β-内酰胺酶抑制剂
β-内酰胺酶抑制剂是指能够抑制β-内酰胺酶活性、减少或防止β-内酰胺类抗生素被水解的物质，与β-内酰胺抗生素联合使用时，可以对抗耐药菌株，扩大抗菌谱并增强其抗菌效果。根据作用机制的不同，β-内酰胺酶抑制剂可分为竞争性和非竞争性两大类。
竞争性抑制剂
- 可逆的：这类抑制剂与β-内酰胺酶上的活性部位竞争结合，但不发生化学反应，一旦移除抑制剂，酶即可恢复功能。常见的例子包括邻氯唑青霉素（cl-oxacillin）和双氯唑青霉素（dicloxacillin）等。
- 不可逆的：这类抑制剂与酶之间会发生不可逆的化学反应，导致酶失活。即使移除抑制剂，酶也无法再生。代表性的例子有棒酸及青霉烷砜。
非竞争性抑制剂 这类抑制剂不与底物竞争酶的催化部位，而是在远离催化位点的地方结合到酶上，从而改变其结构使其失效。甲氧苯青霉素（methicillin）在低浓度时表现为竞争性抑制剂，在高浓度下则转为非竞争性抑制剂。
相关化合物
| 中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
|---|---|---|---|---|
| 西司他丁 | cilastatine | 82009-34-5 | C16H26N2O5S |
|
| 舒巴坦钠 | 69388-84-7 | C8H11NNaO5S |
|
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| 舒巴坦酸 | sulbactum | 68373-14-8 | C8H11NO5S |
|
| 舒巴坦匹酯 | (pivaloyloxy)methyl 6,6-dihydropenicillanate S,S-dioxide | 69388-79-0 | C14H21NO7S |
|
| 舒他西林 | sultamicillin T | 76497-13-7 | C25H30N4O9S2 |
|
| 美罗培南侧链 | (2S,4S)-1-p-nitrobenzyloxycarbonyl-2-dimethylaminocarbonyl-4-thiolpyrrolidine | 96034-64-9 | C15H19N3O5S |
|
| 美罗培南中间体 | 3-(2-Bromopropionyl)spiro-<2,3-dihydro-4H-1,3-benzoxazine-2,1'-cyclohexan>-4-one | 158299-05-9 | C16H18BrNO3 |
|
| 美罗培南 | meropenem | 96036-03-2 | C17H25N3O5S |
|
| 硫霉素 | thienamycin | 59995-64-1 | C11H16N2O4S |
|
| 硫培南 | sulopenem | 120788-07-0 | C12H15NO5S3 |
|
| 泰比培南酯中间体 | 1-(4,5-dihydro-1,3-thiazol-2-yl)-3-mercaptoazetidine hydrochloride | 179337-57-6 | C6H10N2S2*ClH |
|
| 泰比培南酯 | tebipenem | 161715-24-8 | C22H31N3O6S2 |
|
| 泰比培南 | Tebipenem | 161715-21-5 | C16H21N3O4S2 |
|
| 法罗培南钠 | 4-Thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid,6-[(1R)-1-hydroxyethyl]-7-oxo-3-[(2R)-tetrahydro-2-furanyl]-,monosodium salt, (5R,6S)- | 122547-49-3 | C12H15NNaO5S |
|
| 法罗培南酯 | faropenem medoxomil | 141702-36-5 | C17H19NO8S |
|
| 法罗培南 | faropenem | 106560-14-9 | C12H15NO5S |
|
| 氨曲南 | azthreonam | 78110-38-0 | C13H17N5O8S2 |
|
| 比阿培南侧链 | 6-mercapto-6,7-dihydro-5H-pyrazolo<1,2-a><1,2,4>triazolium chloride | 153851-71-9 | C5H8N3S*Cl |
|
| 帕尼培南 | panipenem | 87726-17-8 | C15H21N3O4S |
|
| 头孢唑喃 | cefuzonam | 82219-78-1 | C16H15N7O5S4 |
|
| 头孢唑兰 | cefozopran | 113359-04-9 | C19H17N9O5S2 |
|
| 头孢卡品酯 | cefcapene pivoxil | 105889-45-0 | C23H29N5O8S2 |
|
| 头孢克洛 | cefaclor monohydrate | 70356-03-5 | C15H14ClN3O4S*H2O |
|
| 多尼培南缩合物 | (4R,5S,6S)-3-[[(3S,5S)-5-[[(aminosulfonyl)amino]methyl]-1-[[(4-nitrophenyl)methoxy]carbonyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid (4-nitrophenyl)methyl ester | 491878-07-0 | C30H34N6O12S2 |
|
| 多尼培南侧链 | (2S,4S)-4-mercapto-2-(N-sulfamoyl-aminomethyl)-1-(4-nitrobenzyloxycarbonyl)pyrrolidine | 148017-03-2 | C13H18N4O6S2 |
|
| 多尼培南侧链 | (2S,4S)-4-acetylthio-2-(N-sulfamoyl-tert-butoxycarbonylaminomethyl)-1-(4-nitrobenzyloxycarbonyl)pyrrolidine | 491878-06-9 | C20H28N4O9S2 |
|
| 多尼培南(一水合物) | (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3-[[(3S,5S)-5-(sulfamoylaminomethyl)pyrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid monohydrate | 364622-82-2 | C15H24N4O6S2*H2O |
|
| 多尼培南 | doripenem | 148016-81-3 | C15H24N4O6S2 |
|
| 厄他培南侧链 | 3-[[[(2S,4S)-4-mercapto-1-(4-nitrobenzyloxy)carbonyl-2-pyrrolidinyl]carbonyl]amino]benzoic acid | 202467-69-4 | C20H19N3O7S |
|
| 厄他培南 | ertapenem | 153832-46-3 | C22H25N3O7S |
|
| 卡芦莫南 | Carumonam | 87638-04-8 | C12H14N6O10S2 |
|
| 利替培南 | Ritipenem (FCE 22101) | 84845-57-8 | C10H12N2O6S |
|
| 克拉维酸钾 | Potassium clavulanate, from Streptomyces clavuligerus | 61177-45-5 | C8H9KNO5 |
|
| 保护亚胺培南 | Protected Imipenem | 98367-45-4 | C27H27N5O10S |
|
| 他唑巴坦钠 | 89785-84-2 | C10H12N4NaO5S |
|
|
| 他唑巴坦 | tazobactam acid | 89786-04-9 | C10H12N4O5S |
|
| 亚胺培南母核 | 4-nitrobenzyl (5R,6S)-6-[(R)-1-hydroxyethyl]-2-oxo-1-carbapenam-3-carboxylate | 74288-40-7 | C16H16N2O7 |
|
| 亚胺培南-西司他丁钠 | Imipenem and cilastatin | 92309-29-0 | C28H43N5O9S2 |
|
| 亚胺培南(一水物) | imipenem monohydrate | 74431-23-5 | C12H17N3O4S*H2O |
|
| 1,2-二羧基吡咯烷酸,4-羟基-1-[(4-硝基苯基)甲基]酯 | (2S,4R)-4-Hydroxy-1-(4-nitrobenzyloxycarbonyl)pyrrolidine-2-carboxylic acid | 96034-57-0 | C13H14N2O7 |
|
| (2S,4r)-4-[(甲基磺酰基)氧基]-1,2-吡咯烷二羧酸 2-甲基 1-[(4-硝基苯基)甲基]酯 | (2S,4R)-4-mesyloxy-1-(p-nitrobenzyloxycarbonyl)pyrrolidine-2-carboxylic acid methyl ester | 138324-82-0 | C15H18N2O9S |
|
| —— | aztreonam | 78110-38-0 | C13H17N5O8S2 |
|
| —— | Amasulin | 86832-68-0 | C12H12N6Na2O10S2 |
|
| —— | Cilastatin, Antibiotic for Culture Media Use Only | 82009-34-5 | C16H26N2O5S |
|
| —— | Disodium 3-{[(4-{[2-carboxy-6-(1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-en-3-yl]sulfanyl}pyrrolidin-2-yl)(oxidanidyl)methylidene]amino}benzoate | 153832-38-3 | C22H23N3Na2O7S |
|
| —— | Cefprozil monohydrate | 121123-17-9 | C18H21N3O6S |
|
| —— | (6R,7R)-3-((1H-imidazo[1,2-b]pyridazin-4-ium-1-yl)methyl)-7-((Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(methoxyimino)acetamido)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | 113359-04-9 | C19H17N9O5S2 |
|
| —— | Cilistatin | 82009-34-5 | C16H26N2O5S |
|
| —— | 7-[(2S)-2-amino-2-carboxyethyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | 7-[[2-(5-Amino-1,2,4-thiadiazol-3-yl)-2-methoxyiminoacetyl]amino]-3-(imidazo[1,2-b]pyridazin-1-ium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | 113359-04-9 | C19H17N9O5S2 |
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