- Anticandidal activity of pyrimidine-peptide conjugates
-
The ability of conjugates of peptides and 5-fluorocytosine or 5-fluoro-ortic acid to enter 'Candida albicans' was investigated. A number of conjugates of 5-fluoro-orotic acid and peptides were synthesized using 1-(ethoxycarbonyl)-2-ethoxy-1,2-dihydroquinoline as the coupling agent. Orotyl-L-leucyl-L-leucine, 5-fluoro-4-(N-succinamoyl-L-alanyl-L-leucine)-2(1H)-pyrimidinone [a 5-fluorocytosine derivative], and 5-fluoro-orotyl-L-leucyl-L-leucine all inhibited the uptake of trimethionine into 'C. albicans' WD 18-4. Inhibition by 5-fluoro-orotyl-L-leucine was competitive, as judged using double-reciprocal plots. Evaluation of minimum inhibitory concentrations of peptide - 5 - fluorocytosine conjugates suggest that these conjugates enter 'C. albicans' in the intact form. These results provide the first experimental evidence that peptides can carry pyrimidines into a eukaryote.
- Ti,Steinfeld,Naider,Gulumoglu,Lewis,Becker
-
-
Read Online
- Synthesis process of flocculant additive 5-fluoroorotic acid
-
The invention discloses the technical field of fine chemical engineering and discloses a synthesis process of the flocculant additive 5-fluoroorotic acid. The synthesis process comprises the followingspecific steps that S1, fluoroacetate and oxalate undergo a condensation reaction under the alkaline condition, wherein the condensation reaction temperature ranges from 0 DEG C to 50 DEG C and the reaction time ranges from 1 h to 10 h, S2, a product obtained after the condensation reaction in the step S1 and an O-methylisourea salt undergo a cyclization reaction so that 2-dimethoxy-4-hydroxy-5-fluoro-6-formate pyrimidine is obtained, and S3, 2-dimethoxy-4-hydroxy-5-fluoro-6-formate pyrimidine and hydrochloric acid undergo a hydrolysis reaction so that 5-fluoroorotic acid is obtained. The scheme provides a synthetic process route of the compound 5-fluorolactic acid, and the process route has the advantages of short steps, simple operation, easily available raw materials, low cost and easypurification, and is suitable for industrial production.
- -
-
Paragraph 0044-0045
(2020/08/06)
-
