138995-89-8Relevant academic research and scientific papers
Synthesis and antimycobacterial activity of 3,5-disubstituted thiadiazine thiones
Katiyar,Tiwari,Tripathi,Srivastava,Chaturvedi,Srivastava,Srivastava
, p. 4369 - 4375 (2003)
A series of 3,5-disubstituted thiadiazine thiones (4-24) have been synthesized by reaction of primary amines with carbon disulphide followed by cyclocondensation of the resulting intermediate with formaldehyde and primary amines or amino acids. The compounds were screened for antitubercular activity in vitro against Mycobacterium tuberculosis H37Rv. Three compounds 4, 12 and 18 showed antimycobacterial activity with MIC 12.5 μg/mL. Compound 4, was tested in vitro against five multidrug resistant (MDR) strains of M. tuberculosis and was found to be active. Compound 4 also exhibited activity in vivo. While all the mice died in the untreated group, the mean survival time (MST) of the compound treated mice was enhanced, 33% mice were surviving in treated group and the load of bacilli in the lung was considerably less in the compound treated group than in the untreated control group.
Synthesis and antifungal activities of some new tetrahydro-2H-1,3,5-thiadiazine-2-thiones
Ertan,Ayyildiz,Yulug
, p. 1182 - 1185 (2007/10/02)
A number of new 3-benzyl-5-[α-(substituted)carboxymethyl]-tetrahydro-2H- 1,3,5-thiadiazine-2-thiones has been synthesized as prodrugs by incorporating the amine group of some amino acid into tetrahydro-2H-1,3,5-thiadiazine-2-thione ring. The compounds have been prepared by the reactions of benzylamine with potassium hydroxide, carbon disulphide formaldehyde and various amino acids. The structures of the compounds have been elucidated by UV, IR, 1H-NMR, mass spectra and elementary analysis. The in vitro activity of these compounds against yeast-like fungi (Candida albicans, C. parapsilosis, C. pseudotropicalis, C. stellatoidea) was investigated by tube dilution method. Their minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values were determined. All the compounds were found to be active between 3.12- 12.5 μg/ml against the four fungi tested.
