199601-80-4Relevant articles and documents
Design and synthesis of novel 5-arylisoxazole-1,3,4-thiadiazole hybrids as α-glucosidase inhibitors
Saeedi, Mina,Eslami, Azadeh,Mirfazli, Seyedeh Sara,Zardkanlou, Mahsa,Faramarzi, Mohammad Ali,Mahdavi, Mohammad,Akbarzadeh, Tahmineh
, p. 436 - 444 (2021/10/04)
Background: α-Glucosidase inhibitors have occupied a significant position in the treatment of type 2 diabetes. In this respect, the development of novel and efficient non-sugar-based inhibitors is in high demand. Objective: Design and synthesis of new 5-arylisoxazole-1,3,4-thiadiazole hybrids possessing α-glucosidase inhibitory activity were developed. Methods: Different derivatives were synthesized by the reaction of various 5-arylisoxazole-3-carboxylic acids and ethyl 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)acetate. Finally, they were evalu-ated for their α-glucosidase inhibitory activity. Results: It was found that ethyl 2-((5-(5-(2-chlorophenyl)isoxazole-3-carboxamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5j) was the most potent compound (IC50 = 180.1 μM) compared with acarbose as the reference drug (IC50 = 750.0 μM). Also, the kinetic study of 5j revealed a competitive inhibition and docking study results indicated desired interactions of that compound with amino acid residues located close to the active site of α-glucosidase. Conclusion: Good α-glucosidase inhibitory activity obtained by the title compounds introduced them as an efficient scaffold, which merits to be considered in anti-diabetic drug discovery developments.
Design and Synthesis of Selective Acetylcholinesterase Inhibitors: Arylisoxazole-Phenylpiperazine Derivatives
Saeedi, Mina,Mohtadi-Haghighi, Dorrin,Mirfazli, Seyedeh Sara,Mahdavi, Mohammad,Hariri, Roshanak,Lotfian, Hania,Edraki, Najmeh,Iraji, Aida,Firuzi, Omidreza,Akbarzadeh, Tahmineh
, (2019/02/09)
In this work, a novel series of arylisoxazole-phenylpiperazines were designed, synthesized, and evaluated toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Our results revealed that [5-(2-chlorophenyl)-1,2-oxazol-3-yl](4-phenylpiperazin
Synthesis and biochemical evaluation of N-(4-phenylthiazol-2- yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3- hydroxylase
R?ver, Stephan,Cesura, Andrea M.,Huguenin, Philipp,Kettler, Rolf,Szente, Andre
, p. 4378 - 4385 (2007/10/03)
In this paper we describe the synthesis, structure-activity relationship (SAR), and biochemical characterization of N-(4-phenylthiazol-2- yl)benzenesulfonamides as inhibitors of kynurenine 3-hydroxylase. The compounds 3,4-dimethoxy-N-[4-(3-nitrophenyl)thi