1, 3, 4-Thiadiazole and 1, 2, 4-triazole-3(4 H )-thione bearing salicylate moiety: synthesis and evaluation as anti- Candida albicans

Abstract Dramatically increased occurrence of both superficial and invasive fungal infections has been observed. Candida albicans appear to be the main etiological agent of invasive fungal infections. The anti-C. albicans activity of thiosemicarbazide, 1,3,4-Thiadiazole, and 1,2,4-triazole-3(4H)-thione compounds (compounds 3-23) were investigated. The MIC values of thiadiazole and triazole derivatives 10-23 were in the range of 0.08-0.17 µmol mL-1, while that of fluconazole was 0.052 µmol mL-1. Compound 11 (5-(2-(4-chlorobenzyloxy)phenyl)-N-allyl-1,3,4-thiadiazol-2-amine) and compound 18 (5-(2-(4-chlorobenzyloxy)phenyl)-4-allyl-2H-1,2,4-triazole-3(4H)-thione) were found to be the most active compounds, with MIC values of 0.08 µmol mL-1. The newly synthesized thiadiazole and triazole compounds (compounds 10-23) showed promising anti-Candida activity. The allyl substituent-bearing compounds 11 and 18 exhibited significant anti-Candida albicans activity and showed a binding mode as well as the fluconazole x-ray structure.

The synthesis and antitumor activity of novel N-aryl(arylazo-1,3,4-thiadiazoles) sulfonamides derivatives / 中国药学杂志

OBJECTIVE: To study the synthesis and antitumor activity of N-aryl(arylazo-1, 3, 4-thiadiazoles)sulfonamides derivatives. METHODS: The title compounds were synthesized by the condensation reaction of aromatic amine, salicylaldehyde, thiosemicarbazide and benzene sulfochloride, and their antitumor activities against L1210 and B16 cells were assayed by MTT method. RESULTS: A series of novel N-aryl(arylazo-1, 3, 4-Thiadiazoles)sulfonamides derivatives were synthesized, and their structures were confirmed by IR, MS, 1H-NMR and elemental analysis. Compounds 5a and 5g showed potential antitumor activity. CONCLUSION: N-aryl(arylazo-1, 3, 4-thiadiazoles)sulfonamides derivatives may be useful antitumor candidate drugs.

Synthesis and antimicrobial activity of some newer biphenyl imidazo [2,1-b] [1,3,4] thiadiazole derivatives.

In the present study, we have reported the synthesis of some novel heterocyclic derivatives comprising imidazole and 1,3,4-thiadiazole containing moiety. Imidazothiadiazoles are of interest because of their diverse biological activities and clinical applications. Reactions of biphenyl carboxylic acid with thiosemicarbazide in the presence of phosphorous oxychloride resulted in biphenyl containing 2-amino-1,3,4-thiadiazole which is then further subjected to condensation with α-bromoarylketone under reflux in dry ethanol. The structures of the newly synthesised compounds were characterized by various spectral techniques and screened for antibacterial activity against strains of Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis, and antifungal activity against Candida albicans, Saccharomyces cerevisiae and Aspergillus niger. The compounds exhibited moderate to good activity when compared with standards.

Review on Biological Activities of 1,3,4-Thiadiazole Derivatives.

The Thiadiazole & their derivatives shown the number of pharmacological activity as anti microbial ,anti inflammatory activity, anti tubercular activity, ant diabetic activity, diuretics, anti depressant & cytotoxic activity. these thiadiazole are the heterocyclic compound which contain the five member ring & nitrogen & sulphur. In this paper we mention the recent derivatives of 1,3,4thiadiazole & their activity.

A MORPHOLOGICAL STUDY ON THE NEURAL TUBE DEFECTS INDUCED BY BIS-A-TDA / 解剖学报

30 sexually mature, virgin female SD rats, weighed 200-270 g were mated and used for the study of the teratogenic effect of N, N-methylene-bis (2-amino-1,3,4-thiadiazole) (Bis-A-TDA) on fetal neural tube formation and to explore the possible morphological mechanism of neural tube defects (NTD). In the morning of day 10 of gestation, the experimental group was administered with 10mg/kg body weight Bis-A-TDA mixed in peanut oil, and the control group with the same amount of peanut oil only. The results Showed that the incidence of NTD was 52.9% and the majority of NTD were excencephaly and encephalocele in the experimental group. In the early stage of NTD formation, some neuroepithelial cells showed vacuolated degeneration and necrosis, and the mitochondria became swollen and with indistinct or even disappeared crista. The intercellular spaces widened, and some cells escaped into the lumen of neural tube. The mitotic index of neuroepitbelial cells were sharply decreased. In the closure region of the telencephalon, similar changes of the neuroepithelium were present also, and decreased migration of mesodermal cells was noted. We consider the failure of cranial neural folds to approximate and closure was caused mainly by the damage of neuroepithelial cells, inhibition of cell proliferation, alteration of intercellular junctions and the changes of topographical arrangement of the neuroepithelium. The damage and delayed migration of mesodermal cells might also be involved in this event.