Andrew Sharpe

Synthesis and profile of SCH351591, a novel PDE4 inhibitor

The syntheses and pharmacological profiles of some 2-trifluoromethyl-8-methoxyquinoline-5-carboxamides are described. SCH351591 is a potent selective inhibitor of phosphodiesterase type 4 (PDE4).

7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.

The synthesis and pharmacological profile of a novel series of 7-methoxy-furo[2,3-c]pyridine-4-carboxamides is described. Some of these compounds were found to be potent inhibitors of phosphodiesterase type 4 (PDE4).

8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: A potential treatment for asthma

A series of bicyclic heteroaryl ring systems was considered as a replacement for the 3-cyclopentyloxy-4-methoxyphenyl moiety in rolipram resulting in the discovery of 8-methoxyquinoline-5-carboxamides as potent inhibitors of phosphodiesterase type 4 (PDE4).

4-hydroxyphenoxymethylene bisphosphonic acid derivatives: potent, non-hydrolysable inhibitors of MYO-inositol monophosphatase

Abstract From a series of 4-hydroxyphenoxymethylene bisphosphonic acid derivatives 1-(4-Hydroxyphenoxy)-1-(methyl)methylenebisphosphonic acid has been identified as a structurally simple, competitive, inhibitor of myo -inositol monophosphatase (IC 50 , 0.33 μM). Replacement of the 1-methyl group by a 3-(3,4-dichlorobenzamido)benzyl substituent affords the most potent inhibitor of the series (IC 50 , 0.08 μM).