations of 3 to 48 mcg/ml in the Lowenstein – Jenson media in the present laboratory set up. It is suggested that further studies may be undertaken to confirm the results of the present study.