350474-66-7Relevant articles and documents
Catalyst- and acid-free Markovnikov hydration of alkynes in a sustainable H2O/ethyl lactate system
Dandia, Anshu,Saini, Pratibha,Chithra,Vennapusa, Sivaranjana Reddy,Parewa, Vijay
, (2021/03/15)
An efficient and sustainable protocol for the hydration of alkynes has been developed under metal/acid/catalyst/ligand-free conditions in a water/ethyl lactate mixture. The hydrogen-bond network in the ethyl lactate and water mixture plays a crucial and decisive role in activating the alkynes for hydration to afford the corresponding methyl ketones. This strategy gives the Markovnikov (ketone) addition product selectively over other possible products. The essential role of hydrogen bonding has been confirmed by experimental and theoretical techniques. A probable mechanism has been suggested by various control tests. The efficacy of the method has been further explored for the competent production of value-added α,β-unsaturated carbonyl compounds through the reaction of aldehydes with alkynes as ketonic surrogates. The environmentally benign hydration method takes place under mild conditions, has broad functional-group compatibility, and uses the ethyl lactate/water (1:3) medium as a “green alternative” in the absence of any hazardous, harmful, or expensive substances.
Synthesis and Antiproliferative Activity of Novel Hydrazono Thiazolidene and Thiazole Derivatives Bearing Rhodanine Moiety
Amr, A. E.,Azab, M. E.,Elasasy, M. E. A.,Elnaggar, D. H.,Hafez, N. A. Abdel,Mohamed, A. M.,Omran, M. M.
, p. 915 - 925 (2021/06/26)
Abstract: Some new fluoro-heterocyclic compounds containing thiazole and pyridine moities have been synthesized and studied for their antiproliferative activity. Thiazole derivatives have been synthesized by the reaction of alpha-halo carbonyl compounds with thiosemicarbazones. Some pyridine derivatives have been synthesized by the reaction of chalcone with cyanothioacetamide and/or malononitrile. Spectroscopic methods have been used for elucidating molecular structures of the products. Cytotoxic activity of several derivatives has been tested against human breast cancer (MCF-7), human colon cancer (HCT-116) and human liver cancer (Hep-G2) by the SRB method. Most of compounds exhibit mild effect on the tested cell lines. One of thiazolidin-4-one derivatives has been characterized by moderate to strong effect on MCF-7 cell line.
Design, synthesis, and SAR study of novel 4,5-dihydropyrazole-Thiazole derivatives with anti-inflammatory activities for the treatment of sepsis
Cao, Peichang,Duan, Yajun,Fang, Mengyuan,Han, Jihong,Li, Qing-Shan,Xu, Huajian,Yang, Xiaoxiao,Zhang, Zhen,Zou, Tingfeng
, (2021/08/17)
Systemic inflammatory response syndrome is a major feature of sepsis which is one of the major causes of death worldwide. It has been reported that 3,5-diaryl-4,5-dihydropyrazole and thiazole derivatives have many biological functions, especially in the aspect of anti-inflammation. According to the strategy of pharmacophore combination, we introduced thiazole moiety into dihydropyrazole skeleton to design and synthesize a novel series of 2-(3,5-diphenyl-4,5-dihydro-1H-pyrazol-1-yl)-4-methylthiazole derivatives, and evaluated their anti-inflammatory activities for sepsis treatment. Preliminary structure?activity relationship (SAR) analysis was conducted by their inhibitory activities against nitric oxide (NO) release in LPS-induced RAW264.7 cells, and the optimal compound E26 exhibited more potent anti-inflammatory activity than the positive control treatment indomethacin and dexamethasone. In further mechanism study, our results showed that compound E26 significantly suppressed the production of interleukin-1β (IL-1β), tumor necrosis factor-α (TNF-α), NO and inhibited the expressions of inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2) through blocking MAPKs signaling pathway. In addition, in vivo administration of compound E26 resulted in a significant improvement of LPS-induced sepsis in C57BL/6J mice, with reducing toxicity in multiple organs. Taken together, this study demonstrated the compound E26 could be a promising agent for the treatment of sepsis.