Cilofungin, L-646991, LY-121019
西洛芬净Chemical Name: N-[9beta-[1alpha,2beta-Dihydroxy-2-(4-hydroxyphenyl)ethyl]tetracosahydro-1alpha,13alpha,22alpha,23alpha-tetrahydroxy-6beta,17beta-bis(1beta-hydroxyethyl)-2alpha-methyl-5,8,11,16,19,25-hexaoxo-5H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacycloheneicosin-20beta-yl]-4-(octyloxy)benzamide; 1-[(4R,5R)-4,5-Dihydroxy-N2-[p-(octyloxy)benzoyl]-L-ornithine]echinocandin B; (4R,5R)-4,5-Dihydroxy-N2-[p-(octyloxy)benzoyl]-L-ornithyl-L-threonyl-trans-4-hydroxy-L-prolyl-(S)-4-hydroxy-4-(p-hydroxyphenyl)-L-threonyl-L-threonyl-(3S,4S)-3-hydroxy-4-methyl-L-proline cyclic (6--1)-peptide
CAS No. 79404-91-4
项目整合开发状态: Phase II
项目研究机构: Lilly (Originator)
合成路线:Cilofungin is a semi-synthetic anti-Candida agent that is derived from a three-step process:a) fermentation,isolation and purification of echinocandin B (ECB) (I) using an Aspergillus nidulans strain as the producing culture;b) deacylation of ECB by fermentation using an Actinoplanes utahensis culture to give the ECB nucleus (II); and c) N-acylation of the amino terminus of (II) using an activated ester of 4-octyloxybenzoic acid to give cilofungin.
📌 参考资料/链接：
参考文献标题:Echinocandin B.Ein Neuartiges Polypeptide-antibioticum aus Aspergillus nidulans var echinulatus: Isoleirung and Bausteine
文献作者:Benz,F.; Knusel,F.; Nuesch,J.; Trechler,H.; Voser,W.; Nefeler,R.; Keller-Schierlein,W.
参考来源:Helv Chim Acta 1974,572459
📄 详细内容
合成路线:Cilofungin is a semi-synthetic anti-Candida agent that is derived from a three-step process:a) fermentation,isolation and purification of echinocandin B (ECB) (I) using an Aspergillus nidulans strain as the producing culture;b) deacylation of ECB by fermentation using an Actinoplanes utahensis culture to give the ECB nucleus (II); and c) N-acylation of the amino terminus of (II) using an activated ester of 4-octyloxybenzoic acid to give cilofungin.
参考文献标题:Synthesis of new analogs of echinocandin B by enzymatic deacylation and chemical reacylation of the echinocandin peptide: Synthesis of the antifungal agent cilofungin (LY-121019)
文献作者:Debono,M.; Abbott,B.J.; Fukuda,D.S.; Barnhart,M.; Willard,K.E.; Molloy,R.M.; Michel,K.H.; Turner,J.R.; Butler,T.F.; Hunt,A.H.
参考来源:J Antibiot 1989,42389
合成路线:Cilofungin is a semi-synthetic anti-Candida agent that is derived from a three-step process:a) fermentation,isolation and purification of echinocandin B (ECB) (I) using an Aspergillus nidulans strain as the producing culture;b) deacylation of ECB by fermentation using an Actinoplanes utahensis culture to give the ECB nucleus (II); and c) N-acylation of the amino terminus of (II) using an activated ester of 4-octyloxybenzoic acid to give cilofungin.
参考文献标题:Synthesis and evaluation of LY-121019,a member of a series of semisynthetic analogues of the antifungal lipopeptide echinocandin B
文献作者:Debono,M.; Abbott,B.J.; Turner,J.R.; Howard,L.C.; Gordee,R.S.; Hunt,A.H.; Barnhart,M.; Molloy,R.M.; Willard,K.E.; Fukuda,D.S.; Butler,T.F.; Zeckner,D.J.
参考来源:Ann NY Acad Sci 1988,152
合成路线:Cilofungin is a semi-synthetic anti-Candida agent that is derived from a three-step process:a) fermentation,isolation and purification of echinocandin B (ECB) (I) using an Aspergillus nidulans strain as the producing culture;b) deacylation of ECB by fermentation using an Actinoplanes utahensis culture to give the ECB nucleus (II); and c) N-acylation of the amino terminus of (II) using an activated ester of 4-octyloxybenzoic acid to give cilofungin.
参考文献标题:CILOFUNGIN < Prop INN; USAN >
文献作者:Gordee,R.; Debono,M.
参考来源:Drugs Fut 1989,14(10),939
产品链接: CAS No. 79404-91-4››