3-取代吲哚衍生物的合成(Ⅰ)

基于吲哚衍生物和氮杂环衍生物的抗真菌活性,设计合成了含有噻二唑、三氮唑、二唑等氮杂环及其相应开链硫脲结构的吲哚衍生物和吲哚希夫碱化合物共18个,除化合物2、3和16外其余目标物未见报道,其结构经     

Novel 5-HT3 antagonists. Indole oxadiazoles

The synthesis and biochemical evaluation of a series of indole oxadiazole 5-HT3 antagonists are described. The key pharmacophoric elements have been defined as a basic nitrogen, a linking group capable of H-bonding interactions, and an aromatic moiety. The steric limitations of the aromatic binding site have been determined by substitution about the indole ring. Variation of the heterocyclic linking group has shown that while two hydrogen-bonding interactions are possible, only one is essential for high affinity. The environment of the basic nitrogen has been investigated and shown to be optimal when constrained within an azabicyclic system. These results have been incorporated into a proposed binding model for the 5-HT3 antagonist binding site, in which the optimum distance between the aromatic binding site and the basic amine is 8.4-8.9 A and the steric limitations are defined by van der Waals difference mapping.     

Cytotoxic Activity of Some Indole Derivatives and Indole Metabolites of Streptomyces staurosporeus

The cytotoxic potential and structure activity relationships of several indole metabolites obtained from feeding experiments using Streptomyces staurosporeus, a staurosporine producer, are described. 6-Fluoro-tryptamine and N b -acetyl-tryptamine-5- O -a-L-rhamnopyranoside, a metabolite obtained from the feeding experiment, demonstrated greatest activity with KB cells in culture, by means of an unknown mechanism.     

Preparation of Carbamoyl Derivatives of Indole and of Derivatives of 1,2,4-Triazol-3-one from Semicarbazides

A simple and one-step method for the preparation of the title compounds is described. Semicarbazides 2 react easily with levulinic acid in the presence of HCl to give 4 , whereas in a alkaline medium they cyclize to form the triazole derivatives 3 .     

Indole alkaloids of Odyendea gabonensis

From the trunk bark of Odyendea gabonensis six indole alkaloids have been isolated: Canthin-6-one (I); 5-Methoxy-canthin-6-one (II); 4,5-Dimethoxycanthin-6-one (III); 8-Hydroxy-canthin-6-one (IV); 1-Hydroxy-methyl-beta-carboline (V); and 1-Carboxamide-beta-carboline (VI). This is the first report of these products from this plant.     

以L-半胱氨酸和吲哚酶法合成L-色氨酸

用色氨酸酶基因工程菌ＷＷ－４催化Ｌ－半胱氨酸和吲哚合成Ｌ－色氨酸。８０ｍｌ反应液（Ｌ－半胱氨酸０．７５ｇ，吲哚０．７５ｇ）３７℃反应４８ｈ，可积累Ｌ－色氨酸１．１８ｇ。Ｌ－半胱氨酸转化率为９３．２％，吲哚转化率为９０．１％。产品总回收率达７０％，所得晶体在熔点、旋光性和红外吸收光谱等方面与标准品完全一致。     

以L-半胱氨酸和吲哚为底物酶法合成L-色氨酸(英文)

以Ｌ－半胱氨酸和吲哚为底物,利用色氨酸酶基因工程菌ＷＷ－１１酶法合成Ｌ－色氨酸。方法：以ＩＰＴＧ诱导基因工程菌色氨酸酶表达,将酶活最高时的工程菌游离细胞作为转化反应的酶源,通过纸层析和氨基酸自动分析仪分析并测定转化液中Ｌ－色氨酸的含量。结果：８０ｍＬ反应液（Ｌ－半胱氨酸０.７５ｇ,吲哚０.７５ｇ）３７℃反应４８ｈ,可积累Ｌ－色氨酸１.１８ｇ,Ｌ－半胱氨酸转化率为９３．２％,吲哚转化率为９０.１％。经分离纯化所得的Ｌ-色氨酸晶体,在熔点、旋光性和红外吸收光谱等方面与标准品完全一致。结论：色氨酸酶基因工程菌能有效地催化Ｌ－半胱氨酸和吲哚合成Ｌ－色氨酸,这种酶合成法是工业化生产Ｌ－色氨酸较为有效的方法之一。     

Indole Mannich bases and their antimycobacterial effect

3-[(4-arylpiperazin-1-yl)methyl]lindoles (2a-h) and 3-[(4-hydroxy-4-phenylpiperazin-1-yl)methyl]indole (3) were prepared and characterized by 1H NMR and mass spectrometry. All eight compounds (2a-c, e-h and 3) tested inhibited in vitro the growth of Mycobacterium tuberculosis H37Rv in the range of 98-7% at a concentration of > or = 6.25 microg/ml. From the preliminary microbiological data it is possible to observe that a simple increasing of lipophilicity of the compounds tested to above logPcalc> or =3.8 significantly increases the potencies of their antitubercular action.     

以L—半胱氨酸和吲哚为底物酶合成L—色氨酸

目的：以L－半胱氨酸和吲哚为底物,利用色氨酸酶基因工程菌WW－11酶法合成L－色氨酸。方法：以IPTG诱导基因工程菌色氨酸酶表达,将酶活最高时的工程菌游离细胞作为转化反应的酶源,通过纸层析和氨基酸自动分析仪分析并测定转化液中L－色氨酸的含量,结果：80mL反应液（L－半胱氨酸0．75g,吲哚75g)37℃反应48h,可积累L－色氨酸1．18g,L-半腕氨酸转化率为93．2％,吲哚转化率为90．1％,经分离纯化所得的L－色氨酸晶体,在熔点,旋光性和红外吸收光谱等方面与标准品完全一致,结论：色氨酸酶基因工程菌能有效地催化L－半胱氨酸和吲哚合成L－色氨酸,这种酶合成法是工业化生产L－色氨酸较为有效的方法之一。     

Indole Alkaloids of Odyendea gabonensis.]

From the trunk bark of ODYENDEA GABONENSIS six indole alkaloids have been isolated: Canthin-6-one (I); 5-Methoxy-canthin-6-one (II); 4,5-Dimethoxycanthin-6-one (III); 8-Hydroxy-canthin-6-one (IV); 1-Hydroxy-methyl-beta-carboline (V); and 1-Carboxamide-beta-carboline (VI). This is the first report of these products from this plant.     

Indole alkaloid glucosides from the roots of Isatis indigotica

Five new indole alkaloid glucosides named isatindigotindolosides A-E (1–5), along with three known analogs (6–8), were isolated from an aqueous extract of the Isatis indigotica roots. Their structures including the absolute configurations were determined based on comprehensive spectroscopic data analysis, combined with chemical methods and electronic circular dichroism spectra calculations. In the preliminary assays, compounds 1, 6 and 7 showed antiviral activity against influenza virus A/Hanfang/359/95 (H3N2) with IC₅₀ values of 14.6–33.3 μM. Compound 1 also exhibited inhibitory effect against nitric oxide (NO) production in microglial cell BV2 with an inhibition ratio of 93.0% at 10 μM.     

Quaternary Indole Alkaloids of Strychnos decussata.

A new muscle-relaxant alkaloid named malindine has been isolated from the stem bark of STRYCHNOS DECUSSATA, along with the previously known alkaloids macusine B, O-methylmacusine B and an alkaloid of macusine A or C-type. The structure of malindine is proposed on the basis of spectral data and its pharmacological activity is discussed.     

Tertiary Indole Alkaloids of Tabernaemontana dichotoma Seeds

From the seeds of TABERNAEMONTANA DICHOTOMA, the alkaloids coronaridine, ibogamine, stemmadenine, tabersonine, voacangine, voaphylline and voaphylline hydroxyindolenine were isolated and identified. The crude seed extract showed spasmolytic activity.