55417-80-6Relevant academic research and scientific papers
POTASSIUM CHANNEL MODULATORS
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Paragraph 0398; 0402; 0405; 0407, (2018/01/14)
Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with potassium channels. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with potassium channels.
A Mitochondria-Targeted Photosensitizer Showing Improved Photodynamic Therapy Effects Under Hypoxia
Lv, Wen,Zhang, Zhang,Zhang, Kenneth Yin,Yang, Huiran,Liu, Shujuan,Xu, Aqiang,Guo, Song,Zhao, Qiang,Huang, Wei
, p. 9947 - 9951 (2016/08/16)
Organelle-targeted photosensitizers have been reported to be effective photodynamic therapy (PDT) agents. In this work, we designed and synthesized two iridium(III) complexes that specifically stain the mitochondria and lysosomes of living cells, respectively. Both complexes exhibited long-lived phosphorescence, which is sensitive to oxygen quenching. The photocytotoxicity of the complexes was evaluated under normoxic and hypoxic conditions. The results showed that HeLa cells treated with the mitochondria-targeted complex maintained a slower respiration rate, leading to a higher intracellular oxygen level under hypoxia. As a result, this complex exhibited an improved PDT effect compared to the lysosome-targeted complex, especially under hypoxia conditions, suggestive of a higher practicable potential of mitochondria-targeted PDT agents in cancer therapy.
Preparation method and application of phosphorescence iridium complexes with mitochondrial targeting function
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, (2017/02/23)
The invention discloses phosphorescence iridium complexes with a mitochondrial targeting function, and a preparation method thereof, and an application thereof in biological imaging and oxygen detection. The complexes are composed of a cyclic metal ligand, a metal center and an auxiliary ligand containing a mitochondrial targeting function group, and the structure of the complexes is represented by a general formula shown in the description; the luminous intensity and the emission life of the complexes reduce with the increase of the oxygen concentration; mitochondria of living cells are marked; the change of the concentration of oxygen in the mitochondria of living cells is detected through a confocal imaging and life imaging technology; and the phosphorescence iridium complexes have important application prospect in biological imaging and sensing fields.
The phosphorescence of the response characteristic of a complex, and its preparation method and application
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, (2017/04/29)
The invention relates to a phosphorescent iridium complex with stimuli responsibility. The phosphorescent iridium complex is composed of a cyclometalated ligand, a metal center and an assistant ligand containing an active function group, and has the structure general formula shown in the specification. The compound disclosed by the invention is capable of causing variation of phosphorescence emission wavelength under stimulation of an acidic or basic reagent; also under electricity stimulation, the compound is capable of causing variation of emission wavelength and also is capable of causing variation of emission lifetime; and based on the electricity stimulation response characteristics and by means of time resolution technology, the phosphorescent iridium complex is applicable to construct memory devices for information recording, encryption and decryption. The phosphorescent iridium complex disclosed by the invention has important application prospect on aspects of information recording, information encryption and the like.
A convenient synthesis of pyrimidinone and pyrimidine containing bisheteroarenes and analogs
Maurya, Hardesh K.,Gupta, Atul
, p. 22106 - 22114 (2014/06/23)
The synthesis of pyrimidinone containing bisheteroarenes (3) and related analogs (9 and 10) by the reaction of active methylenes or substituted methyl acrylate with nitrogen containing precursors viz. amidines, or thiourea in water as well as other organic solvents was studied. Synthesized compounds have further been explored for the synthesis of diversified pyrimidines 4, 6-8, 11, 12 and 14 through a sequential approach. This journal is the Partner Organisations 2014.
Pyridinylpyrimidines selectively inhibit human methionine aminopeptidase-1
Zhang, Pengtao,Yang, Xinye,Zhang, Feiran,Gabelli, Sandra B.,Wang, Renxiao,Zhang, Yihua,Bhat, Shridhar,Chen, Xiaochun,Furlani, Manuel,Amzel, L. Mario,Liu, Jun O.,Ma, Dawei
, p. 2600 - 2617 (2013/06/27)
Cellular protein synthesis is initiated with methionine in eukaryotes with few exceptions. Methionine aminopeptidases (MetAPs) which catalyze the process of N-terminal methionine excision are essential for all organisms. In mammals, type 2 MetAP (MetAP2)
4-Amino-2-(pyridin-2-yl)pyrimidine as microbicidal active substances
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Page 14, (2010/11/29)
There are described compounds of formula whereinR1 and R2 are each independently of the other hydrogen; unsubstituted or mono- or polyhalo-substituted C1-C20alkyl, C1-C20alkoxy, C2-C20alkenyl, C2-C20alkynyl, C3-C18cycloalkyl, C3-C7cycloalkyl-C1-C20alkyl; hydroxy; C1-C6alkoxy-C1-C20alkyl; carboxy; C1-C6alkyloxycarbonyl; cyano; mono- or di-C1-C20alkylamino; C1-C6alkylamino-C1-C20alkyl; halogen; phenyl; unsubstituted or C1-C5alkyl-, halo- or hydroxy-substituted phenyl-C1-C20alkyl, phenoxy or phenyl-C1-C20alkoxy; or R1 and R2 form a polymethylene chain of formula -(CH2)m- wherein m = 2-12;R3 is unsubstituted C7-C20alkyl; or amino-, hydroxy-, carboxy- or C1-C6alkyloxycarbonyl-substituted C2-C20alkyl; C8-C18cycloalkyl; C8-C20alkenyl; C8-C20alkynyl; C3-C7cycloalkyl-C8-C20alkyl; C1-C4alkoxy-C8-C20alkyl; R7R8N-C7-C20alkyl; phenyl; phenyl-C1-C4alkyl; or phenyl-C1-C4alkoxy;R4 is hydrogen; unsubstituted or C1-C5alkyl-, halo- or hydroxy-substituted C1-C20alkyl, C2-C20alkenyl, C2-C20alkynyl, C3-C20cycloalkyl, C3-C7cycloalkyl-C1-C20alkyl, C1-C20alkoxy-C1-C6alkyl or R7R8N-C1-C20alkyl, phenyl, phenyl-C1-C20alkyl or phenoxy-C1-C20alkyl;R5 and R6 are each independently of the other hydrogen; C1-C20alkyl; C2-C20alkenyl; C2-C20-alkynyl; C3-C18cycloalkyl; C3-C7cycloalkyl-C1-C20alkyl; hydroxy; C2-C20alkoxy; C1-C6alkoxy-C1-C20alkyl; carboxy; C1-C6alkyloxycarbonyl; cyano; nitro; C1-C20alkylamino; C1-C20alkylaminoalkyl; C1-C20haloalkyl; C1-C20haloalkoxy; halogen; unsubstituted or C1-C5alkyl-, halo- or hydroxy-substituted phenyl, phenoxy or phenyl-C1-C20alkyl or phenyl-C1-C20alkoxy; or R5 and R6 together form a polymethylene chain of formula -(CH2)m- wherein m = 2-12; andR7 and R8 are each independently of the other hydrogen; C1-C20alkyl; C3-C20alkenyl; C3-C20-alkynyl; C3-C7cycloalkyl; C3-C20cycloalkyl-C1-C4alkyl; phenyl; or phenyl-C1-C4alkyl. They are suitable for the antimicrobial treatment of surfaces, as antimicrobial active substances against gram-positive and gram-negative bacteria.
1,3-Oxazines and Related Compounds. VI. Synthesis and Some Reactions of 2,6-Disubstituted 4H-1,3-Thiazin-4-ones
Yamamoto, Yutaka,Ohnishi, Shuhei,Azuma, Yutaka
, p. 1929 - 1935 (2007/10/02)
Various of 2,6-disubstituted 4H-1,3-thizin-4-ones (5) were synthesized by successive treatment of N-acylacetylcarboxamides with acid (such as 70percent perchloric acid or fluorosulfonic acid) and hydrogen sulfide.Reactions of 5 were investigated; ammonolysis with ethanolic ammonia gave the corresponding pyrimidin-4-ones; hydrolysis of 2-alkyl-1,3-thiazine derivatives yielded ring-opend N-acyl-β-mercaptocrotonamides; reduction with NaBH4 or LiALH4 afforded 3,4-dihydro-2H-1,3-thiazin-4-one derivatives.Keywords - 1,3-thiazin-4-one; 3,4-dihydro-2H-1,3-thiazin-4-one; pyrimidin-4-one; 1,3-oxazinium salt; 1,3-thiazinium salt; N-acylacetylcarboxamide; N-acyl-β-mercaptocrotonamide
Unfused Heterobicycles as Amplifiers of Phleomycin.I Some Pyridinyl- and Pyrazolyl-pyrimidines, Bithiazoles and Thiazolylpyridines
Brown, Desmond J.,Cowden, William B.,Grigg, Geoffrey W.,Kavulak, Diana
, p. 2291 - 2298 (2007/10/02)
Syntheses are reported for some simple derivatives of 2-(pyridin-2'-yl)pyrimidine; 4-(pyrazol-1'-yl)pyrimidine; 4-(pyrazol-4'-yl)pyrimidine; 4,5'-bithiazole; 2-, 3-, and 4-(thiazol-4'-yl)pyridine and 2-, 3-, and 4-(thiazol-2'-yl)pyridine.Biological activities, as amplifiers of phleomycin against in vitro cultures of Escherichia coli, are tabulated and discussed.
