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CAS
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78110-38-0
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中文名称
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氨曲南
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英文名称
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Aztreonam
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别名
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SQ-26;776
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纯度
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HPLC≥98%
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分子式
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C13H17N5O8S2
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分子量
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435.43
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外观（性状）
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White to off-white Solid
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储存条件
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Powder : 2-8℃, 2 years; In solvent(母液): -20℃, 1 month; -80℃, 6 months
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溶解性
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Soluble in DMSO ≥5mg/mL
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MDL
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MFCD00072145
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EC
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EINECS 278-839-9
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InChIKey
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WZPBZJONDBGPKJ-VEHQQRBSSA-N
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InChI
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InChI=1S/C13H17N5O8S2/c1-5-7(10(20)18(5)28(23,24)25)16-9(19)8(6-4-27-12(14)15-6)17-26-13(2,3)11(21)22/h4-5,7H,1-3H3,(H2,14,15)(H,16,19)(H,21,22)(H,23,24,25)/b17-8-/t5-,7-/m0/s1
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PubChem CID
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5742832
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SMILES
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CC(C)(O/N=C(C1=CSC(N)=N1)\C(N[C@H]2[C@H](C)N(S(=O)(O)=O)C2=O)=O)C(O)=O
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描述
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是单环β-内酰胺抗生素,与青霉素结合蛋白3(PBP-3)有较高亲和力。(It is a monocyclic β-lactam antibiotic with high affinity for penicillin-binding protein 3 (PBP-3).)
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靶点
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Bacterial
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通路
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Anti-infection
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生物活性
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Aztreonam (also known as SQ 26776) is a synthetic monocyclic beta-lactam antibiotic, used to treat Gram-negative aerobic bacteria infection. It has a very high affinity for penicillin-binding protein 3 (PBP-3). Aztreonam causes significant suppression of human colony forming unit-erythroid (cfu-e), burst forming unit-erythroid (bfu-e) and colony forming unit-granulocyte macrophage (cfu-gm) at both peak and trough serum concentrations in human bone marrow cells. Aztreonam is hydrolyzed at measurable rates by class A beta-lactamases, a TEM-2 type penicillinase and the Proteus vulgaris cephalosporinase with a broad substraterange.[1-3]
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In Vitro
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Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic (a monobactam), with the nucleus based on a simpler monobactam isolated from Chromobacterium violaceum. It was approved by the U.S. Food and Drug Administration in 1986. It is resistant to some beta-lactamases, but is inactivated by extended-spectrum beta-lactamases. Aztreonam has no useful activity against gram-positive or anaerobic microorganisms[1]. Aztreonam (SQ-26) is similar in action to penicillin. It inhibits mucopeptide synthesis in the bacterial cell wall, thereby blocking peptidogly can crosslinking. It has a very high affinity for penicillin-binding protein 3 (PBP-3) and mild affinity for PBP-1a. Aztreonam (SQ-26) binds the penicillin-binding proteins of gram-positive and anaerobic bacteria very poorly and is largely ineffective against them. Aztreonam (SQ-26) is bactericidal but less so than some of the cephalosporins[2].
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In Vivo
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Aztreonam (300 mg/kg) results in a significant decrease in the content of hepatic microsomal P450, while no significant change is observed in hepatic cytochrome b5 content and NADPH-cytochrome c (P450) reductase activity[3]
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数据来源文献
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[1]. Kobayashi Y, et al. Synergy with aztreonam and arbekacin or tobramycin against Pseudomonas aeruginosa isolated from blood. J Antimicrob Chemother. 1992 Dec;30(6):871-2.
[2]. Guay DR, et al. Aztreonam, a new monobactam antimicrobial. Clin Pharm. 1985 Sep-Oct;4(5):516-26.
[3]. Ohmori S, et al. Pharmacology,?994, 48(3), 137-142.
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规格
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10mg 10mM*1mL (in DMSO) 50mg 100mg
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单位
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瓶
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