- BENZENE DERIVATIVES,PROCESS FOR PREPARING THE SAME AND USE THEREOF
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Novel benzene derivatives represented by the formula (I) : wherein R1, R4 and R6 each independently represents a hydrogen atom, a halogen atom or a hydrocarbon group, R2 represents a hydrocarbon group or a heterocyclic group, R3 represents a hydrocarbon group, NR7'R7 or OR8 (wherein R7' represents a hydrogen atom or a hydrocarbon group, R7 represents a non-aromatic group, or R7' and R7 may form a ring with the adjacent nitrogen atom, and R8 represents a hydrocarbon group or a heterocyclic group), R5 represents a hydrocarbon group or a heterocyclic group (except for a quinolyl group), R5' represents a hydrogen atom, or a hydrocarbon group, or R5 and R5' may form a ring with the adjacent nitrogen atom, and R5" represents a hydrogen atom or a hydrocarbon group, which have vanilloid receptor agonist activity and are useful as a drug such as an analgesic and an agent for preventing and/or treating urinary frequency and/or urinary incontinence.
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- Vanilloid and isovanilloid analogues as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases
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As aminoacyl adenylate surrogates, a series of methionyl and isoleucyl phenolic analogues containing bioisosteric linkers mimicking ribose have been investigated. Inhibition of synthesized compounds to the aminoacylation reaction by the corresponding Escherichia coli methionyl-tRNA and isoleucyl-tRNA synthetases indicated that 18 was found to be a potent inhibitor of isoleucyl-tRNA synthetase. A molecular modeling study demonstrated that in 18, isovanillate and hydroxamate served as proper surrogates for adenine and ribose in isoleucyl adenylate, respectively.
- Lee, Jeewoo,Kang, Sang Uk,Kim, Su Yeon,Kim, Sung Eun,Jo, Yeong Joon,Kim, Sunghoon
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p. 965 - 968
(2007/10/03)
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- Absolute Stereochemistry of Aplaminone and Neoaplaminone, Cytotoxic Bromodopamines from a Marine Mollusc: Enantioselective Synthesis of Debromoneoaplaminone
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The absolute stereochemistry of potent cytotoxic bromodopamines, aplaminone and neoaplaminone has been determined by means of enantioselective synthesis of debromoneoaplaminone, a derivative of aplaminone and neoaplaminone.
- Kigoshi, Hideo,Adachi, Yuichi,Yoshikawa, Kohji,Yamada, Kiyoyuki
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p. 4195 - 4198
(2007/10/02)
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