Pazufloxacin
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Pazufloxacin 속성
- 녹는점
- 269-271°C
- 알파
- D25 -88.0° (c = 0.5 in 0.05N aq NaOH)
- 끓는 점
- 531.5±50.0 °C(Predicted)
- 밀도
- 1.56
- 저장 조건
- 2-8°C
- 용해도
- Aqueous Base (Slightly, Sonicated), DMSO (Slightly, Heated), Methanol (Slightly)
- 산도 계수 (pKa)
- 5.05±0.40(Predicted)
- 색상
- 황백색에서 연한 노란색
- CAS 데이터베이스
- 127045-41-4(CAS DataBase Reference)
안전
위험품 표기 | Xn,C,F | ||
---|---|---|---|
위험 카페고리 넘버 | 20/21/22-34-11 | ||
안전지침서 | 36/37-45-36/37/39-26-16 | ||
WGK 독일 | 3 | ||
RTECS 번호 | UU8815300 | ||
독성 | LD50 i.v. in male mice: >500 mg/kg (Todo) |
Pazufloxacin MSDS
(3S)-10-(1-Aminocyclopropyl)-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid
Pazufloxacin C화학적 특성, 용도, 생산
개요
Pazufloxacin is a novel quinolone marketed for the treatment of bacterial infections in Japan. This tricyclic fluoro-quinolone can be synthesized in 11 steps from commercially available 2,3,4,5tetrafluorobenzoic acid. The cyclopropyl substituent is first introduced in 6 steps including 4-F-substitution with tert-butylcyanoacetate, decarboxylation, aa alkylation with 1 ,Zdibromoethane, partial nitrile hydrolysis and Hoffmann-rearrangement. The pyridoxazine ring is then introduced in 5 steps including 6-ketoester formation and pryridoxazine annulation. Pazufloxacin displays a broad spectrum activity against Grampositive and Gram-negative bacteria, although it is less active that ciprofloxacin against pneumococci and is not active against ciprofloxacin-resistant isolates. In patients with gonococcal urethritis a high prevalence of fluoroquinolone-resistant N. gonorrhoeae isolates with the Ser-91-to-Phe mutation in GyrA was observed. However, good clinical responses have been seen in clinical trials of patients with urinary tract infections and to a lesser extent with respiratory tract infections. Pazufloxacin is mainly excreted in urine with a short half-life (2-2.5 h). It has a phototoxicity equal to that of ciprofloxacin and its adverse effect profile resembles that of other quinolones.용도
Pazufloxacin is a potential antimicrobial and/or antiviral agent.Pharmaceutical Applications
A tricyclic fluoroquinolone, formulated as mesylate and hydrochloride salts for oral or parenteral use or as a methane sulfonate (eye ointment).It displays good activity in vitro against methicillin susceptible Staph. aureus (MIC 0.2 mg/L), but is inactive against Str. pyogenes, Str. pneumoniae (MIC ≥4 mg/L) and enterococci. L. pneumophila is inhibited by 0.03 mg/L. Activity against Enterobacteriaceae, fastidious Gram-negative bacilli, Ps. aeruginosa and Acinetobacter spp. is similar to that of ofloxacin. It is weakly active against Sten. maltophilia and Burkholderia cepacia (MIC c. 2 mg/L). Against M. tuberculosis, MICs range from 0.8 to 4 mg/L. It is inactive against anaerobes.
After oral doses of 100 or 400 mg, peak plasma concentrations range from 0.94 mg/L (100 mg) to 4.5 mg/L (400 mg) after <1 h. The apparent elimination half-life is around 2 h. Most of the administered dose is eliminated in urine, about 70% within 24 h. Four metabolites have been reported. In elderly patients, according to the renal function, the peak plasma concentration may be elevated (up to 5.6 mg/L) and significantly delayed (2–6 h). The plasma protein binding ranges from 17% to 28%.
Pazufloxacin 준비 용품 및 원자재
원자재
1,1′-카보닐디이미다졸
DE
Di-tert-Butyl malonate
소디움 아지이드
Ethyl 2,3,4,5-tetrafluorobenzoate
메탄술폰산
아황산나트륨
트리플루오로아세트 산
Para-포름알데하이드
5-(Acetamido)-N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide
Diphenyldiazomethane
황화디메틸
Ethyl chloroformate
초산에틸
N,N-디메틸포름아마이드 디메틸 아세탈
준비 용품
Pazufloxacin 공급 업체
글로벌( 177)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21691 | 55 |
career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29914 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 |
linda@hubeijusheng.com | CHINA | 28180 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 |
sales@chemdad.com | China | 39916 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 47465 | 58 |
Shaanxi Dideu Medichem Co. Ltd | 18192627656 |
1012@dideu.com | China | 3422 | 58 |
SIMAGCHEM CORP | +86-13806087780 |
sale@simagchem.com | China | 17367 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1026@dideu.com | China | 29271 | 58 |
AFINE CHEMICALS LIMITED | 0571-85134551 |
info@afinechem.com | CHINA | 15377 | 58 |
Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 |
gksales1@gk-bio.com | China | 9339 | 58 |