13751-83-2Relevant academic research and scientific papers
CYCLIC PEPTIDE ANTIBIOTICS
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Paragraph 00275, (2019/04/11)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of lipoprotein signal peptidase II (LspA), a key protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.
2-Amino-5,6-difluorophenyl-1 H-pyrazole-Directed PdII Catalysis: Arylation of Unactivated β-C(sp3)-H Bonds
Yang, Jinyue,Fu, Xiaopan,Tang, Shibiao,Deng, Kezuan,Zhang, Lili,Yang, Xianjin,Ji, Yafei
, p. 10221 - 10236 (2019/08/20)
Palladium-catalyzed arylation of unactivated β-C(sp3)-H bonds in carboxylic acid derivatives with aryl iodides is described for the first time using 2-amino-5,6-difluorophenyl-1H-pyrazole as an efficient and readily removable directing group. Two fluoro groups are installed at the 5- and 6-position of the anilino moiety in 2-aminophenyl-1H-pyrazole, clearly enhancing the directing ability of the auxiliary. In addition, the protocol employs Cu(OAc)2/Ag3PO4 (1.2/0.3) as additives, evidently reducing the stoichiometric amount of expensive silver salts. Furthermore, this process exhibits high β-site selectivity, compatibility with diverse substrates containing α-hydrogen atoms, and excellent functional group tolerance.
A C-H Insertion Approach to Functionalized Cyclopentenones
Wang, Youliang,Zarca, Maxence,Gong, Liu-Zhu,Zhang, Liming
supporting information, p. 7516 - 7519 (2016/07/06)
Cyclopentenones are synthetically versatile structures, and their straightforward construction from alkynone substrates by employing synthetically streamlining C-H insertion is conceptually appealing and of high synthetic potential. But, its implementation is very limited. Herein we report a Au-catalyzed version, which affords 2-bromocyclopent-2-en-1-ones with a broad scope and synthetically desirable diastereoselectivities. The proposed key intermediate capable of the observed insertion into unactivated C-H bonds is a fully functionalized gold vinylidene, which is generated via a novel intermolecular strategy. This flexible access of likely gold vinylidenes opens various opportunities to explore their versatile reactivities.
Design, synthesis and biological evaluation of novel isoniazid derivatives with potent antitubercular activity
Martins, Filomena,Santos, Susana,Ventura, Cristina,Elvas-Leit?o, Ruben,Santos, Lídia,Vitorino, Susana,Reis, Marina,Miranda, Vanessa,Correia, Henrique F.,Aires-De-Sousa, Jo?o,Kovalishyn, Vasyl,Latino, Diogo A.R.S.,Ramos, Jorge,Viveiros, Miguel
, p. 119 - 138 (2014/06/09)
The disturbing emergence of multidrug-resistant strains of Mycobacterium tuberculosis (Mtb) has been driving the scientific community to urgently search for new and efficient antitubercular drugs. Despite the various drugs currently under evaluation, ison
Methylation-dependent acyl transfer between polyketide synthase and nonribosomal peptide synthetase modules in fungal natural product biosynthesis
Zou, Yi,Xu, Wei,Tsunematsu, Yuta,Tang, Mancheng,Watanabe, Kenji,Tang, Yi
supporting information, p. 6390 - 6393 (2015/02/19)
Biochemical studies of purified and dissected fungal polyketide synthase and nonribosomal peptide synthetase (PKS-NRPS) hybrid enzymes involved in biosynthesis of pseurotin and aspyridone indicate that one α-methylation step during polyketide synthesis is a prerequisite and a key checkpoint for chain transfer between PKS and NRPS modules. In the absence of the resulting γ-methyl feature, the completed polyketide intermediate is offloaded as an α-pyrone instead of being aminoacylated by the NRPS domain. These examples illustrate that precisely timed tailoring domain activities play critical roles in the overall programming of the iterative PKS (and NRPS) functions.
Peptide immunostimulants
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, (2008/06/13)
Peptide compounds of formula 1, pharmaceutically acceptable base salts thereof, pharmaceutical compositions and their use as antiinfective agents where R1 is alkyl, cycloalkyl or cycloalkylmethyl; R2 is hydrogen or alkyl and R3 is hydroxy or an amino acid residue of the formula where X is hydrogen, alkyl or hydroxymethyl and nis an integer of 0 to 4 and R4 and R5 are alkyl, hydrogen, benzyl or cyclohexylmethyl.
