抗生素类药物
人类发现的第一个抗生素类药物是青霉素，它是在第二次世界大战期间发展起来的一种有效抗感染药剂。实际上，早在19世纪70年代，人们就认识到了微生物之间拮抗现象的存在。直到1942年，瓦克斯曼（S.A. Waksman）在多年研究这些作用的活性后，才首次使用了“抗生素”一词。
1928年，弗莱明（A. Fleming）已发现青霉素，但当时尚未证实这种天然来源的抗微生物药剂能对人和动物全身感染发挥效力。直至战争的压力刺激了防治传染病药剂的研究，弗洛里（H.W. Florey）及其同事钱恩（E.B. Chain）才成功提取出青霉素并证明其治疗效果。1943年，瓦克斯曼发现第二个抗生素——链霉素，随后又观察分离出的杆菌肽、新霉素、多粘菌素、氯霉素、金霉素和土霉素等其他抗生素的作用后，抗生素的重要性逐渐显现。
随着抗生素在化学治疗中的成功应用，它们也被发现广泛用于植物保护、动物饲养和食品保藏等方面。抗生素又称“抗菌素”，一般是指由细菌、霉菌或其他微生物在生活过程中产生的具有抗病原体性能的一类物质。这类药物是控制人、畜传染病，对抗肿瘤以及防治植物病虫害的重要工具。抗生素通常是从微生物培养液中提取或通过半合成和合成方法制造。它们根据来源和作用大致分为青霉素类、头孢菌素类、氨基糖甙类、四环素族、氯霉素类、大环内脂类、抗霉菌类、抗肿瘤类等，并可根据抗菌谱范围分为广谱和窄谱。
各种抗生素的抗菌机制和作用各不相同。例如，青霉素和杆菌肽能阻碍细菌细胞壁的合成；多肽类抗菌素可破坏细菌质膜；氯霉素、链霉素等则可抑制蛋白质合成或干扰核酸合成。有些抗生素的作用范围有限，如青霉素只对革兰氏阳性菌有效，被称为狭谱抗生素。而四环素类药物对多数细菌有抑制作用，则称为广谱性抗生素。
目前广泛应用的约100种抗生素包括青霉素、链霉素和庆大霉素等，这些药物在医疗上普遍使用；而在农业中，春雷霉素、井岗霉素已广泛用于水稻病菌防治，灭瘟素则用于防治稻瘟病，赤霉素则促进植物生长。然而，在使用抗生素时需谨慎，不可滥用或乱用。有些抗生素可能产生副作用，例如长期使用链霉素和庆大霉素会导致耳聋；过量服用氯霉素可能导致白细胞减少。另外，某些人对抗生素可能有过敏反应，严重者甚至有致命危险，因此在使用青霉素等药物前应进行“皮试”。
合理用药是抗生素应用中的关键问题。盲目滥用广谱抗生素不仅会促使抗药菌株的产生，还会导致不可忽视的毒副作用，并可能导致因破坏体内正常菌群而引发“二次感染”。因此，严格按照医嘱用药至关重要。
| 中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
|---|---|---|---|---|
| —— | [(2R,3R,4S,5R)-6-[2-chloro-1-[[(2S)-1-methyl-4-propylpyrrolidine-2-carbonyl]amino]propyl]-4,5-dihydroxy-2-methylsulfanyloxan-3-yl] hexadecanoate;hydrochloride | 25507-04-4 | C34H64Cl2N2O6S |
|
| —— | (6S,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-(6,7-dihydro-5H-cyclopenta[b]pyridin-1-ium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate;sulfuric acid | 98753-19-6 | C22H24N6O9S3 |
|
| —— | 1-methyl-1-nitroso-3-[(2R,4R,5S,6R)-2,4,5-trihydroxy-6-(hydroxymethyl)oxan-3-yl]urea | 18883-66-4 | C8H15N3O7 |
|
| —— | (2S,4R)-N-[2-hydroxy-1-[(3R,4R,5S)-3,4,5-trihydroxy-6-methylsulfanyloxan-2-yl]propyl]-1-methyl-4-propylpyrrolidine-2-carboxamide;hydrochloride | 859-18-7 | C18H35ClN2O6S |
|
| —— | sodium;(6S,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | 68401-82-1 | C13H12N5NaO5S2 |
|
| —— | (3R,4S,5S,6S,7R,9R,10E,11S,12R,13S,14R)-6-[4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl)oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one | 80214-83-1 | C41H76N2O15 |
|
| —— | 6H-Oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione, 8-chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-, (1aR,2Z,4E,14R,15aR)- | 12772-57-5 | C18H17ClO6 |
|
| —— | (3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[(3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecan-2-one | 80214-83-1 | C41H76N2O15 |
|
| —— | [(2S,3R,4S,6R)-4-(dimethylamino)-2-[[(3R,4S,5S,6R,7R,9R,11R,12R,13R,14R)-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yl]oxy]-6-methyloxan-3-yl] propanoate;dodecyl hydrogen sulfate | 3521-62-8 | C52H97NO18S |
|
| —— | 2,7-(Epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]pyrido[1,2-a]benzimidazole-1,15(2H)-dione,25-(acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-,(2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)- | 80621-81-4 | C43H51N3O11 |
|
| —— | [(4R,5S,6S,7R,9R,10R,11Z,13Z,16R)-6-[(2S,3R,4R,5S,6R)-4-(dimethylamino)-3-hydroxy-5-[(2S,4R,5S,6S)-4-hydroxy-4,6-dimethyl-5-propanoyloxyoxan-2-yl]oxy-6-methyloxan-2-yl]oxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)-1-oxacyclohexadeca-11,13-dien-4-yl] propanoate | 35457-80-8 | C41H67NO15 |
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| —— | (4R,5S,6S,7R,9R,11Z,13Z,15R,16R)-6-[(2R,3R,4S,5S,6R)-4-(dimethylamino)-3,5-dihydroxy-6-methyloxan-2-yl]oxy-7-[2-[(3R,5S)-3,5-dimethylpiperidin-1-yl]ethyl]-16-ethyl-4-hydroxy-15-[[(2R,3R,4R,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyloxan-2-yl]oxymethyl]-5,9,13-trimethyl-1-oxacyclohexadeca-11,13-diene-2,10-dione | 108050-54-0 | C46H80N2O13 |
|
| —— | (1R,2R,4R,6S,7R,8R,10R,13S,14S)-7-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyl-tetrahydropyran-2-yl]oxy-13-ethyl-6-methoxy-2,4,6,8,10,14-hexamethyl-17-[4-[4-(3-pyridyl)imidazol-1-yl]butyl]-12,15-dioxa-17-azabicyclo[12.3.0]heptadecane-3,9,11,16-tetrone | 191114-48-4 | C43H65N5O10 |
|
| —— | (2S,3R,4R,5R,6S)-2-[(2R,3R,4S,5S,6R)-5-hydroxy-6-(hydroxymethyl)-2-[[(1S,2S,7S,10R,14S,15R,16S,17R,20S)-10,14,16,20-tetramethyl-22-azahexacyclo[12.10.0.02,11.05,10.015,23.017,22]tetracos-4-en-7-yl]oxy]-4-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol | 20562-02-1 | C45H73NO15 |
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| —— | N-[(2S)-4-amino-1-[[(2S,3R)-1-[[(2S)-4-amino-1-oxo-1-[[(3S,6S,9S,12S,15R,18R,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxobutan-2-yl]-6-methyloctanamide;sulfuric acid | 1405-20-5 | C56H100N16O17S |
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| —— | Antibiotic AM-2282;STS;AM-2282 | 62996-74-1 | C28H26N4O3 |
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| —— | [(4Z,6Z,8R,9R,10Z,12R,13S,14R,16R)-13-hydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-9-yl] carbamate | 30562-34-6 | C29H40N2O9 |
|
| —— | Leucomycin V, 9-O-[(2R,5S,6R)-5-(dimethylamino)tetrahydro-6-methyl-2H-pyran-2-yl]- | 8025-81-8 | C43H74N2O14 |
|
| —— | (5R)-2-[4,6-diamino-3-[3-amino-6-[1-(methylamino)ethyl]oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-(methylamino)oxane-3,5-diol | 1403-66-3 | C21H43N5O7 |
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| —— | (1S)-33-(4-amino-3,5-dihydroxy-6-methyloxan-2-yl)oxy-1,3,4,7,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo[33.3.1]nonatriaconta-19,21,25,27,29,31-hexaene-36-carboxylic acid | 1400-61-9 | C47H75NO17 |
|
| —— | (1R,35R)-33-(4-amino-3,5-dihydroxy-6-methyloxan-2-yl)oxy-1,3,5,6,9,11,17,37-octahydroxy-15,16,18-trimethyl-13-oxo-14,39-dioxabicyclo[33.3.1]nonatriaconta-19,21,23,25,27,29,31-heptaene-36-carboxylic acid | 1397-89-3 | C47H73NO17 |
|
| —— | 2-[5-hydroxy-6-(hydroxymethyl)-2-[[(10R,14S)-10,14,16,20-tetramethyl-22-azahexacyclo[12.10.0.02,11.05,10.015,23.017,22]tetracos-4-en-7-yl]oxy]-4-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol | 20562-02-1 | C45H73NO15 |
|
| —— | (1S,2R,18R,19R,22S,25R,28R,40S)-2-[(2R,4S,5R,6S)-4-amino-5-hydroxy-4,6-dimethyloxan-2-yl]oxy-22-(2-amino-2-oxoethyl)-5,15-dichloro-48-[(2S,3R,4S,5S,6R)-3-[(2S,4S,5R,6S)-4-[[4-(4-chlorophenyl)phenyl]methylamino]-5-hydroxy-4,6-dimethyloxan-2-yl]oxy-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-18,32,35,37-tetrahydroxy-19-[[(2R)-4-methyl-2-(methylamino)pentanoyl]amino]-20,23,26,42,44-pentaoxo-7,13-dioxa-21,24,27,41,43-pentazaoctacyclo[26.14.2.23,6.214,17.18,12.129,33.010,25.034,39]pentaconta-3,5,8,10,12(48),14,16,29(45),30,32,34(39),35,37,46,49-pentadecaene-40-carboxylic acid;phosphoric acid | 192564-14-0 | C86H100Cl3N10O30P |
|
| —— | (1S,2R,3R,6R,7R,8R,9R,10R,12R,13S,15R,17R)-9-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-3-ethyl-2,10-dihydroxy-7-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-15-(2-methoxyethoxymethyl)-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one | 62013-04-1 | C42H78N2O14 |
|
| —— | (1R,2S,5R,7R,8R,9R,11R,13R,14R)-8-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-2-ethyl-9-methoxy-1,5,7,9,11,13-hexamethyl-15-[4-(4-pyridin-3-ylimidazol-1-yl)butyl]-3,17-dioxa-15-azabicyclo[12.3.0]heptadecane-4,6,12,16-tetrone | 191114-48-4 | C43H65N5O10 |
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| —— | Ceftriaxone Sodium | 74578-69-1 | C36H46N16Na4O21S6 |
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| —— | (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 |
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| —— | (2R,3R)-2,3-dihydroxybutanedioic acid;2-[(4R,5S,6S,7R,9R,11Z,13Z,15R,16R)-6-[(2R,3R,4R,5S,6R)-5-[(2S,4R,5S,6S)-4,5-dihydroxy-4,6-dimethyloxan-2-yl]oxy-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-16-ethyl-4-hydroxy-15-[[(2R,3R,4R,5R,6R)-5-hydroxy-3,4-dimethoxy-6-methyloxan-2-yl]oxymethyl]-5,9,13-trimethyl-2,10-dioxo-1-oxacyclohexadeca-11,13-dien-7-yl]acetaldehyde | 1405-54-5 | C50H83NO23 |
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| —— | 6,11,28-Trioxatricyclo[22.3.1.05,7]octacosa-8,14,16,18,20-pentaene-25-carboxylic acid,22-[(3-amino-3,6-dideoxy-b-D-mannopyranosyl)oxy]-1,3,26-trihydroxy-12-methyl-10-oxo-,(1R,3S,5R,7R,8E,12R,14E,16E,18E,20E,22R,24S,25R,26S)- | 7681-93-8 | C33H47O13N |
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| —— | (1S,5Z,7R,9S,11Z,13S,14S,16R,17S,18S,19S)-19-benzyl-7-hydroxy-7,9,16,17-tetramethyl-2,4,15-trioxa-20-azatetracyclo[11.8.0.01,18.014,16]henicosa-5,11-diene-3,8,21-trione | 36011-19-5 | C28H33NO7 |
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| —— | (2S,3'R,4S,4'S,5'R,6R,6'R,7S,7aS)-4-[(2S,3R,5S,6R)-3-amino-2,6-dihydroxy-5-(methylamino)cyclohexyl]oxy-6'-[(1R)-1-amino-2-hydroxyethyl]-6-(hydroxymethyl)spiro[4,6,7,7a-tetrahydro-3aH-[1,3]dioxolo[4,5-c]pyran-2,2'-oxane]-3',4',5',7-tetrol | 31282-04-9 | C20H37N3O13 |
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| —— | Thiostrepton 1 | 1393-48-2 | C72H85N19O18S5 |
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| —— | (2R,3R,6R,7S,8S,9R,10S,12R,13S,15R,17S)-9-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-3-ethyl-2,10-dihydroxy-7-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-15-(2-methoxyethoxymethyl)-2,6,8,10,12,17-hexamethyl-4,16-dioxa-14-azabicyclo[11.3.1]heptadecan-5-one | 62013-04-1 | C42H78N2O14 |
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| —— | Formacidine | 8025-81-8 | C43H74N2O14 |
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| —— | 5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid,7-[[2-(2-amino-4-thiazolyl)-4-carboxy-1-oxo-2-butenyl]amino]-8-oxo-,hydrate, [6R-[6a,7b(Z)]]- | 118081-34-8 | C15H16N4O7S2 |
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| —— | Natacyn (TN) | 7681-93-8 | C33H47NO13 |
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| —— | Disodium;7-[[2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(2-methyl-6-oxido-5-oxo-1,2,4-triazin-3-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | 74578-69-1 | C18H16N8Na2O7S3 |
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| —— | 7-[[2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-(6,7-dihydro-5H-cyclopenta[b]pyridin-1-ium-1-ylmethyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid;hydrogen sulfate | 98753-19-6 | C22H24N6O9S3 |
|
| —— | Rifomycin O | 14487-05-9 | C39H47NO14 |
|
| —— | 2-[[1-(2-Amino-1,3-thiazol-4-yl)-2-[[2-carboxy-8-oxo-3-(pyridin-1-ium-1-ylmethyl)-5-thia-1-azabicyclo[4.2.0]oct-2-en-7-yl]amino]-2-oxoethylidene]amino]oxy-2-methylpropanoate;pentahydrate | 78439-06-2 | C22H32N6O12S2 |
|
| —— | (E)-roxithromycin | 80214-83-1 | C41H76N2O15 |
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| —— | 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 |
|
| —— | Bacitracin A | 1405-87-4 | C66H103N17O16S |
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| —— | 7-Amino-3-(methoxymethyl)-3-cephem-4-carboxylic acid | 24701-69-7 | C9H12N2O4S |
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| —— | (4R,6S,8R,9Z,11E)-16-chloro-17,19-dihydroxy-4-methyl-3,7-dioxatricyclo[13.4.0.06,8]nonadeca-1(15),9,11,16,18-pentaene-2,13-dione | 12772-57-5 | C18H17ClO6 |
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| —— | pipemidic acid trihydrate | 72571-82-5 | C14H17N5O3*3H2O |
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| —— | 7β-[2-(2-amino-4-thiazoIyl)-2-(Z-hydroxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid | 91832-40-5 | C14H13N5O5S2 |
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| —— | 1ξ-oxo-6β-(2-phenyl-acetylamino)-1λ<sup>4</sup>-penicillanic acid 4-methoxy-benzyl ester | 30034-13-0 | C24H26N2O6S |
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| —— | diphenylmethyl 7-amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate | 36923-21-4 | C20H18N2O3S |
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| —— | (1R,2R,3E,7S,11E,13R,15S)-2,15-dihydroxy-7-methyl-6-oxabicyclo[11.3.0]hexadeca-3,11-dien-5-one | 20350-15-6 | C16H24O4 |
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