- Overcoming AlbD Protease Resistance and Improving Potency: Synthesis and Bioactivity of Antibacterial Albicidin Analogues with Amide Bond Isosteres
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Albicidin is a potent antibacterial oligoaromatic peptide that is susceptible to the protease AlbD, a resistance factor. This potentially restricts the use of albicidin as a drug. To overcome this obstacle, we synthesized and evaluated six analogues with
- Kleebauer, Leonardo,Zborovsky, Lieby,Hommernick, Kay,Seidel, Maria,Weston, John B.,Süssmuth, Roderich D.
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supporting information
p. 7023 - 7027
(2021/09/08)
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- Boron Containing PDE4 Inhibitors
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The present invention relates to boron containing compounds of Formula (I) [in-line-formulae]X—Y—Z?? Formula (I)[/in-line-formulae] that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
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Paragraph 0635-0636
(2020/04/29)
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- The first total synthesis of (±)-methyl salvianolate A using a convergent strategy
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Herein, a convergent, practicable and first total synthesis of the natural product, (±)-methyl salvianolate A, is reported. The key features of the approach are the use of a Horner–Wadsworth–Emmons reaction and the protection of multiple hydroxyls using s
- Wang, Bo,Wang, Liping,Peng, Ying,Pang, Yiying,Xiao, Hesheng,Wang, Xiaoji,Huang, Shuangping
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- COMPOUNDS FOR TREATMENT OF CARDIAC ARRHYTHMIAS AND HEART FAILURE
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This disclosure concerns compounds and a method for modulating the activity of calcium ion channels, including Ca2+-induced (or Ca2+-activated) calcium release channels and conformationally coupled calcium release channels such as ryanodine receptors. Some of the compounds have a structure according to formula I, or a stereoisomer, tautomer, hydrate, solvate, prodrug, or pharmaceutically acceptable salt thereof.
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Page/Page column 55
(2019/10/19)
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- Salvianolic acid A intermediate and preparation method thereof
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The invention relates to a medicine salvianolic acid A intermediate used for treating angina and acute myocardial infarction, i.e., a new synthesis method for trans-3-bromo-2-(3,4-di-substituted styryl)-6-substituted phenol. The method comprises the follo
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Paragraph 0038; 0039
(2018/09/08)
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- Fibrauretine synthetic method (by machine translation)
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The invention relates to O-vanillin (11) as the starting material, by the acylation reaction generating 2 - acetoxy - 3 - methoxybenzaldehyde (12), by the bromo, hydrolysis reaction to produce the 2 - hydroxy - 6 - bromo - 3 - methoxybenzaldehyde (13), produced by the methylation reaction 6 - bromo - 2, 3 - dimethoxy benzaldehyde (14), produced by the condensation reaction of 2 - (6 - bromo - 2, 3 - dimethoxyphenyl) - 1, 3 - dioxolane (15); and then to 3, 4 - dimethoxy acetic acid (21) as raw materials, generated by the reduction reaction of the 3, 4 - dimethoxy ethanol (22), the acylation reaction generated by 3, 4 - dimethoxy new valeric acid environmentally (23), the acylation reaction is generated by the 2 - ethoxy - 3, 4 - dimethoxy new valeric acid environmentally (24), intermediate (15) and (24) after coupling, cyclized two-step reaction process for preparing the target product fibrauretin. (by machine translation)
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Paragraph 0042; 0043; 0061
(2018/09/21)
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- Synthesis of (+)-salvianolic acid A from sodium Danshensu
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(+)-Salvianolic acid A, one of the most active components in the traditional Chinese medicine Danshen, has been synthesized over 10 steps in 6.5% overall yield. Starting from inexpensive ortho-vanillin and sodium Danshensu (synthesized via asymmetric catalysis in our group), the process consists of the following: A Wittig reaction that gives the desire product with absolute E-configuration, a demethylation reaction with AlCl3 in a satisfactory yield, and a practical deprotection of allylic groups to afford the terminal product (+)-salvianolic acid A. The current synthetic technology possesses the advantages of using inexpensive starting materials, mild reaction conditions and has the potential for use in large scale synthesis.
- Xu, Kai,Liu, Hao,Liu, Delong,Sheng, Cheng,Shen, Jiefeng,Zhang, Wanbin
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p. 5996 - 6002
(2018/09/06)
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- Synthesis of SMND-309, a derivate of salvianolic acid B
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(E)-2-(6-((E)-2-carboxyvinyl)-2,3-dihydroxyphenyl)-3-(3,4-dihydroxyphenyl) acrylic acid, designated SMND-309, was synthesized starting from 2-hydroxy-3-methoxybenzaldehyde in 12 steps and with an overall yield of 44%. The synthetic key features were the c
- Wu, Kong,Song, Chan,Cui, Dong-Mei,Zhang, Chen
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supporting information
p. 1387 - 1391
(2017/07/25)
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- Method for synthesizing natural product salvianolic acid A methyl ester
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The invention relates to a novel method for synthesizing natural product salvianolic acid A methyl ester. A synthetic route is unique and novel in design; key strategies and steps comprise the step of using an easily-removed t-butyldimethylsilyl protectin
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Paragraph 0079; 0080; 0081; 0082
(2017/07/20)
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- New synthesis method of natural product Salvianolic Acid F
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The invention discloses a new synthesis method of a natural product Salvianolic Acid F. The method comprises the following steps: carrying out hydroxyl group protection on 4-methycatechol used as a raw material, carrying out a methyl radical reaction, and
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Paragraph 0014; 0031; 0032; 0033
(2018/01/04)
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- NOVEL CYSTOBACTAMIDES
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The present invention provides cystobactamides of formula (I) and the use thereof the treatment or prophylaxis of bacterial infections.
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Page/Page column 55
(2016/06/14)
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- CYSTOBACTAMIDES
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The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections:
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Paragraph 0548; 0575; 0576; 0577
(2016/06/13)
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- Synthesis and biological evaluation of cystobactamid 507: A bacterial topoisomerase inhibitor from Cystobacter sp.
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Abstract The first total synthesis of cystobactamid 507, a member of a class of new natural products with strong inhibitory activity towards bacterial topoisomerases, is reported. Synthetic key challenges are the central tetrasubstitued arene and the low chemical reactivity of anilines and ortho-phenolic and isopropoxy-substituted benzoic acids. Biological evaluations demonstrate that cystobactamid 507 inhibits several Gram-positive pathogens but at significantly lower concentrations than described for the larger members of this natural product family.
- Moreno, María,Elgaher, Walid A.M.,Herrmann, Jennifer,Schl?ger, Nadin,Hamed, Mostafa M.,Baumann, Sascha,Müller, Rolf,Hartmann, Rolf W.,Kirschning, Andreas
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supporting information
p. 1175 - 1178
(2015/06/02)
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- Total Synthesis and Antimicrobial Activity of Chlorocatechelin A
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Chlorocatechelin A (1) is a structurally unique microbial siderophore containing two units of 4-chloro-2,3-dihydroxybenzoic acid (CDB) and a characteristic acylguanidine structure. Purification from the microbe culture is not an easy task due to the labil
- Kishimoto, Shinji,Nishimura, Shinichi,Hatano, Masaki,Igarashi, Masayuki,Kakeya, Hideaki
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p. 6076 - 6082
(2015/06/30)
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- NOVEL BIOACTIVE SUBSTANCE
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PROBLEM TO BE SOLVED: To provide a novel compound useful as an aminopeptidase A inhibitor. SOLUTION: This invention provides a compound represented by formula (I) or salt thereof, and a pharmaceutical composition comprising the same, wherein R1
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Paragraph 0074-0075
(2018/02/08)
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- Copper(I)-catalyzed hydroalkoxylation/hydrogen-bonding-induced asymmetric hetero-diels-alder cycloaddition cascade: An approach to aromatic spiroketals
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One thing leads to another: Bis(benzannelated) 5,6-spiroketal skeletons can be constructed by an efficient cascade process involving an unprecedented CuI-catalyzed intramolecular alkyne hydroalkoxylation and an asymmetric hetero-Diels-Alder cyc
- Li, Xin,Xue, Jijun,Huang, Chusheng,Li, Ying
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supporting information; experimental part
p. 903 - 906
(2012/07/03)
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- NOVEL INHIBITORS OF HEPATITIS C VIRUS REPLICATION
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The embodiments provide compounds of the general Formulae I, II, III, IV, or V as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
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Page/Page column 131-132
(2011/07/06)
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- Synthesis and biological activities of novel furo[2,3,4-jk][2]benzazepin- 4(3H)-one derivatives
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A novel seven-membered lactam formation method has been established by intramolecular ring closure reaction of 4-bromo-(E)-3-[(2-alkylvinyl) carbonylamino]benzo[b]furans (17) under Heck coupling conditions. A number of furo[2,3,4-jk][2]benzazepin-4(3H)-on
- Ando, Kumiko,Akai, Yukiko,Kunitomo, Jun-Ichi,Yokomizo, Takehiko,Nakajima, Hidemitsu,Takeuchi, Tadayoshi,Yamashita, Masayuki,Ohta, Shunsaku,Ohishi, Takahiro,Ohishi, Yoshitaka
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p. 655 - 663
(2008/03/14)
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- Combretastatin analogs with tubulin binding activity
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Analogs of combretastatin have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.
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- Hydroxyphenstatin and the prodrugs thereof
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The benzophenone derivative of combretastatin A-1, designated “hydroxyphenstatin”, was synthesized by compiling a protected bromobenzene and a benzaldehyde to form a benzhydrol which was subsequently oxidized to the ketone. Hydroxyphenstatin was converted
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- A stereoselective intramolecular Diels-Alder strategy for the tricyclo[9.3.1.03,8]pentadecane core of aromatic C-ring taxanes
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A stereoselective Lewis acid-catalyzed and chelation controlled intramolecular Diels-Alder entry into the tricyclo[9.3.1.03,8]pentadecane core of aromatic C-ring taxanes is described. The approach affords an efficient, high yield, access to aromatic C-ring taxanes variably functionalized at the C2, C4, C5, and C9 positions.
- Smil, David V.,Laurent, Alain,Spassova, Nidejda S.,Fallis, Alex G.
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p. 5129 - 5132
(2007/10/03)
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- Convenient synthesis of a simple coumarin from salicylaldehyde and wittig reagent. IV: Improved synthetic method of substituted coumarins
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The reaction of salicylaldehydes (2) with Horner-Wadsworth-Emmons (HWE) or Ando-HWE reagents was attempted to afford intramolecular phosphonate derivatives (6). A new synthetic method for coumarins (1) was achieved by using protected 2.
- Takeuchi, Yasuo,Ueda, Norihiro,Uesugi, Koji,Abe, Hitoshi,Nishioka, Hiromi,Harayama, Takashi
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p. 217 - 224
(2007/10/03)
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- Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug
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A structure - activity relationship (SAR) study of the South African willow tree (Combretum caffrum) antineoplastic constituent combretastatin A-4 (3b) led to the discovery of a potent cancer cell growth inhibitor designated phenstatin (5a). This benzophenone derivative of combretastatin A-4 showed remarkable antineoplastic activity, and the benzophenone derivative of combretastatin A-1 was therefore synthesized. The benzophenone, designated hydroxyphenstatin (6a), was synthesized by coupling of a protected bromobenzene and a benzaldehyde to give the benzhydrol with subsequent oxidation to the ketone. Hydroxyphenstatin was converted to the sodium phosphate prodrug (6e) by a dibenzyl phosphite phosphorylation and subsequent benzyl cleavage (6a → 6d → 6e). While hydroxyphenstatin (6a) was a potent inhibitor of tubulin polymerization with activity comparable to that of combretastatin A-1 (3a), the phosphorylated derivative (6e) was inactive.
- Pettit, George R.,Grealish, Matthew P.,Herald, Delbert L.,Boyd, Michael R.,Hamel, Ernest,Pettit, Robin K.
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p. 2731 - 2737
(2007/10/03)
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- Synthesis of Halodimethoxy-1,2-benzoquinones
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Syntheses of a large number of halodimethoxy-1,2-benzoquinones are described.A key reaction in these syntheses is the chlorination of methoxy-1,2-benzoquinones upon treatment with tert-butyl hypochlorite.
- Wriede, Ulrich,Fernandez, Mario,West, Kevin F.,Harcourt, Dale,Moore, Harold W.
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p. 4485 - 4489
(2007/10/02)
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