5024-66-8Relevant academic research and scientific papers
Systematic evaluation of structure-activity relationships of the riminophenazine class and discovery of a C2 pyridylamino series for the treatment of multidrug-resistant tuberculosis
Liu, Binna,Liu, Kai,Lu, Yu,Zhang, Dongfeng,Yang, Tianming,Li, Xuan,Ma, Chen,Zheng, Meiqin,Wang, Bin,Zhang, Gang,Wang, Fei,Ma, Zhenkun,Li, Chun,Huang, Haihong,Yin, Dali
, p. 4545 - 4559 (2012)
Clofazimine, a member of the riminophenazine class of drugs, is the cornerstone agent for the treatment of leprosy. This agent is currently being studied in clinical trials for the treatment of multidrug-resistant tuberculosis to address the urgent need for new drugs that can overcome existing and emerging drug resistance. However, the use of clofazimine in tuberculosis treatment is hampered by its high lipophilicity and skin pigmentation side effects. To identify a new generation of riminophenazines that is less lipophilic and skin staining, while maintaining efficacy, we have performed a systematic structure-activity relationship (SAR) investigation by synthesizing a variety of analogs of clofazimine and evaluating their anti-tuberculosis activity. The study reveals that the central tricyclic phenazine system and the pendant aromatic rings are important for anti-tuberculosis activity. However, the phenyl groups attached to the C2 and N5 position of clofazimine can be replaced by a pyridyl group to provide analogs with improved physicochemical properties and pharmacokinetic characteristics. Replacement of the phenyl group attached to the C2 position by a pyridyl group has led to a promising new series of compounds with improved physicochemical properties, improved anti-tuberculosis potency, and reduced pigmentation potential.
pyrimidine derivatives substituted with aryl- or heteroaryl- substituted fluorene group, and organic electroluminescent device including the same
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, (2017/10/28)
Aryl group or a heteroaryl group substituted pyrimidine derivatives of formula 1 is coupled to polyarylenic backbone containing encoded ball number. [Formula 1] [In said formula 1, Ar1 And Ar2 Are each independently a hydrogen, methyl or phenyl, The C L6 - C24 C aryl of reflector3 - C24 It will be biting and heteroatoms, N is an integer 0 or 1 and, Ar3 The C6 - C30 C aryl of reflector3 - C30 A variety of printers] (by machine translation)
Fused phenanthridine derivatives substituted with aryl or heteroaryl, and organic electroluminescent device including the same
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, (2018/03/28)
Aryl group or a heteroaryl group substituted [...] phenanthridine derivatives of formula 1 to ball number encoded. [Formula 1] [In said formula 1, Ar1 Is phenyl or pyridyl [...], Z1 And the O or S, L is a phenyl or pyridyl [...], Ar2 To is selected from the group represented by either formula 3] [Formula 3] , , , , (by machine translation)
ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE
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Page/Page column 123, (2008/12/06)
The present invention is directed to aryl sulfamide derivatives of formula (I): or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.
Synthesis and Characterization of Water-Soluble and Photolabile 10-Arylisoalloxazines: Tools for Studying the Mechanism of Action of Flavin-Type Antimalarials
Kirsch, Peer,Schoenleben-Janas, Annette,Schirmer, R. Heiner
, p. 1275 - 1282 (2007/10/02)
Isoalloxazine derivatives such as 1a-d are promising antimalarial agents which act as inhibitors of the antioxidant enzyme glutathione reductase and possibly of other proteins.The molecular mechanism of the pharmacological effects has not been studied in detail because compounds 1a-d are poorly soluble in aqueous solutions of physiological pH.In the present study we introduce two new types of isoalloxazine derivatives with improved solubility properties.The 10-aryl-3-carboxymethylisoalloxazines 2a-d, and the isomeric 3-methyl-10-(N-methylpyridiniumyl)isoalloxazine salts 3 and 4.In addition, for the purpose of photoaffinity labeling experiments, the 10-aryl-8-azido-3-methylisoalloxazine 5 was designed.The syntheses and characterizations of these new flavins as well as an alternative synthetic approach to the known antimalarials 1a-d are described. - Keywords: Flavins/Isoalloxazines/Arylisoalloxazines/Malaria/Antimalarials/Glutathione reductase inhibitors/Photoaffinity labels
