Table 3: Antifungal activity of 1,3,4-thiadiazole derivatives
An attempt was made to utilize the concept of bio-isosterism for the synthesis to afford novel fused thiadiazole, thiadiazine compounds by Sivasubramanian et al. The novel synthesized compounds were characterized by MP, IR, 1H NMR spectra. These synthesized compounds were subjected to anti-microbial and anti cancer studies. All the synthesized compounds in the present study showed significant activity against microbes when compared with that of ampicillin and ketoconazole as standards. Synthesized compounds (Fig. 14) were found to exhibit moderate cytotoxicity activities in all cell lines .
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Several new derivatives of 1,2,4-triazoles and 1,3,4-thiadiazole were synthesized by Mavrova et al and investigated for cytotoxic activity by trypan blue exclusion test (Fig. 15). The performed results revealed that some of the compounds showed good cytotoxicity against infected cells .
Cancer is a leading cause of death throughout the world and Malaysia is of no exception. However, the conventional treatments available for cancer disease, such as chemotherapy or radical surgery, eventually fail to exert control on the disease. Metastatic disease frequently develops even after these treatments and may cause death. Cancer chemoprevention has been an active area of research for several decades. Various efforts were done by different scientists like:
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The thiadiazole drugs were the first effective chemotherapeutic agents to be employed systematically for the prevention and cure of bacterial infection in human beings (e.g. Sulphamethazole). They are also choice for the drug as diuretic (e.g. Acetazolamide). Ceftazolene (antibiotic), Atibeprone (anti-depressant) etc .
JO - Turkish Journal of Chemistry
Method 4. In order to improve the yield and purity of the products, easy isolation or work up; researchers developed the new synthetic strategies, innovative methods, new reagents for the synthesis of thiadiazoles. Thiourea is introduced as a new reagent for the direct conversion of 2.5-diaryl- 1,3,4-oxadiazole to 2.5-diaryl-1,3,4-thiadiazole. In order to reduce the reaction time and to increase the yield, reaction is carried out in a sealed tube at water bath temperature for 10-15 hr.
T2 - Turkish Journal of Chemistry
Method 5. A series of fluorine-containing thiadiazoles were synthesized from thiosemicarbazides by conventional method by heating mixture of thiosemicarbazide and 2N sodium hydroxide, by green synthesis such as ultrasonification and microwave irradiation. The ultrasonication method, the reaction mixture was subjected to ultrasonic irradiated for 30-35 min at room temperature. The microwave irradiation technique involved the irradiation of the reaction mixture inside a microwave oven for 1 to 2.5 min at an output of 300W power, with short interruption of 15 sec.
JF - Turkish Journal of Chemistry
1,3,4-Thiadiazole and its derivatives continue to be of a great interest to a large number of researchers owing to their great pharmaceutical and industrial importance. 1,3,4-Thiadiazole was first described in 1882 by Fischer and further developed by Busch and his coworkers. The advent of sulfur drugs and the later discovery of mesoionic compounds greatly accelerated the rate of progress in this field. 1,3,4-Thiadiazoles were conveniently divided into three subclasses, one is Aromatic systems which include the neutral thiadiazole (1) and constitute a major part of this review. Second is mesoionic systems (2) which is defined as five-membered heterocycles which are not covalent or polar and possess a sextet of electrons in association with the five atoms comprising the ring. And lastly non aromatic systems such as the 1,3,4-thiadiazolines (3,4) and the tetrahydo 1,3,4-thiadiazolidines (5) (fig.1) .
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Method 6. Another method of synthesis of 2-Amino-5-aryl-1,3,4-thiadiazole is by the reaction of thiosemicarbazide, aromatic carboxylic acid in conc. sulphuric acid. Then the compound was converted to chloroacetyl derivative by its reaction with chloroacetyl chloride in the presence of sodium acetate in acetic acid. Finally it was transformed in to N-(5-(4-aminophenyl)-1,3,4-thiadiazole-2-yl)-2-chloroacetamide.