- 2-mercapto-5-methyl-1,3,4-thiadiazole compound and synthesis method thereof
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The invention relates to the technical field of chemical synthesis, particularly to a 2-mercapto-5-methyl-1,3,4-thiadiazole compound and a synthesis method thereof. The synthesis method of the 2-mercapto-5-methyl-1,3,4-thiadiazole compound comprises the following steps: mixing and emulsifying a sulfur-containing compound and a nitrogen-containing compound, and carrying out a cyclization reaction under the action of a catalyst. The synthesis method is simple to operate, the synthesis conditions are easy to realize, the yield is high, and the purity of the prepared 2-mercapto-5-methyl-1,3,4-thiadiazole compound is also high.
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Paragraph 0042-0061
(2020/09/16)
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- NOVEL CEPHALOSPORIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF
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The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
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Paragraph 0199
(2014/03/25)
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- NOVEL CEPHALOSPORIN DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
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Page/Page column 53
(2012/10/23)
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- Azo dye and azo compound
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An azo dye including a compound represented by formula (I): wherein R1 represents a hydroxyl group, an aliphatic sulfonyl amino group, an aryl sulfonyl amino group, an aliphatic oxy group, an aryloxy group, or -CH(R2)(R3); R2 and R3 each represent a substituent with a a value of the Hammett's rule in the range of 0.2 or more and less than 1.4, and may be identical to or different from each other; W represents a sulfur atom or -N-(-R4)-; R4 represents a substituent; R5 represents a substituent; X, Y, and Z each represent an atom required for forming a five-membered aromatic heterocycle, where at least one atom of X, Y, and Z represents a nitrogen atom but both X and Y do not represent a carbon atom when Z represents a nitrogen atom; and R6 represents a hydrogen atom or a substituent, n represents 1 or 2, and two R6s may be coupled together to form an aromatic ring or a heteroaromatic ring when n represents 2.
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Page/Page column 19
(2008/12/07)
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- Synthesis and evaluation of novel dipeptide-bound 1,2,4-thiadiazoles as irreversible inhibitors of guinea pig liver transglutaminase.
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Herein we report the synthesis and evaluation of 14 novel peptides as potential irreversible inactivators of guinea pig liver transglutaminase (TGase). These peptides were designed to resemble Cbz-L-Gln-Gly, known to be a good TGase substrate, and to include a 1,2,4-thiadiazole group. The side chain length of the amino acid residue bearing the inhibitor group was also varied in order to permit investigation of this effect. Their inactivation rate constants were measured using a direct continuous spectrophotometric method and were found to vary between 0.330 to 0.89 microM(-1) min(-1).
- Marrano,de Macedo,Gagnon,Lapierre,Gravel,Keillor
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p. 3231 - 3241
(2007/10/03)
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- Method for preparing 5-amino-1,2,4-thiadiazol acetic acid derivatives
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The invention provides useful intermediates as acylating agents for preparing 7-acylaminocephalosporin compounds which show excellent antimicrobial activities. More particularly, the present invention relates to a process for preparing 5-amino-1,2,4-thiadiazole acetic acid derivatives.
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