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Source: From Graham, S.L. et al. (1989) Journal of Medicinal Chemistry 32, 2548-2554. With permission.

Source: From Graham, S.L. et al. (1989) Journal of Medicinal Chemistry 32, 2548-2554. With permission.

presence of pyridine hydrochloride afforded the phenols 4.94a and b (Graham et al. 1989). These compounds were used to prepare diverse esters and ethers (4.94c-h; Table 4.12), but derivatives bearing other groups and other substitution patterns were also prepared by variants of the synthesis shown in Scheme 4.12.

The inhibitory activity of these derivatives was very good, as seen from the data in Table 4.12. Furthermore, these compounds were devoid of allergenic properties, and some of them, such as the phenol 4.94b or its acetate 4.94c, were shown to act as potent ocular hypotensive agents in animal models (Graham et al. 1989).

SO2NH2

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