Formamides

A number of studies have been published wherein formoterol was used as a lead and the results suggest that the increase of lipophilicity of new analogues is related to the increase in their duration of action [24]. The authors suggest that the extended duration of action of compounds 8 and 9 is attributable to greater membrane partitioning of these analogues in line with the diffusion micro kinetic theory [21]. Both analogues 8 and 9 produced greater than twofold longer duration of action than formoterol in EFS-stimulated guinea-pig trachea preparations. Additionally, compound 8 also appeared to have a rapid onset of action. No further information regarding the development of either 8 or 9 has been reported.

NHCHO

NHCHO

With the intense interest in developing once daily ^-adrenoceptor agonists and with a heavy reliance on common structural leads, it is not surprising that more similarities than differences exist between final products from independent research efforts (cf. 8 and 10).

Progress in the Development of Adrenoceptor Agonists OH

Progress in the Development of Adrenoceptor Agonists OH

NHCHO

NHCHO

Extensive efforts to further develop the series exemplified by 10 [25] have delivered compounds 11 and 12, which contain alternative heteroatom patterns [26,27]. For compound 12, the preparation of a crystalline salt form was confirmed by powder X-ray diffraction studies.

NHCHO

NHCHO

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