Gupta A, Mishra P, Kashaw S K, Jatav V
Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar-470 003, India.
Indian J Pharm Sci. 2008 Jul-Aug;70(4):535-8. doi: 10.4103/0250-474X.44614.
A series of 1,2,4-dithiazole were synthesized from 1,2,4-thiadiazoles in the presence of CS(2) and evaluated for their antimicrobial, anticonvulsant, analgesic and neurotoxicity potential. The compounds provided significant protection against maximal electroshock-induced seizures and seizures induced by 300 mg/kg of subcutaneous pentylenetetrazole administration. The designed compounds (3a-g) were screened in vitro for antibacterial activity against Staphylococcus aureus Escherichia coli, Bacillus subtilis and Pseudomonas aeruginosa and antifungal activity in fungal strains of Candida albicans and Aspergillus niger. Synthesized compounds exhibited moderate antibacterial and antifungal activity. N,N -Di-naphthalen-1-yl-N -(thioxo-5H -[1,2,4]dithiazol-3-yl)-guanidine and N,N -Bis-(4-fluoro-phenyl)-N -(5-thioxo-5H -[1,2,4]dithiazol-3-yl)-guanidine showed analgesic activity by tail flick method.
在二硫化碳存在的情况下，由1,2,4-噻二唑合成了一系列1,2,4-二噻唑，并对其抗菌、抗惊厥、镇痛和神经毒性潜力进行了评估。这些化合物对最大电休克诱导的癫痫发作以及皮下注射300mg/kg戊四氮诱导的癫痫发作提供了显著的保护作用。对设计的化合物（3a-g）进行了体外筛选，以检测其对金黄色葡萄球菌、大肠杆菌、枯草芽孢杆菌和铜绿假单胞菌的抗菌活性，以及对白色念珠菌和黑曲霉真菌菌株的抗真菌活性。合成的化合物表现出中等的抗菌和抗真菌活性。N,N-二萘-1-基-N-(硫代-5H-[1,2,4]二噻唑-3-基)-胍和N,N-双-(4-氟苯基)-N-(5-硫代-5H-[1,2,4]二噻唑-3-基)-胍通过甩尾法显示出镇痛活性。
