Tibezonium iodide

Names

[ Name ]:
Tibezonium iodide

[Synonym ]:
tibezonium iodide
tibenzonium iodide
Antoral
Ethanaminium,N,N-diethyl-N-methyl-2-[[4-[4-(phenylthio)phenyl]-3H-1,5-benzodiazepin-2-yl]thio]-,iodide
Tibezonium
N,N-Diethyl-N-methyl-2-[[4-[4-(phenylthio)phenyl]-3H-1,5-benzodiazepin-2-yl]thio]ethanaminium iodide
Rec 15-0691
Thiabenzazonium
2-(Methyl-diaethylammonium-aethylthio)-4-(p-phenyl-thio-phenyl)-3H-1,5-benzodiazepin-jodid
Tibezonium-jodid

Biological Activity

[Description]:

Tibezonium iodide, an oropharyngeal disinfectant, has antibacterial activity for the prevention of mouth infections[1].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

[In Vitro]

Tibezonium iodide (5-10 μg/mL; 15-30 min) displays good bacteriostatic and bactericidal activity against gram-positive strain, especially against S. aureus and S. pyogens humanus with the minimum inhibitory concerntration (MIC) values ≤1 μg/mL)[3]. Tibezonium iodide (0.25-5 μg/mL; 30 min) displays increasing bactericidal activity against S. aureus and S. pyogens 821 while pH value going up from 6.5-7.0 to 8.0-8.5[3].

[References]

[1]. M Veronese, et al. Mutagenicity studies on tibezonium, a new oropharyngeal disinfectant. Arzneimittelforschung. 1983;33(3):369-72.

[2]. M Calzavara, et al. [Clinico-experimental study of a new antibactorial agent for local use in stomatology]. Minerva Stomatol. Apr-Jun 1976;25(2):55-66.

[3]. Veronese M, et al. Antimicrobial activity of tibezonium (TBZ). Chemotherapy. 1977. 23(2):90-7.

Chemical & Physical Properties

[ Melting Point ]:
162ºC

[ Molecular Formula ]:
C₂₈H₃₂IN₃S₂

[ Molecular Weight ]:
601.60800

[ Exact Mass ]:
601.10800

[ PSA ]:
75.32000

[ LogP ]:
3.48710

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KH2770000

CHEMICAL NAME :: Ethanaminium, N,N-diethyl-N-methyl-2-((4-(4-(phenylthio)phenyl)- 3H-1,5-benzodiazepin-2-yl) thio)-, iodide

CAS REGISTRY NUMBER :: 54663-47-7

LAST UPDATED :: 199206

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C28-H32-N3-S2.I

MOLECULAR WEIGHT :: 601.65

WISWESSER LINE NOTATION :: T67 GN KN IHJ HS2K2&2&2 JR DSR &I

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >10 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 31,440,1975

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 3,152,1978

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 9 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 31,440,1975

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 42 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: EXPEAM Experientia. (Birkhaeuser Verlag, POB 133, CH-4010 Basel, Switzerland) V.1- 1945- Volume(issue)/page/year: 31,440,1975