- SUBSTITUTED BENZAMIDES AS MODULATORS OF TREX1
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Provided are compounds of Formula (I): (I) and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with TREX1.
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Paragraph 00104; 00106
(2021/12/08)
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- Cefiderocol (S-649266), A new siderophore cephalosporin exhibiting potent activities against Pseudomonas aeruginosa and other gram-negative pathogens including multi-drug resistant bacteria: Structure activity relationship
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The structure-activity relationship (SAR) for a novel series of catechol conjugated siderophore cephalosporins is described with their in vitro activities against multi-drug resistant Gram-negative pathogens including Pseudomonas aeruginosa, Acinetobacter baumannii, Stenotrophomonas maltophilia and Enterobacteriaceae. Cefiderocol (3) was one of the best molecules which displayed well-balanced and potent activities against multi-drug resistant Gram-negative pathogens including carbapenem resistant bacteria among the prepared compounds with the modified C-7 side chain and the modified C-3 side chain. Cefiderocol (3) is a highly promising parenteral cephalosporin for the treatment of multi-drug resistant Gram-negative infection.
- Aoki, Toshiaki,Yoshizawa, Hidenori,Yamawaki, Kenji,Yokoo, Katsuki,Sato, Jun,Hisakawa, Shinya,Hasegawa, Yasushi,Kusano, Hiroki,Sano, Masayuki,Sugimoto, Hideki,Nishitani, Yasuhiro,Sato, Takafumi,Tsuji, Masakatsu,Nakamura, Rio,Nishikawa, Toru,Yamano, Yoshinori
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p. 847 - 868
(2018/07/03)
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- Competition of substituents for ortho direction of metalation of veratric acid
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LTMP (5 equiv) metalates randomly veratric acid (1). Under external quench conditions, the thermodynamically more stable lithium 2-lithio-3,4-dimethoxybenzoate (2) reacts with a variety of electrophiles to give versatile building units that are not easily accessible by conventional means. Under in situ quench conditions (LTMP/TMSCl), a reversal of regioselectivity is observed and 6-trimethylsilyl-3,4-dimethoxybenzoic acid (10) is formed predominantly.
- Chau, Nguyet Trang Thanh,Nguyen, Thi Huu,Castanet, Anne-Sophie,Nguyen, Kim Phi Phung,Mortier, Jacques
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p. 10552 - 10557
(2008/12/23)
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- Synthesis of N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidinium acetate [α-14C]
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14C-Labelled N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidinium acetate has been synthesized as a part of a four-step procedure which involved decarboxylation of 2-chloro-3,4-dimethoxybenzoic acid by Pb(OAc)4 to give 2-chloro-3,4-dimethoxy-1-iodobenzene, followed by a selective lithiation at the iodine position and electrophilic substitution with N,N-dimethylformamide [α-14C] and final reaction with aminoguanidine bicarbonate. The specific activity was 59 mCi/mmol and the overall yield 49%. Copyright
- Almeida, Maria,Boman, Arne,Lundstedt, Torbjrn
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p. 371 - 377
(2007/10/03)
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