zankiren hydrochloride

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

zankiren hydrochloride: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	3086651
CHEMBL ID	2105775
SCHEMBL ID	121553
MeSH ID	M0206685

Synonyms (20)

Synonym
zankiren hydrochloride (usan)
138810-64-7
D03745 ,
zankiren hydrochloride
fb7rz4huhj ,
4-thiazolepropanamide, n-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-alpha-((2-(((4-methyl-1-piperazinyl)sulfonyl)methyl)-1-oxo-3-phenylpropyl)amino)-, monohydrochloride, (1s-(1r,(r(r)),2s,3r*))-
(s)-n-(1s,2r,3s)-1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-alpha((alphas)-alpha-(((4-methyl-1-piperazinyl)sulfonyl)methyl)hydrocinnamamido)-4-thiazolepropionamide monohydrochloride
abbott-72517
4-thiazolepropanamide, n-((1s,2r,3s)-1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-alpha-(((2s)-2-(((4-methyl-1-piperazinyl)sulfonyl)methyl)-1-oxo-3-phenylpropyl)amino)-, monohydrochloride, (alphas)-
zankiren hcl
4-thiazolepropanamide, n-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-alpha-((2-(((4-methyl-1-piperazinyl)sulfonyl)methyl)-1-oxo-3-phenylpropyl)amino)-, monohydrochloride, (1s-(1r(r(r)),2s,3r*))-
zankiren hydrochloride [usan]
unii-fb7rz4huhj
CHEMBL2105775
4-thiazolepropanamide, n-(1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl)-.alpha.-((2-(((4-methyl-1-piperazinyl)sulfonyl)methyl)-1-oxo-3-phenylpropyl)amino)-, monohydrochloride, (1s-(1r,(r(r)),2s,3r*))-
(s)-n-(1s,2r,3s)-1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl]-alpha[(alphas)-alpha-[[(4-methyl-1-piperazinyl)sulfonyl]methyl]hydrocinnamamido]-4-thiazolepropionamide monohydrochloride
zankiren hydrochloride [who-dd]
SCHEMBL121553
DTXSID50160800
Q27277907

Research Excerpts

Bioavailability

Excerpt	Reference	Relevance
"Peptidic renin inhibitors have been poorly absorbed across the intestine or rapidly eliminated by the liver and have been reported to have oral bioavailabilities of less than 2%."	( Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy. Baker, WR; Barlow, J; Cohen, J; Kleinert, HD; Klinghofer, V; Kovar, P; Polakowski, J; Rosenberg, SH; Spina, K; Stein, HH, 1992)	0.28
"Zankiren HCl (A-72517) is a potent renin inhibitor shown to have substantial bioavailability in several animal species and to produce dose-related reductions in blood pressure, plasma renin activity, and angiotensin II (Ang II) in salt-depleted dogs."	( Dose-dependent effects of the renin inhibitor zankiren HCl after a single oral dose in mildly sodium-depleted normotensive subjects. Boger, RS; Glassman, HN; Guyene, TT; Kleinert, HD; Ménard, J; Moyse, DM, 1995)	0.29
" It is an orally bioavailable candidate which is being developed for oral as well as intravenous use."	( Parenteral formulation development of renin inhibitor Abbott-72517. Gupta, SL; Jones, DL; Partipilo, RW; Patel, JP, )	0.13
"Employing a set of empirical guidelines for the design of well-absorbed renin inhibitors, we have followed two strategies to improve potency while maintaining bioavailability."	( Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyc Barlow, JL; Cohen, J; Condon, SL; Klinghofer, V; Kovar, P; Polakowski, J; Rosenberg, SH; Spina, KP; Stein, HH; Yao, Z, 1993)	0.29

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	7 (77.78)	18.2507
2000's	2 (22.22)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 11.56

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	11.56 (24.57)
Research Supply Index	2.64 (2.92)
Research Growth Index	4.20 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.56)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	2 (18.18%)	5.53%
Reviews	3 (27.27%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (54.55%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.	3.37	1	1	chlorobenzoic acid; furans; sulfonamide	environmental contaminant; loop diuretic; xenobiotic
aldosterone [no description available]	3.37	1	1	11beta-hydroxy steroid; 18-oxo steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid hormone; mineralocorticoid; primary alpha-hydroxy ketone; steroid aldehyde	human metabolite; mouse metabolite
valine Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine.	2.02	1	0	L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid; valine	algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
thiazoles [no description available]	7.15	9	2	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.	1.98	1	0	alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
enalkiren [no description available]	3.12	1	0	peptide
valsartan Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION.. valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity.	2.02	1	0	biphenylyltetrazole; monocarboxylic acid amide; monocarboxylic acid	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
bradykinin [no description available]	1.98	1	0	oligopeptide	human blood serum metabolite; vasodilator agent
fumarates Fumarates: Compounds based on fumaric acid.. fumarate(2-) : A C4-dicarboxylate that is the E-isomer of but-2-enedioate(2-)	2.02	1	0	butenedioate; C4-dicarboxylate	human metabolite; metabolite; Saccharomyces cerevisiae metabolite
benazeprilat benazeprilat: structure given in first source. benazeprilat : A benzazepine that is 1,3,4,5-tetrahydro-2H-1-benzazepin-2-one in which the hydrogen attached to the nitrogen is replaced by a carboxy methyl group and in which the 3-pro-S hydrogen is replaced by the amino group of (2S)-2-amino-4-phenylbutanoic acid. An angiotensin-converting enzyme inhibitor, it is used as its monoester prodrug benazepril in the treatment of hypertension and heart failure.	2.02	1	0	benzazepine; dicarboxylic acid; lactam	EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
aliskiren aliskiren: orally active nonpeptidic renin inhibitor. aliskiren : A monomethoxybenzene compound having a 3-methoxypropoxy group at the 2-position and a multi-substituted branched alkyl substituent at the 4-position.	2.02	1	0	monocarboxylic acid amide; monomethoxybenzene	antihypertensive agent
ro 42-5892 remikiren : An L-histidine derivative that is L-histidine in which one of the amino hydrogens is replaced by a (2S)-2-[(2-methylpropane-2-sulfonyl)methyl]-3-phenylpropanoyl group and the carboxy group is replaced by a [(2S,3R,4S)-1-cyclohexyl-4-cyclopropyl-3,4-dihydroxybutan-2-yl]amino group. It is a renin inhibitor which was under development for the treatment of hypertension (now discontinued).	3.5	2	0	cyclopropanes; diol; L-histidine derivative; secondary carboxamide; sulfone	antihypertensive agent; EC 3.4.23.15 (renin) inhibitor; peptidomimetic; vasodilator agent
icatibant icatibant: a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer. icatibant : A ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acute attacks of hereditary angioedema in adult patients.	1.98	1	0
a 74273 A 74273: structure given in first source	3.08	1	0

Condition	Relationship Strength	Studies	Trials
Hypertension, Renal Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.	2.94	1	0
Blood Pressure, Low [description not available]	1.98	1	0
Hypotension Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.	1.98	1	0
Hypotension, Postural [description not available]	3.37	1	1
Hypotension, Orthostatic A significant drop in BLOOD PRESSURE after assuming a standing position. Orthostatic hypotension is a finding, and defined as a 20-mm Hg decrease in systolic pressure or a 10-mm Hg decrease in diastolic pressure 3 minutes after the person has risen from supine to standing. Symptoms generally include DIZZINESS, blurred vision, and SYNCOPE.	3.37	1	1
Cardiac Failure [description not available]	2.9	1	0
Blood Pressure, High [description not available]	2.9	1	0
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	2.9	1	0
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	2.9	1	0

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