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Cilazapril monohydrate

Cilazapril monohydrate structure

CAS No:
92077-78-6
Formula:
C22H31N3O5.H2O
Chemical Name:
Cilazapril monohydrate
Synonyms:
6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid,9-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]octahydro-10-oxo-,hydrate (1:1),(1S,9S)-;6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid,9-[[1-(ethoxycarbonyl)-3-phenylpropyl]amino]octahydro-10-oxo-,monohydrate,[1S-[1α,9α(R*)]]-;6H-Pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid,9-[[(1S)-1-(ethoxycarbonyl)-3-phenylpropyl]amino]octahydro-10-oxo-,monohydrate,(1S,9S)-;Cilazapril monohydrate
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Cilazapril Monohydrate is a angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and congestive heart failure.Target: ACECilazapril is a new nonthiol group containing angiotensin converting enzyme (ACE) inhibitor. Cilazapril has been investigated in more than 4000 patients with all degrees of hypertension, as well as in the special patient groups such as the elderly, renally impaired, and patients with concomitant diseases, such as congestive cardiac failu

Cilazapril monohydrate is a hydrate that is the monohydrate of cilazapril. It is used for the treatment of hypertension and heart failure. It has a role as an antihypertensive agent, an EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor and a prodrug. It contains a cilazapril.|Cilazapril Monohydrate is a pyridazine angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, cilazapril is rapidly metabolized in the liver to cilazaprilat; cilazaprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II, resulting in vasodilation. Cilazaprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.|One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat.

Cilazapril monohydrate Basic Attributes

Molecular Weight：

435.51

Exact Mass：

435.23700

UNII：

19KW7PI29F

DSSTox ID：

DTXSID00238846

NCI Thesaurus Code：

C76133

Characteristics

PSA：

100

XLogP3：

1.79790

Melting Point：

98° (dec)

Boiling Point：

598.1ºC at 760mmHg

Flash Point：

315.5ºC

Specific rotation：

D20 -62.51° (c = 1% in ethanol)

Safety Information

Precautionary statement(s)：

P201, P202, P281, P308+P313, P405, P501

Hazard Statements：

H361

GHS Classification：

|Warning|H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]|P201, P202, P281, P308+P313, P405, and P501|Aggregated GHS information provided by 3 companies from 2 notifications to the ECHA C&L Inventory.

Drug Information

MeSH：

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS. (See all compounds classified as Antihypertensive Agents.)|A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility. (See all compounds classified as Angiotensin-Converting Enzyme Inhibitors.)

MeSH Entry Terms：

Cilazapril

Cilazapril monohydrate Use and Manufacturing

Angiotensin converting enzyme inhibitor. Used for mild to moderate primary and intractable hypertension.

Computed Properties

Molecular Weight:435.5
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:9
Exact Mass:435.23693578
Monoisotopic Mass:435.23693578
Topological Polar Surface Area:100
Heavy Atom Count:31
Complexity:608
Defined Atom Stereocenter Count:3
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

Material

Potassium bicarbonate

Sodium carbonate