77982-74-2

Upstream product

• 77982-73-1 (R,S)-5-benzoylamino-4-oxo-6-phenylhexanoic acid methyl ester 
• 83084-67-7 2-Phenyl-4-benzyl-4-β-carbomethoxypropionyloxazolone 
• 83148-55-4 δ-(benzoylamino)-γ-oxobenzenehexanoic acid 
• 5874-61-3 4-benzyl-2-phenyl-2-oxazolin-5-one 

Downstream Products

• 100242-07-7 methyl 5-amino-4-oxo-6-phenylhexanoate hydrochloride 
• 99630-61-2 6-phenyl-5-<(tert-butoxycarbonyl)amino>-4-oxohexanoic acid 
• 100242-08-8 Boc-Tyr-D-Ala-Phe-CH₂-CH₂-CO-OH 
• 100242-11-3 Boc-Tyr-D-Ala-Phe-CH₂-CH₂-CO-NH₂ 
• 100242-09-9 Boc-Tyr-D-Ala-Phe-CH₂-CH₂-CO-OMe 
• 100242-12-4 Boc-tyr-D-Ala-Phe-CH₂-CH₂-CO-NH-Ad 
• 77921-60-9 (S)-1-((S)-5-Acetylamino-4-oxo-6-phenyl-hexanoyl)-pyrrolidine-2-carboxylic acid 
• 83450-73-1 (S)-1-((S)-5-Decanoylamino-4-oxo-6-phenyl-hexanoyl)-pyrrolidine-2-carboxylic acid 
• 83509-06-2 (S)-1-((S)-5-Octanoylamino-4-oxo-6-phenyl-hexanoyl)-pyrrolidine-2-carboxylic acid 
• 83084-86-0 5-n-butyloxycarbonylamino-4-oxo-6-phenylhexanoyl-L-proline 
• 83084-94-0 (S)-1-((S)-5-Hexanoylamino-4-oxo-6-phenyl-hexanoyl)-pyrrolidine-2-carboxylic acid 
• 83450-72-0 5-Decanoylamino-4-oxo-6-phenyl-hexanoic acid methyl ester 

Relevant academic research and scientific papers

Structure-activity relationships of dermorphin tetrapeptides carrying a ketomethylene linkage

The synthesis and in vitro pharmacological tests of 5 ketomethylene tetrapeptide analogues of the opioid heptapeptide dermorphin H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2 are described in this study. The substitution of the original Phe-Gly peptide bond (-CO-NH-) by the ketomethylene linkage (-CO-CH2-) provided analogues with reduced opioid activity.

Derivatives of the potent angiotensin converting enzyme inhibotor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline: Effect of changes at positions 2 and 5 of the hexanoic acid portion

Several derivatives of the potent angiotensin converting enzyme inhibitor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline (1) were synthesized and tested for converting enzyme inhibition activity and blood pressure lowering effects in rats. One compound, 5(S)-benzamido-2(R)-methyl-4-oxo-6-phenylhexanoyl-L-proline (2a), had an I50 against angiotensin converting enzyme of 1.0 x 10-9 M and is the most potent inhibitor prepared thus far in this class of compounds. Testing of 2a orally at 30 mg/kg for inhibition of the angiotensin I induced blood pressure increase in conscious normotensive rats gave 100% inhibition that required 143 min before the angiotensin I blood pressure response returned to 70% of the pretreatment control response. In the conscious renal hypertensive rat, 2a given orally at a dose of 3 mg/kg caused a lowering of blood pressure that reached its maximum of 40 mmHg 8 h following drug administration.