62507-78-2Relevant academic research and scientific papers
Solid-phase synthesis of coralmycin A/epi-coralmycin A and desmethoxycoralmycin A
Hawkins, Paige M. E.,Liu, Dennis Y.,Linington, Roger G.,Payne, Richard J.
supporting information, p. 6291 - 6300 (2021/07/28)
The total synthesis of the natural product coralmycin A/epi-coralmycin A, as well as a desmethoxy analogue is described. Synthesis was achievedviaa divergent, bidirectional solid-phase strategy, including a key on-resinO-acylation,OtoNacyl shift, andO-alkylation protocol to incorporate the unusual 4-amino-2-hydroxy-3-isopropoxybenzoic acid motifs. The synthetic natural product was generated as a 1?:?1 mixture of epimers at the central β-methoxyasparagine residue and exhibited potent antibacterial activity against a panel of ten Gram-negative and seven Gram-positive organisms. The desmethoxy analogue possessed significantly more potent antimicrobial activity against this panel with minimal inhibitory concentrations (MICs) as low as 50 nM.
METHOD FOR PREPARING COAGULATION FACTOR XIA INHIBITOR AND INTERMEDIATE THEREOF
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Paragraph 0114-0117, (2021/09/26)
The present disclosure involves a method for preparing a coagulation factor XIa inhibitor and an intermediate thereof. Specifically, the present disclosure involves a method for preparing an oxypyridine amide derivative. The method has the advantages of high yield, good product purity, and mild reaction conditions.
Copper nanoparticles (CuNPs) catalyzed chemoselective reduction of nitroarenes in aqueous medium
Chand, Dillip Kumar,Rai, Randhir
, (2021/08/20)
Abstract: A procedure for practical synthesis of CuNPs from CuSO4·5H2O is established, under appropriate reaction conditions, using rice (Oryza sativa) as an economic source of reducing as well as a stabilizing agent. Optical and microscopic techniques are employed for the characterization of the synthesized CuNPs and the sizes of the particles were found to be in the range of 8 ± 2 nm. The nanoparticles are used as a catalyst for chemoselective reduction of aromatic nitro compounds to corresponding amines under ambient conditions and water as a reaction medium. Graphic abstract: CuNPs are synthesized using hydrolysed rice and used as catalyst for chemoselective reduction of nitroarenes to their corresponding amines in water. [Figure not available: see fulltext.]
Metagenome-Guided Analogue Synthesis Yields Improved Gram-Negative-Active Albicidin- and Cystobactamid-Type Antibiotics
Brady, Sean F.,Freundlich, Joel S.,Kasper, Amanda,Li, Shaogang,Mehmood, Rabia,Ternei, Melinda,Wang, Zongqiang
supporting information, p. 22172 - 22177 (2021/09/09)
Natural products are a major source of new antibiotics. Here we utilize biosynthetic instructions contained within metagenome-derived congener biosynthetic gene clusters (BGCs) to guide the synthesis of improved antibiotic analogues. Albicidin and cystoba
NOVEL CYSTOBACTAMIDE DERIVATIVES
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Page/Page column 43; 47, (2019/03/12)
The present invention relates to novel derivatives of cystobactamides of formula (lb) and the use thereof for the treatment or prophylaxis of bacterial infections.
Discovery and Total Synthesis of Natural Cystobactamid Derivatives with Superior Activity against Gram-Negative Pathogens
Hüttel, Stephan,Testolin, Giambattista,Herrmann, Jennifer,Planke, Therese,Gille, Franziska,Moreno, Maria,Stadler, Marc,Br?nstrup, Mark,Kirschning, Andreas,Müller, Rolf
supporting information, p. 12760 - 12764 (2017/09/06)
Antibiotic discovery and development is challenging as chemical scaffolds of synthetic origin often lack the required pharmaceutical properties, and the discovery of novel ones from natural sources is tedious. Herein, we report the discovery of new cystob
2,2-Bis(ethoxycarbonyl)vinyl (BECV) as a versatile amine protecting group for selective functional-group transformations
Ilangovan, Andivelu,Kumar, Rajendran Ganesh
supporting information; experimental part, p. 2938 - 2943 (2010/07/02)
A 2,2-Bis(ethoxycarbonyl) vinyl- (BECV) group was used for the selective protection of amines at room temperature in the presence of potentially interfering functional groups such as OH, SH, COOH as well as other NH 2 groups. Several functional group transformations such as esterification, O-alkylation, O-acylation, N-alkylation, N-acylation, S-alkylation can selectively be carried out in the presence of the BECV group. The selective deprotection of the BECV group was achieved in a short time using ethylenediamine at room temperature while several other functional groups such as benzoate, aliphatic esters, amides and ethers remain intact. The BECV group shows orthogonal stability against the common protecting groups such as Fmoc, Cbz and Boc.
N→S acyl-transfer-mediated synthesis of peptide thioesters using anilide derivatives
Tsuda, Shugo,Shigenaga, Akira,Bando, Kiyomi,Otaka, Akira
scheme or table, p. 823 - 826 (2009/09/06)
N→S acyl-transfer-mediated synthesis of peptide thioesters utilizing an N-aminoacyl-N-sulfanylethylaminobenzoic acid derivative has been examined. The developed synthetic methodology for peptide thioesters is compatible with Fmoc solid-phase peptide synth
Design and synthesis of phosphotyrosine peptidomimetic prodrugs
Garrido-Hernandez, Hugo,Moon, Kyung D.,Geahlen, Robert L.,Borch, Richard F.
, p. 3368 - 3376 (2007/10/03)
A novel approach to the intracellular delivery of aryl phosphates has been developed that utilizes a phosphoramidate-based prodrug approach. The prodrugs contain an ester group that undergoes reductive activation intracellularly with concomitant expulsion
Di(aromatic) compounds and their use in human and veterinary medicine and in cosmetics
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, (2008/06/13)
Di(aromatic) compounds corresponding to the following formula: STR1 in which: Ar represents either STR2 n=1 or 2 or: STR3 X represents a divalent radical, Z represents O, S or a divalent radical, and R1, R2, R3, R4 and R5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R1 is a carboxylic acid function. Use in human and veterinary medicine and in cosmetics.
