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Clinafloxacin hydrochloride

NMR下載 COA and HPLC MSDS下載
names：
Clinafloxacin hydrochloride, fluoroquinolone antibiotic
CAS號(hào)：
105956-97-6
MDL Number： MFCD00865120
MF(分子式)： C17H17ClFN3O3 MW(分子量)： 365.79
EINECS: Reaxys Number:
Pubchem ID:60063 Brand:BIOFOUNT

克林沙星(105956-97-6,Clinafloxacin,PD-127391)是一種氟喹諾酮類抗生素，克林沙星具有廣泛的抗菌活性?？肆稚承峭瑫r(shí)抑制DNA促旋酶和拓?fù)洚悩?gòu)酶IV。

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中文別名	Clinafloxacin hydrochloride(105956-97-6);克林沙星;7-（3-氨基-1-吡咯烷基）-8-氯-1-環(huán)丙基-6-氟-1,4-二氫-4-氧代-3-喹啉羧酸;7-（3-氨基吡咯烷-1-基）-8-氯-1-環(huán)丙基-6-氟-4-氧代-1,4-二氫喹啉-3-羧酸；
英文別名	Clinafloxacin hydrochloride, fluoroquinolone antibiotic(105956-97-6);AM 1091;AM-1091;CI 960;CI-960;clinafloxacin;PD 127,391;PD 127391;PD-127,391;PD-127391;PD127,391;;7-(3-amino-1-pyrrolidinyl)-8-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid; 7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid;
CAS號(hào)	105956-97-6
Inchi	InChI=1S/C17H17ClFN3O3/c18-13-14-10(5-12(19)15(13)21-4-3-8(20)6-21)16(23)11(17(24)25)7-22(14)9-1-2-9/h5,7-9H,1-4,6,20H2,(H,24,25)CopyCopied
InchiKey	QGPKADBNRMWEQR-UHFFFAOYSA-NCopyCopied
分子式 Formula	C17H17ClFN3O3
分子量 Molecular Weight	365.79
溶解度Solubility	生物體外In Vitro:DMSO溶解度2 mg/mL(5.47 mM;ultrasonic and warming and heat to 80°C)
性狀	淺米色固體
儲(chǔ)藏條件 Storage conditions	-20°C Freezer

克林沙星(105956-97-6,Clinafloxacin,PD-127391)實(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ)，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
152. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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產(chǎn)品說明	克林沙星(105956-97-6,Clinafloxacin,PD-127391)可以作為藥物雜質(zhì)對(duì)照品以及生物醫(yī)藥類試劑。
Introduction	克林沙星(105956-97-6,Clinafloxacin,PD-127391)can be used as a reference substance for drug impurities and reagents，only for research.
Application1
Application2
Application3

克林沙星(105956-97-6,Clinafloxacin,PD-127391)藥理學(xué)：

1、克林沙星是目前正在研究的氟喹諾酮類抗菌劑。已證明具有良好的抗生素特性。但是，由于存在嚴(yán)重的副作用，其批準(zhǔn)和發(fā)布已被暫停。7-（3-氨基-1-吡咯烷基）-8-氯-1-環(huán)丙基-6-氟-4-氧代-3-喹啉羧酸是喹啉的成員。

2、克林沙星是拓?fù)洚悩?gòu)酶II抑制劑，克林沙星可以抑制DNA拓?fù)洚悩?gòu)酶II活性的化合物。包括在該類別中的是靶向拓?fù)洚悩?gòu)酶II的真核形式的多種抗腫瘤劑和靶向于拓?fù)洚悩?gòu)酶II的原核形式的抗微生物劑。

3、克林沙星是抗菌劑，克林沙星可以抑制細(xì)菌生長(zhǎng)或繁殖的物質(zhì)。

4、克林沙星（PD-127391）是氟喹諾酮類抗生素。目標(biāo)：抗菌藥物克林沙星是一種廣譜抗生素，目前正在開發(fā)用于嚴(yán)重感染的靜脈內(nèi)和口服治療的喹諾酮羧酸類。Clinafloxacin是一種新型的氟喹諾酮，對(duì)革蘭氏陽(yáng)性，革蘭氏陰性和厭氧菌具有強(qiáng)大的廣譜體外活性。Clinafloxacin對(duì)肺炎鏈球菌7785具有很高的活性（MIC，0.125μg/ mL），單獨(dú)的gyrA和parC喹諾酮耐藥性突變都對(duì)這種活性沒有太大影響。與氧氟沙星，左氧氟沙星，司巴沙星，格帕沙星相比，克林沙星被認(rèn)為是對(duì)肺炎鏈球菌最具活性的氟喹諾酮。

警示圖
危險(xiǎn)性	warning
危險(xiǎn)性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H333吸入可能對(duì)身體有害
安全防護(hù)	P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P313獲得醫(yī)療建議/護(hù)理
備注	Clinafloxacin實(shí)驗(yàn)過程中防止吸入、食入，做好安全防護(hù)

克林沙星(105956-97-6,Clinafloxacin,PD-127391)危害標(biāo)識(shí)：

象形圖
信號(hào)	Warning
GHS危險(xiǎn)說明	Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory.
	H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]
	Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范說明代碼	P201, P202, P281, P308+P313, P405, and P501
防范說明代碼	(The corresponding statement to each P-code can be found at the GHS Classification page.)

Humphrey, G.H., et al., Pharmacokinetics of clinafloxacin enantiomers in humans. J Clin Pharmacol, 1999. 39(11): p. 1143-50.

Pan, X.S. and L.M. Fisher, DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae. Antimicrob Agents Chemother, 1998. 42(11): p. 2810-6.

Jorgensen, J.H., et al., Activities of clinafloxacin, gatifloxacin, gemifloxacin, and trovafloxacin against recent clinical isolates of levofloxacin-resistant Streptococcus pneumoniae. Antimicrob Agen

Ciprofloxacin and Clinafloxacin Antibodies for an Immunoassay of Quinolones: Quantitative Structure?Activity Analysis of Cross-Reactivities PMID 30641870; International journal of molecular sciences 2

In vitro activities of 11 fluoroquinolones against 226 Campylobacter jejuni strains isolated from Finnish patients, with special reference to ciprofloxacin resistance PMID 16223936; The Journal of ant

克林沙星(105956-97-6,Clinafloxacin,PD-127391)參考文獻(xiàn)：

1.Synthesis of (99m)TcN-clinafloxacin Dithiocarbamate Complex and Comparative Radiobiological Evaluation in Staphylococcus aureus Infected Mice.
Shah SQ1, Khan MR2. World J Nucl Med. 2014 Sep;13(3):154-8. doi: 10.4103/1450-1147.144813.

Clinafloxacin dithiocarbamate (CNND) preparation and radiolabeling through [(99m)Tc ≡ N](2+) core with the gamma (γ) emitter ((99m)Tc) was assessed. The potentiality of the (99m)Tc(V) ≡ N-CNND complex was investigated as perspective a Staphylococcus aureus (S.a.) in vivo infection radiotracer in terms of radiochemical stability in normal saline (n.s.), human serum (h.s.), binding efficacy with live and heat killed S.a. and biodistribution in female nude mice model (FNMD). More than 90% stability was observed in n.s. for 4 h with the highest yield of 98.70 ± 0.26% at 30 min after reconstitution. In h.s., the (99m)Tc(V) ≡ N-CNND complex was found stable up to 16 h with 15.35% side products. Maximum in vitro binding (68.75 ± 0.80%, 90 min) with S.a. was observed after 90 min of incubation. In FNMD, (infected with live strain) approximately six-fold higher uptakes was noted in the infected to inflamed and normal muscles. The higher stability in n.

2.Design and biological evaluation of novel quinolone-based metronidazole derivatives as potent Cu(2+) mediated DNA-targeting antibacterial agents.
Zhang L1, Kumar KV1, Geng RX2, Zhou CH3. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3699-705. doi: 10.1016/j.bmcl.2015.06.041. Epub 2015 Jun 16.

A series of novel quinolone-based metronidazole derivatives as new type of antimicrobial agents were developed and characterized. Most of them gave good antibacterial activity towards the Gram-positive and negative bacteria. Noticeably, quinolone derivative 3i exhibited low MIC value of 0.25 μg/mL against Pseudomonas aeruginosa, which was even superior to reference drugs Norfloxacin, Ciprofloxacin and Clinafloxacin. The further research revealed that compound 3i could intercalate into P. aeruginosa DNA through copper ion bridge to form a steady 3i-Cu(2+)-DNA ternary complex which might further block DNA replication to exert the powerful bioactivities.

3.Heat stable antimicrobial activity of Burkholderia gladioli OR1 against clinical drug resistant isolates.
Bharti P1, Anand V, Chander J, Singh IP, Singh TV, Tewari R. Indian J Med Res. 2012 May;135(5):666-71.

BACKGROUND & OBJECTIVES: Drug resistant microbes are a serious challenge to human health. During the search for novel antibiotics/inhibitors from the agricultural soil, a bacterial colony was found to inhibit the growth of clinical isolates including Staphylococcus (resistant to amikacin, ciprofloxacin, clindamycin, clinafloxacin, erythromycin, gentamicin and methicillin) and Candida (resistant to fluconazole and itraconazole). The culture was identified as Burkholderia gladioli and produced at least five different antimicrobial compounds which were highly stable at high temperature (121 o C) and in the broad pH range (3.0-11.0). We report here the antimicrobial activity of B. gladioli against drug resistant bacterial pathogens.

4.Relationship of cellular topoisomerase IIα inhibition to cytotoxicity and published genotoxicity of fluoroquinolone antibiotics in V79 cells.
Williams GM1, Brunnemann KD, Smart DJ, Molina D, Jeffrey AM, Duan JD, Krebsfaenger N, Kampkoetter A, Schmuck G. Chem Biol Interact. 2013 Apr 25;203(2):386-90. doi: 10.1016/j.cbi.2013.01.003. Epub 2013 Jan 20.

Fluoroquinolone (FQ) antibiotics are bacteriocidal through inhibition of the bacterial gyrase and at sufficient concentrations in vitro, they can inhibit the homologous eukaryotic topoisomerase (TOPO) II enzyme. FQ exert a variety of genotoxic effects in mammalian systems through mechanisms not yet established, but which are postulated to involve inhibition of TOPO II enzymes. To assess the relationship of inhibition of cell nuclear TOPO II to cytotoxicity and reported genotoxicity, two FQ, clinafloxacin (CLFX) and lomefloxacin (LOFX), having available genotoxicity data showing substantial differences with CLFX being more potent than LOFX, were selected for study. The relative inhibitory activities of these FQ on nuclear TOPO IIα in cultured Chinese hamster lung fibroblasts (V79 cells) over dose ranges and at equimolar concentrations were assessed by measuring nuclear stabilized cleavage complexes of TOPO IIα-DNA. Cytotoxicity was measured by relative cell counts.

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