| abstract |
The present invention relates to the field of pharmacochemistry and pharmacotherapeutics, and specifically relates to a nitric oxide (NO) donor-type ripasudil derivative, a preparation method therefor, and use thereof. The derivative retains strong ROCK inhibitory activity, inhibits the phosphorylation of myosin light chains in trabecular meshwork cells, and relaxes an aqueous humor efflux pathway of the trabecular meshwork; the released NO can relax the aqueous humor efflux pathway of the trabecular meshwork and inhibit generation of the aqueous humor; the derivative and NO synergistically reduce the intraocular pressure and protect retinal ganglion cells of a mouse in a high intraocular pressure model. The present invention relates to the NO donor-type ripasudil derivative, or a pharmaceutically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing these compounds, and medical use thereof, especially an application in preparing a drug for preventing and/or treating ophthalmic diseases such as glaucoma and high intraocular pressure. |