Tazobactam acid

한글명:Tazobactam acid

카스 번호89786-04-9

상품명:Tazobactam acid

CBNumberCB7473784

분자식C10H12N4O5S

포뮬러 무게300.29

MOL 파일89786-04-9.mol

화학적 성질

녹는점	115-145℃
끓는 점	77℃
밀도	1.92±0.1 g/cm3(Predicted)
RTECS 번호	XI0191400
인화점	>110°(230°F)
저장 조건	Sealed in dry,Store in freezer, under -20°C
용해도	DMSO(약간 가열), 메탄올(약간 가열, 초음파 처리)에 용해됨
산도 계수 (pKa)	2.33±0.40(Predicted)
색상	흰색에서 황백색까지
수용성	물에 용해됨
안정성	감광성
InChI	InChI=1S/C10H12N4O5S/c1-10(5-13-3-2-11-12-13)8(9(16)17)14-6(15)4-7(14)20(10,18)19/h2-3,7-8H,4-5H2,1H3,(H,16,17)/t7-,8+,10+/m1/s1
InChIKey	LPQZKKCYTLCDGQ-WEDXCCLWSA-N
SMILES	N12[C@@]([H])(CC1=O)S(=O)(=O)[C@@](C)(CN1C=CN=N1)[C@@H]2C(O)=O
CAS 데이터베이스	89786-04-9(CAS DataBase Reference)

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

36/37/38

안전지침서

26-36

WGK 독일

HS 번호

2941106000

NFPA 704:

	0
2		0

그림문자(GHS)

Tazobactam acid 화학적 특성, 용도, 생산

개요
Tazobactam often is coadministered with piperacillin because of tazobactam's ability to inhibit β-lactamases. T azobactam, like other β-lactamase inhibitors, has little or no antibacterial activity. This effect is analogous to that of clavulanic acid and sulbactam.
화학적 성질
White or off-white powder
용도
b-lactamase inhibitor
정의
ChEBI: A member of the class of penicillanic acids that is sulbactam in which one of the exocyclic methyl hydrogens is replaced by a 1,2,3-triazol-1-yl group; used (in the form of its sodium salt) in combination with ceftolozane sulfate for treatment of complicat d intra-abdominal infections and complicated urinary tract infections.
Antimicrobial activity
Tazobactam exhibits little useful antimicrobial activity, although weak activity against Acinetobacter spp. and Borrelia burgdorferi has been reported.
Mechanism of action
Tazobactam functions as an irreversible inhibitor by covalently binding to β-lactamases, and prevents the enzyme hydrolysis of ceftolozane, thereby enhancing its activity against resistant ESBL-producing pathogens, along with expanding coverage to include anaerobes (e.g., Bacteroides spp.)
Clinical Use
Tazobactam is a penicillanic acid sulfone that is similar instructure to sulbactam. It is a more potent β-lactamaseinhibitor than sulbactam and has a slightly broader spectrumof activity than clavulanic acid. It has very weak antibacterialactivity. Tazobactam is available in fixed-dose, injectablecombinations with piperacillin, a broad-spectrum penicillinconsisting of an 8:1 ratio of piperacillin sodium to tazobactamsodium by weight and marketed under the trade name Zosyn.The pharmacokinetics of the two drugs are very similar. Bothhave short half-lives (t_1/2 ～1 hour), are minimally proteinbound, experience very little metabolism, and are excreted inactive forms in the urine in high concentrations.
Approved indications for the piperacillin–tazobactamcombination include the treatment of appendicitis, postpartumendometritis, and pelvic inflammatory disease caused byβ-lactamase–producing E. coli and Bacteroides spp., skin andskin structure infections caused by β-lactamase–producingS. aureus, and pneumonia caused by β-lactamase–producingstrains of H. influenzae.

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