133690-83-2

Upstream product

• 999-09-7 ethyl valerimidate 
• 497-19-8 sodium carbonate 
• 146949-06-6 ethyl N-carbethoxy-valerimidate 
• 10449-07-7 (2-chlorophenyl)hydrazine 
• 557-01-7 Pyrimidin-2(1H)-one 

Downstream Products

• 137314-30-8 5-butyl-4-[4-[(1-carbomethoxy)(1-phenyl)methoxy]phenyl]methyl-2-(2-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one 
• 150312-88-2 4-(4-aminobenzyl)-5-n-butyl-2-(2-chlorophenyl)-2,4-dihydro-3H-1,2,4-triazol-3-one 
• 150312-87-1 5-n-butyl-2-(2-chlorophenyl)-2,4-dihydro-4-(4-nitrobenzyl)-3H-1,2,4-triazol-3-one 
• 150312-86-0 5-n-butyl-2-(2-chlorophenyl)-2,4-dihydro-4-<<2'-(N-trityltetrazol-5-yl)biphenyl-4-yl>methyl>-3H-1,2,4-triazol-3-one 

Relevant academic research and scientific papers

SUBSTITUTED 1,2,4-TRIAZOLES BEARING ACIDIC FUNCTIONAL GROUPS AS ANGIOTENSIN II ANTAGONISTS

Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. STR1

ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED THIOPHENE OR FURAN

Substituted heterocycles attached through a methylene bridge to novel substituted phenyl thiophene or phenyl furan derivative of the Formula I are useful as angiotensin II antagonists. STR1

QUINAZOLINONE, TRIAZOLINONE AND PYRIMIDINONE ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED BENZYL ELEMENT

Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. STR1

Triazolinones as Nonpeptide Angiotensin II Antagonists. 1. Synthesis and Evaluation of Potent 2,4,5-Trisubstituted Triazolinones

A series of 2,4-dihydro-2,4,5-trisubstituted-3H-1,2,4-triazol-3-ones was prepared via several synthetic routes and evaluated as AII receptor antagonists in vitro and in vivo.The preferred compounds contained a methyl side chain at N4 and an n-butyl group at C5.A number of these bearing an alkyl or aralkyl substituent at N2 showed in vitro potency in the nanomolar range (rabbit aorta membrane receptor), and several of these, e.g., the 2,2-dimethyl-1-propyl analogue (54, IC50 = 2.1 nM), effectively blocked the AII pressor response in conscious rats with significant duration (2.5 h at 1 mg/kg orally for 54).Among analogues possessing aryl substituents at N2, ortho substitution on the phenyl moiety resulted in several derivatives with in vitro potency in the low nanomolar range.One of these, featuring a 2-(trifluoromethyl)phenyl substituent at N2 (25, IC50 = 1.2 nM), was effective at 1 mg/kg orally in the rat model, with a duration of >6 h.Implications for hydrophobic and hydrogen-bonding interactions with the AT1 receptor are discussed.

ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED INDOLE OR DIHYDROINDOLE

Substituted heterocycles attached through a methylene bridge to novel substituted indole or dihydroindole derivative of the Formula I are useful as angiotensin II antagonists. STR1

ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED BENZYL ELEMENT

Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. STR1