4454-63-1Relevant academic research and scientific papers
Thiadiazole thiazolinone compounds, and preparation method and application thereof
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Paragraph 0052; 0086; 0092-0095, (2018/04/03)
The invention discloses thiadiazole thiazolinone compounds. The thiadiazole thiazolinone compounds have a chemical structure as shown in a formula which is described in the specification. In the formula, R is selected from the group consisting of chemical groups which are described in the specification. The preparation method comprises the following steps: with thiosemicarbazide as a raw material,carrying out cyclodehydration with formic acid under the catalytic condition of concentrated sulfuric acid so as to synthesize a first intermediate product, then carrying out synthesizing with chloroacetyl chloride so as to obtain a second intermediate product, carrying out cyclization under the action of ammonium thiocyanate so as to synthesize a third intermediate product, and allowing a thirdcompound to react with R1 through a Knoevenagle condensation reaction so as to obtain the thiadiazole thiazolinone compounds. According to the invention, by utilization of an active structure splicingprinciple, bis-heterocyclic compounds with a thiazole ring and thiazolinone are synthesized through structure splicing of 1,3,4-thiadiazole and 4-thiazolinone, so bis-heterocyclic pesticide derivatives with excellent activity are obtained; a novel green pesticide variety with high activity, low toxicity and less pollution is selected; and the thiadiazole thiazolinone compounds can be applied to bactericides or pesticides.
Synthesis, antioxidant, and antitumor evaluation of certain new N-substituted-2-amino-1,3,4-thiadiazoles
Hamama, Wafaa S.,Gouda, Moustafa A.,Badr, Marwa H.,Zoorob, Hanafi H.
, p. 3556 - 3565 (2013/07/26)
Reaction of 2-amino-1,3,4-thiadiazole (1) with chloroacetyl chloride afforded the chloroacetamide 2 which used as starting compound for the synthesis of 2-thiocyanatoacetamide 3 and N-(1,3,4-thiadiazol-2-yl)acetamides 5-9 via reaction of 1 with various re
Synthesis and antifungal activity of thiadiazole-functionalized chitosan derivatives
Li, Qing,Ren, Jianming,Dong, Fang,Feng, Yan,Gu, Guodong,Guo, Zhanyong
, p. 103 - 107 (2013/06/27)
A groups of novel water soluble chitosan derivatives containing 1,3,4-thiadiazole group were synthesized including 1,3,4-thiadiazole (TPCTS), 2-methyl-1,3,4-thiadiazole (MTPCTS), and 2-phenyl-1,3,4-thiadiazole (PTPCTS). Their antifungal activity against three kinds of phytopathogens was estimated by hypha measurement in vitro, and the fungicidal assessment shows that the synthesized chitosan derivatives have excellent activity against tested fungi. Of all the synthesized chitosan derivatives, MTPCTS inhibited the growth of the tested phytopathogens most effectively with inhibitory indices of 75.3%, 82.5%, and 65.8% against Colletotrichum lagenarium (Pass) Ell.et halst, Phomopsis asparagi (Sacc.) Bubak, and Monilinia fructicola (Wint.) Honey respectively at 1.0 mg/mL. These indices are higher than those of chitosan. These data also demonstrate that the hydrophobic moiety (alkyl and phenyl) and the length of alkyl substituent in thiadiazole tend to affect the antifungal activity of chitosan derivatives. It is hypothesized that thiadiazole groups enable the synthesized chitosan to possess obviously better antifungal activity and good solubility in water.
Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7
Zheng, Weihong,Degterev, Alexei,Hsu, Emily,Yuan, Junying,Yuan, Chengye
scheme or table, p. 4932 - 4935 (2009/05/26)
Necroptosis is a regulated caspase-independent cell death mechanism characterized by morphological features resembling non-regulated necrosis. Necrotatin-7 (Nec-7), a novel potent small-molecule inhibitor of necroptosis, is structurally distinct from previously described necrostatins (Nec-1, Nec-3, Nec-4 and Nec-5). Here, we describe a series of structural modifications and the structure-activity relationship (SAR) of the Nec-7 series for inhibiting necroptosis.
