Novel 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivatives targeting serotonin 2A and adrenergic alpha1 receptors as ocular antihypertensive agents

NOVEL 3,4‐DIHYDROPYRAZINO[1,2‐B]INDAZOL‐1(2H)‐ONE DERIVATIVES TARGETING SEROTONIN 2A AND ADRENERGIC ALPHA1 RECEPTORS AS OCULAR ANTIHYPERTENSIVE AGENTS
Guido Furlotti
TWO TARGETS (5‐HT2A and 1) ONE BULLET (#14) as ocular antihypertensive agent
•Action on different sites of the aqueous humour dynamic pathway (potential synergism)
•Target validated with some drugs (e.g. ketanserin, trazodone)
Our starting point
SAR analysis
In vivo model
14, 0.5%
5‐HT2A
5‐HT4
5‐HT2C 5‐HT2B
1
17th RSC/SCI Medicinal Chemistry Symposium, 8‐11 September 2013, Cambridge, UK