SALINAZID

Details

Stereochemistry	ACHIRAL
Molecular Formula	C13H11N3O2
Molecular Weight	241.2453
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC1=CC=CC=C1\C=N\NC(=O)C2=CC=NC=C2

InChI

InChIKey=VBIZUNYMJSPHBH-OQLLNIDSSA-N

InChI=1S/C13H11N3O2/c17-12-4-2-1-3-11(12)9-15-16-13(18)10-5-7-14-8-6-10/h1-9,17H,(H,16,18)/b15-9+

HIDE SMILES / InChI

Description
Sources: http://www.drugfuture.com/chemdata/salinazid.html | http://www.reference.md/files/C049/mC049137.html

Salinazid (Acozid, Nupasal-213) is an antibacterial agent used primarily as a tuberculostatic. It used to be the treatment of choice for tuberculosis.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mycobacterium tuberculosis H37Rv 11 Target ID: CHEMBL2111188 Sources: https://www.ncbi.nlm.nih.gov/pubmed/13278849	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Tuberculosis 83 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14386367 https://www.ncbi.nlm.nih.gov/pubmed/13446417	Primary		Approved 8583	Acozid Approved Use Antibacterial agent used primarily as a tuberculostatic. It remains the treatment of choice for tuberculosis.

Doses

Dose	Population	Adverse events
800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/13446417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/13446417/	Other AEs: Neuritis... Other AEs: Neuritis (26.3%) Sources: https://pubmed.ncbi.nlm.nih.gov/13446417/

AEs

AE	Significance	Dose	Population
Neuritis	26.3%	800 mg 2 times / day multiple, oral Studied dose Dose: 800 mg, 2 times / day Route: oral Route: multiple Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/13446417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/13446417/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP19A1 429 CYP1A2 2153 CYP2C19 2057	P-gp 2052

Drug as perpetrator

Target	Modality	Activity
CYP3A4 2633	inducer 1966 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 200.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 2.0	yes [IC50 0.5746 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 23.0	yes [IC50 12.3018 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 13.0	yes [IC50 2.1876 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 6.0	yes [IC50 2.1876 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 36.0	yes [IC50 27.5404 uM]
CYP19A1 430	inhibitor 4027 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 14.0	yes [IC50 5.9557 uM]

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
P-gp 2052	substrate 4014 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 156 \| 198 \| 199	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://pubchem.ncbi.nlm.nih.gov/compound/135400471#section=BioAssay-Results Page: 234.0

PubMed

Title	Date	PubMed
Methyl and ethyl ketone analogs of salicylaldehyde isonicotinoyl hydrazone: novel iron chelators with selective antiproliferative action.	2012-05-30	22521999
Inhibition of prolyl hydroxylase protects against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity: model for the potential involvement of the hypoxia-inducible factor pathway in Parkinson disease.	2009-10-16	19679656
The effect of new lipophilic chelators on the activities of cytosolic reductases and P450 cytochromes involved in the metabolism of anthracycline antibiotics: studies in vitro.	2004	15588138

Patents

Sample Use Guides

In Vivo Use Guide

In the therapeutic trial the drugs were given to a test group in the dose of'200 mg of INAH plus 1600 mg of Salinazid (Nupasal-213) daily. Two tablets each containing50 mg INAH and 400 mg Nupasal-213 were given twice daily.A dose of Nupasal-213 of 1500 mg daily is well toleratedby patients not receiving INAH.

Route of Administration: Oral

In Vitro Use Guide

In vitro, the minimum inhibitory concentration (MIC) of Salinazid was 0.09 ug/ml

Name

Type

Language

NSC-33760

Preferred Name

English

SALINAZID

Official Name

English

SALINAZID [MI]

Common Name

English

SALIZID

Common Name

English

Salinazid [WHO-DD]

Common Name

English

salinazid [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C280