Phenolic compounds from <Emphasis Type="Italic">Ranunculus chinensis</Emphasis>

Ranunchinesin A, a new phenolic compound, and four known phenolic compounds were isolated from Ranunculus chinensis Bge. The structure of the new compound was elucidated by spectral methods.     

Synthesis,structural, spectral,computational, docking and biological activities of Schiff base (E)-4-bromo-2-hydroxybenzylidene) amino)-N-(pyrimidin-2-yl) benzenesulfonamide from 5-bromosalicylaldehyde and sulfadiazine

The newly synthesized, characterized, and theoretically investigated Schiff base compound (E)-4-bromo-2-hydroxybenzylidene) amino)-N-(pyrimidin-2-yl) benzenesulfonamide (5BRSDA). Sulfadiazine and 5-bromosalicylaldehyde Schiff-base were the building blocks for the new compound. We were surprised by the variety in the structure of the results. By employing density functional theory (DFT), researchers were able to analyze the new compound molecular properties, geometric optimization, vibrational, frontier molecular orbitals, and energy evaluation. In addition, disc well diffusion was used to test the compounds antibacterial and antifungal properties. As compared to free ligands, the compound had a more potent pathogenic effect on the tested microbes, according to the findings. An in-depth molecular docking study on 1NTA provided new information about the inhibitory effects it has on pathogenic microbes. When compared to a literature survey, comparative analysis revealed that the titled compound had higher antibacterial and antifungal activity.     

New aromatic annulation reaction via a C14 enaminone synthon: synthesis of ‘terpenoid-like chalcones’

Diverse functionalized synthons from a new enaminone are reported. These synthons were easily obtained in a one pot process starting from a compound derived from β-ionone. A new annulation reaction of this C-14 compound with several anions led to new ‘terpenoid-like’ chalcones.     

Cordycedipeptide A, a new cyclodipeptide from the culture liquid of Cordyceps sinensis (Berk.) Sacc

A new cyclodipeptide named as cordycedipeptide A, a new natural compound and two known compound were isolated from the culture liquid of Cordyceps sinensis (BERK.) SACC. Their structures were elucidated as 3-acetamino-6-isobutyl-2,5-dioxopiperazine (1), 3-isopropyl-6-isobutyl-2,5-dioxopiperazine (2) and 3,6-di(4-hydroxy)benzyl-2,5-dioxopiperazine (3) by 1D and 2D-NMR techniques. The cytotoxic assay showed compound 1 had the cytotoxic activities to L-929, A375, and Hela.     

Formation, isolation and characterization of an AB-biaryl atropisomer of oritavancin

Oritavancin is a semi-synthetic glycopeptide antibiotic which is structurally related to vancomycin. When oritavancin bisphosphate is dried in vacuo with heat, a new compound forms. This new compound is stable only in the solid state and reverts to oritavancin in solution. Highly enriched samples of this compound were obtained by preparative HPLC and the structure of this compound was elucidated by using one and two-dimensional (¹H and ¹³C) NMR spectroscopy in conjunction with computer-assisted molecular modeling. It has been determined that oritavancin adopts a conformation similar to that of vancomycin in solution, while the new compound is the unnatural R-AB-biaryl atropisomer of oritavancin. This is the first observation and isolation of an AB-biaryl atropisomer in an intact member of the vancomycin family of glycopeptide antibiotics.     

Chemical constituents from rauvolfia verticillata and bioactivities research

A new acridone alkaloid, named 9-hydroxynoracronycine (1), together with four known compounds, including coumarins, lignan, and indole alkaloid, was isolated and identified from the roots and rhizomes of Rauvolfia verticillata. The structure of the new compound was determined by spectroscopic means (UV, IR, MS, and NMR). The acridone alkaloid and coumarins were identified as new constituents of Rauvolfia genus. The cytotoxic activities of the new compound were tested against human breast cancer cell line MCF-7 and human promyelocytic leukemia HL-60. Results showed that compound 1 decreased MCF-7 cell proliferation in a statistically IC₅₀ significant manner at 102.8 μmol/L. In addition, compound 1 exhibited moderate small intestine smooth muscle relaxation.     

Exploiting the Evolutionary Relationship between Malarial Parasites and Plants To Develop New Herbicides

Herbicide resistance is driving a need to develop new herbicides. The evolutionary relationship between apicomplexan parasites, such as those causing malaria, and plants is close enough that many antimalarial drugs are herbicidal and so represent novel scaffolds for herbicide development. Using a compound library from the Medicines for Malaria Venture, the model plant Arabidopsis thaliana, and a physicochemical database of known herbicides, a compound was discovered that showed post‐emergence herbicidal activity equal to commercial herbicides. Using structure–activity analysis, important points for its potency were found. The compound was also tested and found to be active against common crop weeds. Physiological profiling suggested the compound was a photosystem II inhibitor, representing a new scaffold for herbicide development. Overall this approach demonstrates the viability of using antimalarial compounds as lead compounds for the development of much needed new herbicides.     

溶胶凝胶复合材料的研究及对生物酶的固定

研究了一种新型的氧化铝/聚乙二醇（Al2O3/PEG）溶胶凝胶复合材料,利用红外光谱、探针电镜对材料的性能进行了表征。试验结果表明：复合膜中含有大量的羟基和氢键,且两种组分形成互穿网络,该材料刚柔相济的特点使其适合于做生物传感器的固定化材料。PEG是极性高聚物,在溶胶凝胶的体系中,可以起到加速反应及防止膜开裂的作用。Al2O3/PEG复合材料对酶具有较好的生物相容性和较高的稳定性,将生物酶固定其中制备成的生物传感器具有良好的反应活性,同时,还证明了这种生物传感器具有稳定性和灵敏度高的特点。     

The isolation,characterization and synthesis of 10-ketotetracosyl arachidate from Ficus hispida

The bark of Ficus hispida, one component of a mixture used as a cancer-cure in Thailand, yielded a new and unusual compound when extracted with light petroleum. The structure of the new compound, 10-ketotetracosyl arachidate, was proven by degradation and synthesis. The lupeol acetate and β-sitosterol found in the light petroleum extract were identified by comparison with authentic samples.     

A new insecticidal protolimonoid from Aegle marmelos

Bioassay-directed fractionation of the ethyl acetate extracts of the stem bark of Aegle marmelos Correa (Rutaceae) afforded a new compound, named skimmiarepin C, along with skimmiarepin A. The latter is a known compound but isolation from A. marmelos is new. The new compound is a senecioate ester analogue of the latter. Full identification of the new compound was achieved using spectroscopic methods on the separated mono-acetate derivatives. Skimmiarepins A and C exhibit moderate insecticidal activity against Phaedon cochleariae and Musca domestica in comparison with natural pyrethrum extract. The two epimeric acetates of skimmiarepin C are both less active.     

New synthetic approaches to development of the chemistry of pentaerythritol bicyclophosphite

Syntheses of the original compact molecular systems were developed and the ways of their practical use were examined. A group of new substances was synthesized on the basis of available penta-erythritol bicyclophosphite and thionophosphate, including respective ammonium salts, phosphocholines, a complex compound of molybdenum, and a hydrophosphoryl compound.     

Isoflavone glycosides from the root wood of Erythrina latissima

The molecular structures of 3 isoflavone glycosides isolated from the root wood of Erythrina latissima were established as 4'-hydroxyisoflavone-7-O-beta-D-glucopyranoside (compound 1); 4'-hydroxyisoflavone-7-O-alpha-L-rhamnosyl (1-->6)-beta-D-glucopyranoside (compound 2); and a new compound 4', 8-dimethoxy isoflavone-7-O-alpha-L-rhamnosyl (1-->6) glucopyranoside (8-O-methylretusin-7-O-alpha-L-rhamnosyl (1-6)-beta-D-glucopyranoside) (compound 3).     

用二点滴定法测定化合物的组成比

本法只要测定三组E—V数据即可计算出化合物的组成比。     

Design and synthesis of 5-cyclopropyl substituted cyclic acylguanidine compounds as BACE1 inhibitors

By taking compound 1 as a lead, a series of 5-cyclopropyl substituted cyclic acylguanidine compounds were designed and synthesized as BACE1 inhibitors, compound 4d exhibited 84-fold improved inhibition efficiency than lead compound 1. The diphenyl fragment at the P3 position and the substituents at the second phenyl ring were essential for the compounds to achieve improved inhibition efficiency. This SAR studies provides new insights into the design and synthesis of more promising BACE1 inhibitors for the potential treatment of AD.     

2-(2-羟基-5-氯苯基)-1H-苯并咪唑-铜(Ⅱ)配合物作为NO荧光探针的初探

常温下合成了2-(2-羟基-5-氯苯基)-1H-苯并咪唑荧光化合物和其二价铜离子的配合物,并对配合物的结构和稳定性进行了表征,用荧光光谱、质谱、红外光谱等研究了配合物与NO反应的机理.结果表明,该配合物与NO的反应具有高度的选择性,不受其他常见干扰分子的影响.配合物应用于脂多糖(LPS)激活的小鼠巨噬细胞中NO的测定,能够得到具有较好分辨率的荧光成像结果.     

新型感绿菁染料的合成

报道了化合物5、季铵盐7和8及三种新型感绿染料(9a、9b、13)的合成方法。对合成的化合物的结构进行了表征。     

8-葵炔基苯并内酰胺-V8的改良合成

8-葵炔基苯并内酰胺-V8是我们最近发现的具有亚基选择性的PKC调节剂,动物实验表明有抗癌活性。本文探讨了一个对于这个化合物的新的合成路线。以4为原料,通过碘基化反应,成环反应,Pd/CuI催化的葵炔与芳基碘代物的偶联反应等关键步骤,以22.4%的收率得到了该化合物。     

Water-soluble constituents of dill

From the water-soluble portion of the methanol extract of dill (fruit of Anethum graveolens L.), which has been used as a spice and medicine, thirty-three compounds, including a new monoterpenoid, six new monoterpenoid glycosides, a new aromatic compound glucoside and a new alkyl glucoside were obtained. Their structures were clarified by spectral investigation.     

A new bromoallene-producing chemical type of the red alga Laurencia nangii masuda

Six populations of Laurencia nangii were found to produce three bromoallenes; dihydroitomanallene B (1), itomanallene B (2) and pannosallene (3). Prior to this report, L. nangii were only known to produce C(15)-acetogenins with acetylene functionality. This could be regarded as a new chemical race of L. nangii. The compound structures were elucidated on the basis of spectroscopic analysis and comparison with those previously reported in literature. Compound 1, dihydroitomanallene B, was isolated as a new compound representing a minor variation of itomanallene B (2).     

Synthesis and bio-evaluation of phenothiazine derivatives as new antituberculosis agents

Two series of phenothiazine derivatives were designed and synthesized. All compounds were tested for anti-tuberculosis activities against Mycobacterium tuberculosis H₃₇R_V. In comparison with mother compound of chlorpromazine, compound 6e shows promising anti-tuberculosis activity and much less mammalian cell cytotoxicity, compound 6e merits to be further explored as new anti-tuberculosis agents.