- Preparation method of 2-methylamino-5-t-butyl-1,3,4-thiadiazole
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The invention relates to a preparation method of 2-methylamino-5-t-butyl-1,3,4-thiadiazole. The method comprises the following steps: adding 4-methylthiosemicarbazide and pivaloyl chloride into a reaction kettle, adding a first organic solvent, performing a reaction, heating the obtained solution, adding the dehydrating agent pivaloyl chloride again, carrying out a reaction for 1-3 h, cooling theobtained solution to 30-60 DEG C, filtering the cooled solution, and adding water to the obtained filtrate to obtain pivalic acid; and adding an alkali to a solid obtained by the filtration in order to adjust the pH value to 7-8, adding a second organic solvent, performing stirring, and carrying out reduced pressure distillation on the obtained organic phase to obtain the 2-methylamino-5-t-butyl-1,3,4-thiadiazole. The method has few side reactions, and the pivalic acid produced by the reaction can be used to further prepare pivaloyl chloride for reuse, so the method is in line with the development direction of modern green chemistry.
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Paragraph 0021-0032
(2019/02/04)
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- 3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-β-lactamase inhibitors
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The production of β-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against β-lactam antibiotics. While inhibitors of serine-β-lactamases are widely used in combination therapy with β-lactam antibiotics, there are no clinically available inhibitors of metallo-β-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods.
- Faridoon,Hussein, Waleed M.,Vella, Peter,Islam, Nazar Ul,Ollis, David L.,Schenk, Gerhard,McGeary, Ross P.
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supporting information; experimental part
p. 380 - 386
(2012/02/04)
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