Synthesis and biological evaluation of oxazole derivatives as T-type

초록

T-type calcium channels are widely expressed in neurons. It is recently reported that T-type calcium channels show subtype-specific and region-specific roles in the pain pathway. At the spinal level, one of subtypes of T-type calcium channel, α1G, is reported to be involved in the development of neuropathic pain presumably by central sensitization. Therefore, antagonizing the subtype may be significant in blocking neuropathic pain at the spinal level. Blocking another subtype of T-type calcium channel, α1H, in the periphery will block all other pain signals that go through the DRG to the central nervous system. As shown previously, the T-type calcium channels are a very important therapeutic target for the treatment of neuropathic pain. The design, synthesis and biological evaluation of oxazole derivatives as T-type calcium channel blockers will be presented in detail.