Sahu Jagdish K, Ganguly Swastika, Kaushik Atul
Department of Pharmaceutical Chemistry, Institute of Professional Studies College of Pharmacy, Gwalior, Madhya Pradesh, India.
Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi, Jharkhand, India.
J Adv Pharm Technol Res. 2014 Apr;5(2):90-5. doi: 10.4103/2231-4040.133434.
In the present investigation, the synthesis and antimicrobial evaluation of 1,2,4-triazolo [3,4-b][1,3,4] thiadiazine including different pharmacophores are aimed at. In this study, a series of 6-aryl-3- (3,4 -dialkoxyphenyl)-7H -[1,2,4]triazolo [3,4-b][1,3,4] thiadiazine (7a-7k) was synthesized by condensing 4-amino-5-(3,4-dialkoxyphenyl)-4H-[1,2,4]- triazole-3-thiol (6) with various aromatic carboxylic acids in the presence of phenacyl bromides through one-pot reaction. Eleven fused heterocyclic derivatives were successfully synthesized. The structures of these newly synthesized compounds were characterized by IR, (1)H NMR and mass spectroscopic studies. All the synthesized compounds were screened for their antimicrobial evaluation. Some of the compounds exhibited promising antimicrobial activity. From the present study it may be concluded that synthesized compounds are fruitful in terms of their structural novelty and marked biological activities. These compounds could be further modified to develop potential and safer antifungal agents.
在本研究中，旨在合成并评估含不同药效基团的1,2,4-三唑并[3,4-b][1,3,4]噻二嗪的抗菌性能。在本研究中，通过4-氨基-5-(3,4-二烷氧基苯基)-4H-[1,2,4]-三唑-3-硫醇(6)与各种芳香羧酸在溴化苯甲酰存在下通过一锅反应缩合，合成了一系列6-芳基-3-(3,4-二烷氧基苯基)-7H-[1,2,4]三唑并[3,4-b][1,3,4]噻二嗪(7a - 7k)。成功合成了11种稠合杂环衍生物。通过红外光谱、¹H核磁共振和质谱研究对这些新合成化合物的结构进行了表征。对所有合成化合物进行了抗菌性能评估。一些化合物表现出良好的抗菌活性。从本研究可以得出结论，合成的化合物在结构新颖性和显著的生物活性方面成果丰硕。这些化合物可以进一步修饰以开发潜在的、更安全的抗真菌剂。
