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    首页 分子通 按物质功能分类 原料药 人工合成抗感染类药 抗真菌类药

    抗真菌类药

    20世纪50年代起，陆续研发出了较为有效的抗真菌药物，如灰黄霉素。直到20世纪60年代，氟胞嘧啶被引入，其抗菌谱局限于念珠菌属和隐球菌，并仅用于与两性霉素B（AmB）联合治疗。

    进入新世纪后，唑类抗真菌药物的发展迎来了新纪元。这类药物减少了毒性，提高了抗真菌效力。第一个唑类药物是克霉唑，主要用于局部黏膜及皮肤念珠菌感染；第二个则是咪康唑，如今几乎仅用于局部治疗。直到20世纪70年代中期，酮康唑的研制成功标志着重要突破——口服对深部真菌感染有效，并且抗菌谱广、毒性有所减小，被视为抗真菌药物发展过程中的革命性进展。然而，由于重症患者无法口服吸收、中枢神经系统穿透力差及抗真菌活性不足等问题，酮康唑的临床应用受到了限制。

    20世纪80年代后期，伊曲康唑和氟康唑等新药的开发显著改善了抗菌谱和生物利用度，它们的出现标志着抗真菌治疗进入了一个崭新时代。尽管如此，没有一种药物能够实现绝对杀真菌的效果。近年来，耐药菌株日益增多，加之药物毒性反应的限制，使得真菌感染治疗面临诸多挑战。

    目前较有希望的药物包括抑制胞膜麦角固醇合成和干扰胞壁β-葡聚糖合成的药物，如氟康唑、伊曲康唑和睫状真菌素。此外，那些抗菌力强及毒性作用大的老药也在不断改进中。联合用药成为抗真菌治疗的方向之一。

    中文名称 英文名称 CAS号 化学式 结构式图片
    奥泽沙星 ozenoxacin 245765-41-7 C21H21N3O3
    奥泽沙星
    奥克太啶 N,N'-(1,10 decanediyldi-1[4H]-pyridinyl-4-ylidene)-bis-(1-octanamine) 71251-02-0 C36H62N4
    奥克太啶
    头孢磺啶钠 52152-93-9 C22H20N4NaO8S2
    头孢磺啶钠
    噻康唑 tioconazole 65899-73-2 C16H13Cl3N2OS
    噻康唑
    咪康唑 miconazole 22916-47-8 C18H14Cl4N2O
    咪康唑
    吖啶琐辛 Acrisorcin 7527-91-5 C12H18O2*C13H10N2
    吖啶琐辛
    卢立康唑 luliconazole 187164-19-8 C14H9Cl2N3S2
    卢立康唑
    利奈唑胺 linezolid 165800-03-3 C16H20FN3O4
    利奈唑胺
    伏立康唑 voriconazole 188416-29-7 C16H14F3N5O
    伏立康唑
    伊曲康唑-d5 Itraconazole-d5 (major) 84625-61-6 C35H38Cl2N8O4
    伊曲康唑-d5
    NSC 317629; 1-[4-[4-[[2-(2,4-二氯苯基)-2-(1H-咪唑-1-甲基)-1,3-二氧杂环戊-4-基]甲氧基]苯基]-1-哌嗪基]乙酮 ketokonazole 65277-42-1 C26H28Cl2N4O4
    NSC 317629; 1-[4-[4-[[2-(2,4-二氯苯基)-2-(1H-咪唑-1-甲基)-1,3-二氧杂环戊-4-基]甲氧基]苯基]-1-哌嗪基]乙酮
    L-肌肽锌 zinc carnosine 107667-60-7 C9H12N4O3Zn
    L-肌肽锌
    5-溴-5-硝基-1,3-二恶烷 bronidox 30007-47-7 C4H6BrNO4
    5-溴-5-硝基-1,3-二恶烷
    2-辛基-4-异噻唑啉-3-酮 2-octyl-isothiazol-3-one 26530-20-1 C11H19NOS
    2-辛基-4-异噻唑啉-3-酮
    2,3,6-三溴对甲酚 2,4,6-tribromo-m-cresol 4619-74-3 C7H5Br3O
    2,3,6-三溴对甲酚
    (Z)-2'-(1-咪唑基)-O-(2,4-二氯苄基)-2,4-二氯苯乙酮肟硝酸盐 Oxiconazole Nitrate 64211-46-7 C18H14Cl4N4O4
    (Z)-2'-(1-咪唑基)-O-(2,4-二氯苄基)-2,4-二氯苯乙酮肟硝酸盐
    (E)-1-(5-氯-2-噻吩基-2-(1H)-咪唑-1-基)乙酮(2,6-二氯苯基)腙盐酸盐 (E)-1-(5-chlorothien-2-yl)-2-(1H-imidazol-1-yl)ethanone 2,6-dichlorophenylhydrazone hydrochloride 80168-44-1 C15H11Cl3N4S*ClH
    (E)-1-(5-氯-2-噻吩基-2-(1H)-咪唑-1-基)乙酮(2,6-二氯苯基)腙盐酸盐
    —— Spectinomycin dihydrochloride pentahydrate 22189-32-8 C14H27ClN2O8
    Spectinomycin dihydrochloride pentahydrate
    —— 85960-17-4 C28H43N5NaO9S2
    —— Pharmakon1600-01500201 642-78-4 C19H18ClN3NaO5S+
    Pharmakon1600-01500201
    —— Phleomycin 11006-33-0 C51H75N17O21S2
    Phleomycin
    —— 1-(2,4-Dichloro-phenyl)-2-imidazol-1-yl-ethanone O-(2,4-dichloro-benzyl)-oxime; compound with nitric acid 64211-46-7 C18H13Cl4N3O*HNO3
    1-(2,4-Dichloro-phenyl)-2-imidazol-1-yl-ethanone O-(2,4-dichloro-benzyl)-oxime; compound with nitric acid
    —— Dihydrostreptomycin Sulfate 1425-61-2 C42H88N14O36S3
    Dihydrostreptomycin Sulfate
    —— Siccanin 22733-60-4 C22H30O3
    Siccanin
    —— decanoyl-Trp-D-Asn-Asp-Thr(1)-Gly-Orn-Asp-D-Ala-Asp-Gly-D-Ser-Glu(3S-Me)-Asp(Ph(2-NH2))-(1) 103060-53-3 C72H101N17O26
    decanoyl-Trp-D-Asn-Asp-Thr(1)-Gly-Orn-Asp-D-Ala-Asp-Gly-D-Ser-Glu(3S-Me)-Asp(Ph(2-NH2))-(1)
    —— (E)-1-(2,4-dichlorophenyl)-N-[(2,4-dichlorophenyl)methoxy]-2-imidazol-1-ylethanimine;nitric acid 64211-46-7 C18H14Cl4N4O4
    (E)-1-(2,4-dichlorophenyl)-N-[(2,4-dichlorophenyl)methoxy]-2-imidazol-1-ylethanimine;nitric acid
    —— 1-(2,4-dichlorophenyl)-N-[(2,4-dichlorophenyl)methoxy]-2-(1-imidazolyl)ethanimine 64211-46-7 C18H13Cl4N3O
    1-(2,4-dichlorophenyl)-N-[(2,4-dichlorophenyl)methoxy]-2-(1-imidazolyl)ethanimine
    —— Bafilomycin A 116764-51-3 C35H58O9
    Bafilomycin A
    —— Setamycin 88899-56-3 C44H65NO13
    Setamycin
    —— Cloxacillin(1-) 642-78-4 C19H17ClN3O5S-
    Cloxacillin(1-)
    —— Ketocanazole 65277-42-1 C26H28Cl2N4O4
    Ketocanazole
    —— (1S,4S,13S,16S,19R,22S,25S,28R,31S,37S,40R,41R,44R,47S,50S,53R,56R,65S,70R)-44-amino-47-(4-aminobutyl)-37-(2-amino-2-oxoethyl)-50-(3-amino-3-oxopropyl)-4,16,22-tribenzyl-31-[(R)-carboxy(hydroxy)methyl]-41,70-dimethyl-2,5,8,14,17,20,23,26,29,32,35,38,45,48,51,54,57,67-octadecaoxo-25-propan-2-yl-42,69,72-trithia-3,6,9,15,18,21,24,27,30,33,36,39,46,49,52,55,58,60,66-nonadecazapentacyclo[38.18.9.319,56.328,53.09,13]triheptacontane-65-carboxylic acid 1391-36-2 C89H125N23O25S3
    (1S,4S,13S,16S,19R,22S,25S,28R,31S,37S,40R,41R,44R,47S,50S,53R,56R,65S,70R)-44-amino-47-(4-aminobutyl)-37-(2-amino-2-oxoethyl)-50-(3-amino-3-oxopropyl)-4,16,22-tribenzyl-31-[(R)-carboxy(hydroxy)methyl]-41,70-dimethyl-2,5,8,14,17,20,23,26,29,32,35,38,45,48,51,54,57,67-octadecaoxo-25-propan-2-yl-42,69,72-trithia-3,6,9,15,18,21,24,27,30,33,36,39,46,49,52,55,58,60,66-nonadecazapentacyclo[38.18.9.319,56.328,53.09,13]triheptacontane-65-carboxylic acid
    —— Cefsulodin sodium salt hydrate, third-generation cephalosporin antibiotic 52152-93-9 C22H21N4NaO8S2+
    Cefsulodin sodium salt hydrate, third-generation cephalosporin antibiotic
    —— (2R)-2-[[(2S)-5-(diaminomethylideneamino)-1-[[(2R)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]carbamoylamino]-3-phenylpropanoic acid 37691-11-5 C27H44N10O6
    (2R)-2-[[(2S)-5-(diaminomethylideneamino)-1-[[(2R)-1-[[(2S)-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]carbamoylamino]-3-phenylpropanoic acid
    —— decanoyl-Trp-D-Asn-Asp-Thr(1)-Gly-D-Orn-Asp-Ala-Asp-Gly-D-Ser-Glu(3S-Me)-Asp(Ph(2-NH2))-(1) 103060-53-3 C72H101N17O26
    decanoyl-Trp-D-Asn-Asp-Thr(1)-Gly-D-Orn-Asp-Ala-Asp-Gly-D-Ser-Glu(3S-Me)-Asp(Ph(2-NH2))-(1)
    —— (3E,5E,7R,8S,9S,11E,13E,15S,16R)-16-[(2S,3R,4S)-4-[(2R,4R,5S,6R)-2,4-dihydroxy-5-methyl-6-propan-2-yloxan-2-yl]-3-hydroxypentan-2-yl]-8-hydroxy-3,15-dimethoxy-5,7,9,11-tetramethyl-1-oxacyclohexadeca-3,5,11,13-tetraen-2-one 88899-55-2 C35H58O9
    (3E,5E,7R,8S,9S,11E,13E,15S,16R)-16-[(2S,3R,4S)-4-[(2R,4R,5S,6R)-2,4-dihydroxy-5-methyl-6-propan-2-yloxan-2-yl]-3-hydroxypentan-2-yl]-8-hydroxy-3,15-dimethoxy-5,7,9,11-tetramethyl-1-oxacyclohexadeca-3,5,11,13-tetraen-2-one
    —— Pharmakon1600-01502029 52152-93-9 C22H20N4NaO8S2+
    Pharmakon1600-01502029
    —— Oxytetracycline dihydrate 6153-64-6 C22H28N2O11
    Oxytetracycline dihydrate
    —— Daptomycin (LY146032) 103060-53-3 C72H101N17O26
    Daptomycin (LY146032)
    —— (3S)-2-(2,4-Difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol 137234-62-9 C16H14F3N5O
    (3S)-2-(2,4-Difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol
    —— Bafilomycin B1 88899-56-3 C44H65NO13
    Bafilomycin B1
    —— decanoyl-Trp-Asn-Asp-DL-xiThr(1)-Gly-D-Orn-Asp-D-Ala-Asp-Gly-Ser-Glu(3-Me)-Asp(Ph(2-NH2))-(1) 103060-53-3 C72H101N17O26
    decanoyl-Trp-Asn-Asp-DL-xiThr(1)-Gly-D-Orn-Asp-D-Ala-Asp-Gly-Ser-Glu(3-Me)-Asp(Ph(2-NH2))-(1)
    —— Ionomycin 56092-81-0 C41H72O9
    Ionomycin
    —— decanoyl-Trp-Asn-Asp-Thr(1)-Gly-Orn-Asp-D-Ala-Asp-Gly-D-Ser-Glu(3S-Me)-Asp(Ph(2-NH2))-(1) 103060-53-3 C72H101N17O26
    decanoyl-Trp-Asn-Asp-Thr(1)-Gly-Orn-Asp-D-Ala-Asp-Gly-D-Ser-Glu(3S-Me)-Asp(Ph(2-NH2))-(1)
    —— cis-2,6-dimethyl-4-((S)-2-methyl-3-(4-(tert-pentyl)phenyl)propyl)morpholine 78613-35-1 C21H35NO
    cis-2,6-dimethyl-4-((S)-2-methyl-3-(4-(tert-pentyl)phenyl)propyl)morpholine
    —— sulfaquinoxaline sodium salt 967-80-6 C14H11N4O2S*Na
    sulfaquinoxaline sodium salt
    —— decanoyl-Trp-Asn-Asp-DL-Thr(1)-Gly-Orn-Asp-D-Ala-DL-Asp-Gly-D-Ser-Glu(3R-Me)-DL-Asp(Ph(2-NH2))-(1) 103060-53-3 C72H101N17O26
    decanoyl-Trp-Asn-Asp-DL-Thr(1)-Gly-Orn-Asp-D-Ala-DL-Asp-Gly-D-Ser-Glu(3R-Me)-DL-Asp(Ph(2-NH2))-(1)
    —— 1-[4-[4-[[(2S)-2-(2,4-Dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone 65277-42-1 C26H28Cl2N4O4
    1-[4-[4-[[(2S)-2-(2,4-Dichlorophenyl)-2-(imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]ethanone
    —— (Z)-Lanoconazole 101530-10-3 C14H10ClN3S2
    (Z)-Lanoconazole
    —— Imipenem-cilastatin sodium 85960-17-4 C28H42N5NaO9S2
    Imipenem-cilastatin sodium