197143-33-2Relevant articles and documents
Preparation and application of imidazo aromatic ring compounds
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Paragraph 0188-0192, (2020/05/02)
The invention provides preparation and application of imidazo aromatic ring compounds, and particularly provides compounds as shown in the following formula I. The definition of each group is as shownin the specification. The compounds have TRK kinase inh
Synthesis and biological activity of novel 1β-Methylcarbapenems with oxyiminopyrrolidinylamide moiety
Lee, Ji Hoon,Lee, Kyung Seok,Kang, Yong Koo,Yoo, Kyung Ho,Shin, Kye Jung,Kim, Dong Chan,Kong, Jae Yang,Lee, Yeonhee,Lee, Sook Ja,Kim, Dong Jin
, p. 4399 - 4403 (2007/10/03)
The synthesis and antibacterial activity of novel 1β- methylcarbapenems 1a-f bearing oxyiminopyrrolidinylamide moiety at C-5 position of pyrrolidine are described. Most compounds exhibited comparable antibacterial activity to meropenem against a wide range of Gram-positive and Gram-negative organisms including Pseudomonas aeruginosa isolates. Of these carbapenems, 1a showed potent and broad spectrum of antibacterial activity and similar stability to DHP-I to meropenem. Against clinical isolates of 40 Gram-negative bacterial species including MDR and ESBL-producing strains, the selected carbapenem 1a possessed excellent in vitro activity except for MDR P. aeruginosa, and was comparable in potency to meropenem.
Novel fluoroquinolone antibacterial agents containing oxime-substituted (Aminomethyl)pyrrolidines: Synthesis and antibacterial activity of 7-(4- (Aminomethyl)-3-(methoxyimino) pyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4- oxo-1,4-dihydro[1,8]naphthyridine-3-carboxylic acid (LB20304)
Hong, Chang Yong,Kim, Young Kwan,Chang, Jay Hyok,Kim, Se Ho,Choi, Hoon,Nam, Do Hyun,Kim, Yong Zu,Kwak, Jin Hwan
, p. 3584 - 3593 (2007/10/03)
New pyrrolidine derivatives, which bear an alkyloxime substituent in the 4-position and an aminomethyl substituent in the 3-position of the pyrrolidine ring, have been synthesized and coupled with various quinolinecarboxylic acids to produce a series of new fluoroquinolone antibacterials. These fluoroquinolones were found to possess potent antimicrobial activity against both Gram-negative and Gram-positive organisms, including methicillin resistant Staphylococcus aureus (MRSA). Variations at the C-8 position of the quinolone nucleus included fluorine, chlorine, nitrogen, methoxy, and hydrogen atom substitution. The activity imparted to the substituted quinolone nucleus by the C-8 substituent was in the order F (C5-NH2) > F (C5-H) > naphthyridine > Cl = OMe = H against Gram-positive organisms. In the case of Gram-negative strains, activity was in the order F (C5-NH2) > naphthyridine = F (C5-H) > H > Cl > OMe. The advantages provided by the newly introduced oxime group of the quinolones were clearly demonstrated by their comparison to a desoximino compound 30. In addition, the oxime moiety greatly improved the pharmacokinetic parameters of the novel quinolones. Among these compounds, compound 20 (LB20304) showed the best in vive efficacy and pharmacokinetic profile in animals, as well as good physical properties. The MICs (μg/mL) of LB20304, compound 30, and ciprofloxacin against several test organisms are as follows: S. aureus 6538p (0.008, 0.031, and 0.13), methicillin resistant S. aureus 241 (4, 16, and 128), Streptococcus epidermidis 887E (0.008, 0.016, and 0.13), methicillin resistant S. epidermidis 178 (4, 32, and 128), Enterococcus faecalis 29212 (0.063, 0.13, and 1), Pseudomonas aeruginosa 1912E (0.25, 0.5, and 0.13), Escherichia coli 3190Y (0.008, 0.016, and 0.008), Enterobacter cloacae P99 (0.008, 0.031, and 0.008), Actinobacter calcoaceticus 15473 (0.063, 0.13, and 0.25). On the basis of these promising results, LB20304 was selected as a candidate for further evaluation.
