DELAPRIL

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C26H32N2O5
Molecular Weight	452.5427
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

CCOC(=O)[C@H](CCC1=CC=CC=C1)N[C@@H](C)C(=O)N(CC(O)=O)C2CC3=C(C2)C=CC=C3

InChI

InChIKey=WOUOLAUOZXOLJQ-MBSDFSHPSA-N

InChI=1S/C26H32N2O5/c1-3-33-26(32)23(14-13-19-9-5-4-6-10-19)27-18(2)25(31)28(17-24(29)30)22-15-20-11-7-8-12-21(20)16-22/h4-12,18,22-23,27H,3,13-17H2,1-2H3,(H,29,30)/t18-,23-/m0/s1

HIDE SMILES / InChI

Description

Delapril is a lipophilic nonsulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been shown to exert potent ACE inhibitory activity and is marketed as an antihypertensive drug. Delapril has been shown to exist in solution as a mixture of s-cis and s-trans conformational isomers, as a result of restricted rotation about the amide bond.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Angiotensin-converting enzyme 94	Inhibitor 8,504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Arterial hypertension 5	Primary		Approved 8,583	VIVACE

C_max

Value	Dose	Analyte	Population
221 ng/mL	30 mg single, oral	DELAPRIL plasma	Homo sapiens
489 ng/mL	30 mg single, oral	DELAPRIL plasma	Homo sapiens
173 ng/mL	30 mg single, oral	DELAPRIL plasma	Homo sapiens
136 ng/mL	30 mg single, oral	DELAPRIL HYDROCHLORIDE plasma	Homo sapiens

AUC

Value	Dose	Analyte	Population
206 ng × h/mL	30 mg single, oral	DELAPRIL plasma	Homo sapiens
572 ng × h/mL	30 mg single, oral	DELAPRIL plasma	Homo sapiens
206 ng × h/mL	30 mg single, oral	DELAPRIL plasma	Homo sapiens
218 ng × h/mL	30 mg single, oral	DELAPRIL HYDROCHLORIDE plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
0.45 h	30 mg single, oral		DELAPRIL plasma	Homo sapiens
0.3 h	30 mg single, oral		DELAPRIL plasma	Homo sapiens

Doses

Doses

Show entries

Dose	Population	Adverse events
90 mg 1 times / day multiple, oral Highest studied dose	unhealthy, ADULT

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PubMed

Show entries

Title	Date	PubMed
Design and synthesis of N-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L -alanyl]-N-(indan-2-yl)glycine (CV-3317), a new, potent angiotensin converting enzyme inhibitor.	1986 Jul	3021350
Long-term effects of delapril on renal function and urinary excretion of kallikrein, prostaglandin E2, and thromboxane B2 in hypertensive patients.	1991 Jan	2009149
Effect of delapril on the vascular angiotensin II release in isolated hind legs of the spontaneously hypertensive rat: evidence for potential relevance of vascular angiotensin II to the maintenance of hypertension.	1991 Sep	1959233
Effects of manidipine and delapril on serum lipids, lipoproteins, and apolipoproteins in patients with mild to moderate essential hypertension: a randomized trial with one-year follow-up.	1992 Nov-Dec	1286488
Pharmacokinetic and pharmacologic properties of delapril, a lipophilic nonsulfhydryl angiotensin-converting enzyme inhibitor.	1995 Jun 16	7778536