15037-34-0Relevant articles and documents
Targeting Serotonin 2A and Adrenergic α1 Receptors for Ocular Antihypertensive Agents: Discovery of 3,4-Dihydropyrazino[1,2-b]indazol-1(2H)-one Derivatives
Furlotti, Guido,Alisi, Maria Alessandra,Cazzolla, Nicola,Ceccacci, Francesca,Garrone, Beatrice,Gasperi, Tecla,La Bella, Angela,Leonelli, Francesca,Loreto, Maria Antonietta,Magarò, Gabriele,Mangano, Giorgina,Bettolo, Rinaldo Marini,Masini, Emanuela,Miceli, Martina,Migneco, Luisa Maria,Vitiello, Marco
supporting information, p. 1597 - 1607 (2018/07/30)
Glaucoma affects millions of people worldwide and causes optic nerve damage and blindness. The elevation of the intraocular pressure (IOP) is the main risk factor associated with this pathology, and decreasing IOP is the key therapeutic target of current pharmacological treatments. As potential ocular hypotensive agents, we studied compounds that act on two receptors (serotonin 2A and adrenergic α1) linked to the regulation of aqueous humour dynamics. Herein we describe the design, synthesis, and pharmacological profiling of a series of novel bicyclic and tricyclic N2-alkyl-indazole-amide derivatives. This study identified a 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivative with potent serotonin 2A receptor antagonism, >100-fold selectivity over other serotonin subtype receptors, and high affinity for the α1 receptor. Moreover, upon local administration, this compound showed superior ocular hypotensive action in vivo relative to the clinically used reference compound timolol.
SEROTONIN ANTAGONISTS, THEIR PREPARATION AND MEDICATIONS CONTAINING THEM
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, (2008/06/13)
This invention relates to compounds of formula: STR1 in which R. sub.1 denotesa 1,2,3,6-tetrahydro-1-pyridyl radical substituted in the 4-position by an optionally substituted phenyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, a 1-piperazinyl radical substituted in the 4-position by an optionally substituted phenyl, 1,2-benzisothiazol-3-yl, 1,2-benzisoxazol-3-yl or 2-pyridyl radical,a piperidino radical substituted in the 4-position by an optionally substituted phenyl, bis(4-fluorophenyl)methylene, 4-fluorobenzoyl, optionally substituted 2-oxo-1-benzimidazolinyl, optionally substituted 3-indolyl or 3-(5-hydroxyindolyl) radical, by two phenyl radicals or a hydroxyl radical and an optionally substituted phenyl radicalR 2 denotes a radical SO. sub.2 R 4 in which R 4 denotes an alkyl or phenyl radical,R 3 denotes a phenyl or naphthyl radical, or else R 2 and R 3 together with the nitrogen atom to which they are attached form a ring,n is equal to 2, 3 or 4, processes for their preparation and medications containing them. The invention relates to treating a disease ameliorated by serotonin.
Synthesis and Biological Activities of 3-Substituted 1-Aryloxyaminopropanes
Agarwal, Shiv K.,Kumar, Yatendra,Saxena, Anil K.,Jain, Padam C.,Anand, Nitya
, p. 435 - 439 (2007/10/02)
A number of 3-substituted 1-aryloxyaminopropanes (9-43) have been prepared by the reaction of appropriate hydroxyaryl compound with 1-chloro-3-1-(N4-aryl-piperazinyl/piperidinyl)>propanes (1-8).The 1-(6/7-quinolyloxy)-3-substituted