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。
| 中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
|---|---|---|---|---|
| —— | (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 |
|
| —— | (Z)-7-[(2S)-2-amino-3-hydroxy-3-oxopropyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | Cefuzoname | 82219-78-1 | C16H15N7O5S4 |
|
| —— | (3S,4S)-3-[(Z)-2-(2-amino-4-thiazolyl)-2-[(carboxymethoxy)imino]acetamido]-4-carbamoyloxymethyl-2-oxo-1-azetidinesulphonic acid | 109362-10-9 | C12H14N6O10S2 |
|
| —— | Cefozopran hydrochloride | 113359-04-9 | C19H17N9O5S2 |
|
| —— | (Z)-7-[(2S)-2-amino-2-carboxyethyl]sulfanyl-2-[[(1R)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | (E)-7-[(2R)-2-amino-2-carboxyethyl]sulfanyl-2-[(2,2-dimethylcyclopropanecarbonyl)amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | 7-[[2-Amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-prop-1-enyl-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;hydrate | 121123-17-9 | C18H21N3O6S |
|
| —— | 6-(1-Hydroxyethyl)-3-[2-[[[(4-nitrophenyl)methoxy-oxomethyl]amino]methylideneamino]ethylthio]-4-[(4-nitrophenyl)methyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate | 98367-45-4 | C27H26N5O10S- |
|
| —— | (4-Nitrophenyl)methyl 2-[(sulfamoylamino)methyl]-4-sulfanylpyrrolidine-1-carboxylate | 148017-03-2 | C13H18N4O6S2 |
|
| —— | trans-2-(((1-(2-Aminothiazol-4-yl)-2-((2-methyl-4-oxo-1-sulphoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropionic acid | 85506-30-5 | C13H17N5O8S2 |
|
| —— | 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid,3-[[(3S,5S)-5-[[(3-carboxyphenyl)amino]carbonyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-, monosodium salt, (4R,5S,6S)- | 153773-82-1 | C22H25N3NaO7S |
|
| —— | (6S,7R)-7-[[(2R)-2-amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(E)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;hydrate | 121123-17-9 | C18H21N3O6S |
|
| —— | 7-[[2-amino-2-(4-hydroxyphenyl)acetyl]amino]-8-oxo-3-[(Z)-prop-1-enyl]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid | 121123-17-9 | C18H19N3O5S |
|
| —— | p-nitrobenzyl (5R,6S)-2-diphenoxy phosphoryloxy-6-[(R)-1-hydroxyethyl]-1-carbapen-2-em-3-carboxylate | 77171-49-4 | C28H25N2O10P |
|
| —— | (4-nitrophenyl)methyl (2S,5S,6R)-6-[(1S)-1-hydroxyethyl]-3,7-dioxo-1-azabicyclo[3.2.0]heptane-2-carboxylate | 74288-40-7 | C16H16N2O7 |
|
| —— | (E)-7-[(2S)-2-amino-2-carboxyethyl]sulfanyl-2-[[(1R)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | (E)-7-[(2R)-2-Amino-2-carboxyethyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | (E)-7-[(2S)-2-amino-2-carboxyethyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoic acid | 82009-34-5 | C16H26N2O5S |
|
| —— | 7-[[(2Z)-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 |
|
| —— | ertapenem sodium | 153773-82-1 | C22H24N3O7S*Na |
|
| —— | cefcapene | 105889-45-0 | C17H19N5O6S2 |
|
| —— | (+)-[[(2Z)-[2-[[(2S 3S)-2-[[(Aminocarbon | 86832-68-0 | C12H14N6NaO10S2 |
|
| —— | Aerugipen | 4697-14-7 | C15H14N2O6S2*2Na |
|
| —— | ticarcillin | 4697-14-7 | C15H14N2O6S2*2Na |
|
| —— | 4-nitrobenzyl-4-(acetylsulfanyl)-2-{[(tert-butoxycarbonyl)(sulfamoyl)amino]methyl}pyrrolidine-1-carboxylate | 491878-06-9 | C20H28N4O9S2 |
|
| —— | 2,2-dimethylpropanoyloxymethyl (2S)-3,3-dimethyl-4,4,7-trioxo-4lambda6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate | 69388-79-0 | C14H21NO7S |
|
| —— | faropenem sodium | 122547-49-3 | C12H14NO5S*Na |
|
| —— | tazobactam sodium | 89785-84-2 | C10H11N4O5S*Na |
|
| —— | tazobactam | 89786-04-9 | C10H12N4O5S |
|
| —— | sodium sulbactam | 69388-84-7 | C8H10NO5S*Na |
|
| —— | Doripenem side-chain | 491878-06-9 | C20H28N4O9S2 |
|
| —— | potassium clavulanate | 61177-45-5 | C8H8NO5*K |
|
| —— | Pivoxil sulbactam | 69388-79-0 | C14H21NO7S |
|
| —— | sulbactam | 68373-14-8 | C8H11NO5S |
|
| —— | 7-[(2-Amino-2-carboxyethyl)thio]-2-[[(2,2-dimethylcyclopropyl)-oxomethyl]amino]-2-heptenoic acid | 82009-34-5 | C16H26N2O5S |
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