Design and syntheses of gramicidin S analogs, cyclo(-X-Leu-X-D-Phe-Pro-)2 (X=His, Lys, Orn, Dab and Dap).

Tamaki M; Fujinuma K; Harada T; Takanashi K; Shindo M; Kimura M; Uchida Y

首页> 外文期刊>The Journal of Antibiotics: An International Journal >Design and syntheses of gramicidin S analogs, cyclo(-X-Leu-X-D-Phe-Pro-)2 (X=His, Lys, Orn, Dab and Dap).

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Design and syntheses of gramicidin S analogs, cyclo(-X-Leu-X-D-Phe-Pro-)2 (X=His, Lys, Orn, Dab and Dap).

机译：设计和合成短杆菌肽S类似物，cyclo（-X-Leu-X-D-Phe-Pro-）2（X = His，Lys，Orn，Dab和Dap）。

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The antibiotic activities and hemolytic activities of 1-5 and GS are summarized in Table 1. 1 with weak basic imidazole side chains showed very little activities against any bacteria or sheep blood cells. The results indicated that the presence of weak basic imidazole side chains is not effective for the interaction with both bacterial membrane and sheep cell membrane. On the other hand, 2-5 with basic amino side chains showed antibiotic activities. 2 with four e-amino side chains and 3 with four 8-amino side chains showed low antibiotic activities against Gram-positive microorganisms. 2 showed no activities against all Gram-negative bacteria tested. 3 showed the same activities to that of GS against Pseudomonas aeruginosa NBRC 3080, but no activity against Escherichia coli NBRC 12734.

机译：表1总结了1-5和GS的抗生素活性和溶血活性。1具有弱碱性咪唑侧链的化合物对任何细菌或绵羊血细胞的活性极低。结果表明，弱碱性咪唑侧链的存在对于与细菌膜和绵羊细胞膜的相互作用均无效。另一方面，具有碱性氨基侧链的2-5显示出抗生素活性。具有四个e-氨基侧链的2个和具有四个8个氨基侧链的3个对革兰氏阳性微生物的抗生素活性较低。 2显示没有针对所有测试的革兰氏阴性细菌的活性。图3显示了与GS相同的针对铜绿假单胞菌NBRC 3080的活性，但是没有针对大肠杆菌NBRC 12734的活性。

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《The Journal of Antibiotics: An International Journal》 |2011年第8期|共3页
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Tamaki M; Fujinuma K; Harada T; Takanashi K; Shindo M; Kimura M; Uchida Y;
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7. Design and syntheses of gramicidin S analogs, cyclo(-X-Leu-X-D-Phe-Pro-)2 (X=His, Lys, Orn, Dab and Dap) [O] . Makoto Tamaki, Kenta Fujinuma, Takuji Harada, 2011

机译：禾本科素类似物的设计和合成，Cyclo（-X-Leu-X-D-Phe-pro-）2（X =他，Lys，Orn，Dab和Dap）

Design and syntheses of gramicidin S analogs, cyclo(-X-Leu-X-D-Phe-Pro-)2 (X=His, Lys, Orn, Dab and Dap).

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