A Review on Pyridazinone Compounds ABT-963 as Selective CyclooxygenaseInhibitor

M. Asif
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引用次数: 2

Abstract

Vicinally disubstituted pyridazinones act as potent and selective COX-2 inhibitors. Compound, ABT-963, (2-(3,4-difluoro-phenyl)-4-(3-hydroxy-3-methyl-butoxy)-5-(4-methanesulfonyl-phenyl)-2H-pyridazin-3-one) has an excellent selectivity (ratio of 276, COX-2/COX-1), improved aqueous solubility compared with celecoxib and rofecoxib, high oral anti-inflammatory potency and gastric safety in the animals. After oral administration, ABT-963 reduced prostaglandin (PG) E2 production and reduced the edema. ABT-963 dose dependently reduced nociception. ABT-963 significantly reduced bone loss and soft tissue destruction. ABT-963 is a highly selective COX-2 inhibitor that may be used in the treatment of the pain and inflammation associated with arthritis.
吡嗪酮类化合物ABT-963作为选择性环氧化酶抑制剂的研究进展
邻近二取代吡啶嗪酮作为有效的和选择性的COX-2抑制剂。化合物ABT-963(2-(3,4-二氟苯基)-4-(3-羟基-3-甲基-丁氧基)-5-(4-甲磺酰基-苯基)- 2h -吡嗪-3- 1)具有优良的选择性(比例为276,COX-2/COX-1),与塞来昔布和罗非昔布相比,水溶性提高,口服抗炎效力高,动物胃安全。口服ABT-963后,可减少前列腺素E2的产生,减轻水肿。ABT-963剂量依赖性地减少伤害感受。ABT-963显著减少骨质流失和软组织破坏。ABT-963是一种高选择性COX-2抑制剂,可用于治疗与关节炎相关的疼痛和炎症。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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