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Synthesis of novel thiadiazolotriazin-4-ones and study of their mosquito-larvicidal and antibacterial properties

, : Synthesis of novel thiadiazolotriazin-4-ones and study of their mosquito-larvicidal and antibacterial properties. European Journal of Medicinal Chemistry 84: 194-199

A series of novel 3-tert-butyl-7-(aryloxymethyl)-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-ones (5a-5n) were synthesized by refluxing 3,3-dimethyl-2-oxobutanoic acid (trimethyl pyruvic acid) (1) and thiocarbohydrazide (2) in ethanol as solvent for 12 h, to yield 3-mercapto-4-amino-6-tert-butyl-1,2,4-triazine-5(4H)-one (3) (Scheme 1), then the compound (3) was condensed with different substituted aryloxyacetic acids (4) in POCl3 at 90 °C for 8 h (Scheme 2). The structures of the newly synthesized compounds were confirmed by IR, (1)H NMR, (13)C NMR, elemental analyses and mass spectroscopic studies. Few of the synthesized compounds exhibited moderate mosquito-larvicidal and antibacterial activities. Among the novel derivatives, the compound (5f) showed relatively high larvicidal activity against a malaria vector. Compounds (5i) and (5m) exhibited a broad spectrum antibacterial activity against Gram positive and Gram negative species and hence they may be considered as drug candidates for bacterial pathogens.


PMID: 25019476

DOI: 10.1016/j.ejmech.2014.06.072

Other references

D'Avino, A.;, M.; Marmo, E., 1971: Experimental studies of the ototoxicity of some drugs. Minerva Otorinolaringologica 21(4): 156-161

Rourke, B.P., 1988: Socioemotional disturbances of learning disabled children. Journal of Consulting and Clinical Psychology 56(6): 801-810

Fredj, G.; Dietlin, F.; Barbier, G.; Jasmin, C.; Bonhomme, L.; Esctein, S.; Misset, J.L.; Meyer, P.; Kalifa, D.; Beugre, T., 1992: Comparison of tacrine (THA) hepatotoxicity in Alzheimer disease or AIDS patients. Previously used in Alzheimer disease Tacrine (THA): tetrahydroaminoacridine has shown a rise of hepatic transaminase enzyme activity (TEA) in 18% of patients for Summers and 19% for Ames. Although studies using THA from USA or Canada have noticed...

Villafuerte-Trisolini, B.; Adrianzén-Álvarez, F.; Duque, K.R.; Palacios-García, J.; Vizcarra-Escobar, D., 2017: Cyclic Alternating Pattern Associated with Catathrenia and Bruxism in a 10-Year-Old Patient. Cyclic alternating pattern (CAP) is widely recognized as an expression of sleep instability in electroencephalogram activity during non-rapid eye movement sleep. We report a case with sequences of CAP followed by bruxism and catathrenia in a 10-y-...

Longerich, B., 2007: The greed that is among us. Krankenpflege. Soins Infirmiers 100(1): 33-33

Voss, G.J.; Kump, D.Kevin.; Walker, J.A.; Voss, S.Randal., 2014: Variation in salamander tail regeneration is associated with genetic factors that determine tail morphology. Very little is known about the factors that cause variation in regenerative potential within and between species. Here, we used a genetic approach to identify heritable genetic factors that explain variation in tail regenerative outgrowth. A hybri...

Itoh, K.; Ozaki, A.; Yamamoto, T.; Mitsuoka, T., 1978: An autoclavable stainless steel isolator for small scale gnotobiotic experiments. A lightweight stainless steel autoclavable pentagon isolator was designed for experiments using gnotobiotic mice. The chamber, 400 x 450 x 350 mm, has an entry port 200 mm in diameter at the back and a window at the ceiling. The globes and two fil...

Jeon, G.Sun.; Byun, H.Jine.; Park, S.Kyung.; Park, S.Wook.; Kim, D.Woon.; Seo, J.Hoon.; Cha, C.Ik.; Cho, S.Sun., 2006: Induction of transcription factor A-myb expression in reactive astrocytes following an excitotoxic lesion in the mouse hippocampus. In the present study, we examined patterns of A-myb expression in the kainic acid (KA)-treated mouse hippocampus. Western blot analysis revealed that A-myb expression was dramatically increased in brain 3 days after KA treatment, and was sustaine...

Schmidt-J|orgensen, J., 1953: Stability of gelatin solutions. Dansk Tidsskrift for Farmaci 27(2): 37-42

Brunner, F.; Krneta, A., 1972: Side-to-side for "steal"?. Annals of Internal Medicine 77(2): 325-326