| Budget Amount *help |
¥26,260,000 (Direct Cost: ¥20,200,000、Indirect Cost: ¥6,060,000)
Fiscal Year 2012: ¥5,590,000 (Direct Cost: ¥4,300,000、Indirect Cost: ¥1,290,000)
Fiscal Year 2011: ¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2010: ¥15,730,000 (Direct Cost: ¥12,100,000、Indirect Cost: ¥3,630,000)
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| Research Abstract |
The caprazamycins (CPZs), muraymycins (MRYs), and mureidomycins (MRDs) which constitute a class of nucleoside natural products, exhibit excellent antimicrobial activity against. This work presents a total synthesis, systematic structure-activity relation-ship (SAR) study, and simplification of CPZs, MRYs, and MRDs. The analogues exhibited good activity against a range of Gram-positive bacterial pathogens, including MRSA and VRE. The oxazolidine analogues were developed through simplification of CPZs, and they exhibited antibacterial activity with a similar potency to the CPZs. Our SAR study of the CPZs and MRYs suggests a probable mechanism for inhibition of the MraY.
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