19099-93-5Relevant articles and documents
Chemo-Enzymatic Synthesis of Poly(4-piperidine lactone- b-ω-pentadecalactone) Block Copolymers as Biomaterials with Antibacterial Properties
Xiao, Yan,Pan, Jinghao,Wang, Dong,Heise, Andreas,Lang, Meidong
, p. 2673 - 2681 (2018)
With increasing troubles in bacterial contamination and antibiotic-resistance, new materials possessing both biocompatibility and antimicrobial efficacy are supposed to be developed for future biomedical application. Herein, we demonstrated a chemo-enzymatic ring opening polymerization (ROP) approach for block copolyester, that is, poly(4-benzyl formate piperidine lactone-b-ω-pentadecalactone) (PNPIL-b-PPDL), in a one-pot two-step process. Afterward, cationic poly(4-piperidine lactone-b-ω-pentadecalactone) (PPIL-b-PPDL) with pendent secondary amino groups was obtained via acidic hydrolysis of PNPIL-b-PPDL. The resulting cationic block copolyester exhibited high antibacterial activity against Gram negative E. coli and Gram positive S. aureus, while showed low toxicity toward NIH-3T3 cells. Moreover, the antibacterial property, cytotoxicity and degradation behavior could be tuned simply by variation of PPIL content. Therefore, we anticipate that such cationic block copolymers could potentially be applied as biomaterials for medicine or implants.
Unconventional Synthetic Process of Fasudil Hydrochloride: Costly Homopiperazine Was Avoided
Niu, Jinming,Wang, Dingding,Wu, Weiting,Yang, Wu-Lin,Zhao, Jianhong
, (2021/12/06)
An efficient, robust, and cost-effective synthetic process of fasudil hydrochloride 1 was developed. Starting from readily available ethylenediamine and 5-isoquinoline sulfonyl chloride, the target product 1 was prepared through a six-step reaction, including sulfonamidation, protection, nucleophilic substitution, deprotection, cyclization, and salification. The process afforded 1 in 67.1% overall yield (based on 5-isoquinoline sulfonyl chloride) with 99.94% purity. Compared to the earlier published methodologies, the use of homopiperazine or its derivatives as intermediates was avoided. The salient features of this environmentally friendly synthetic route include easily available starting materials and operational simplicity, which could be suitable for large-scale industrial production.
HPK1 ANTAGONISTS AND USES THEREOF
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Paragraph 0746; 0747, (2021/03/19)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.