Crystal Structures of Schiff Base from 4-Aminoantipyrine and Pyridine-2-carboxaldehyde and Its Perchlorate

The Schiff base pyridine-2-carboxaldehyde-4-aminoantipyrine （CI7H16N4O 1） and its perchlorate （C17H17N4O·ClO4 2） have been prepared and characterized by elemental analysis, IR spectra and single-crystal X-ray crystallography analysis. Both 1 and 2 crystallize in the monoclinic system, space group P21/c. For 1, a = 8.6820（12）, b = 24.934（3）, c = 7.0064（10） A,, β= 97.942（3）°, V = 1502.2（4） A^3, Z = 4, Dc = 1.293 g/cm^3, F（000） = 616,μ = 0.084 mm^-1, the final R = 0.0592 and wR = 0.1244. For 2, a = 5.9302（2）, b = 20.347（7）, c = 14.663（6） A, β= 90.200（9）°, V= 1769.201） A^3, Z = 4, Dc = 1.475 g/cm^3, F（000） = 816, μ = 0.254 mm^-1, the final R = 0.0533 and wR = 0.0819. As expected, both molecular structures of 1 and 2 adopt a trans configuration about the central C=N double bond. 2 is an ionic compound with the protonation at N（1） of pyridine-2-carboxaldehyde-4- aminoantipyrine.

链霉菌Streptomyces sp.294的化学成分研究

采用硅胶、凝胶柱色谱及制备薄层色谱从链霉菌Streptomyces sp.294发酵液的乙酸乙酯萃取物中分离纯化得到6个化合物,经核磁共振波谱及质谱鉴定其为indole-2-methylcarboxylate(Ⅰ)、spirotryprostatin A(Ⅱ)、cyclotryprostatin A(Ⅲ)、cyclotryprostatin B(Ⅳ)、fumitremorgin C(Ⅴ)和1,2-benzenedicarboxylic acid bis(2α-methyl heptyl)ester(Ⅵ)。其中化合物indole-2-methylcarboxylate(Ⅰ)对南方根结线虫(Meloidogyne incognita)具有微弱的毒杀活性。

5-Alkylpyrrole-2-carboxaldehyde derivatives from the Chinese sponge Mycale lissochela and their PTP1B inhibitory activities

Two new 5-alkylpyrrole-2-carboxaldehyde derivatives,mycalenitrile-15（1） and mycalenitrile-16（2）,along with five known related ones（3-7）,were isolated from the South China Sea sponge Mycale lissochela.The structures of the new compounds were elucidated on the basis of extensive spectroscopic analysis and by comparison of their NMR data with those reported in the literature.In bioassay,compounds 1 and 7 exhibited significant PTPIB（Protein-tyrosine phosphatase 1B,a recognized target for diabetes and obesity） inhibitory activities with IC（50） values of 8.6 and 3.1 μmoI/L,respectively.A preliminary SAR analysis of the isolated compounds with their PTP1 B inhibitory effects was described.

Synthesis and antiviral activity of some novel indole-2-carboxylate derivatives

A series of novel indole-2-carboxylate derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities.The biological results showed that some of the synthesized compounds exhibited potent broad-spectrum antiviral activity.Notably,compound 8f showed the highest SI value(17.1)to Cox B3 virus.Compound 14f showed both potent inhibitory activity against influenza A(IC_(50)=7.53μmol/L)and the highest SI value(12.1).SAR results showed that the alkyloxy at the 4-position of indole ring was not crucial to the antiviral activities.Incorporation of an acetyl substituent at the amino group disfavored antiviral activity towards RNA viruses.

Synthesis, Reactions and Antimicrobial Activity of Some New 3-Substituted Indole Derivatives

Reaction of indole-3-carboxaldehydes 4 with hydrazine derivatives and different substituted acid hydrazides afforded the corresponding hydrazine derivatives 5a-c and acid hydrazide derivatives 7-11 respectively. Condensation of indole-3-carboxaldehydes 4 with phenacyl bromide and thiourea gives 1,3-thiazol-2-amine derivative 18. On the other hand, reaction 4 with 3-acetylchromene-2-one afforded chalcone derivative 19. Compound 4 undergoing Knoevenagel condensation with cyanoacetamide, ethyl cyanoacetate, benzimidazol-2-ylacetonitrile, rhodanine-3-acetic acid, 2,3-dihydropyrimidin-4-one derivative and 2,4-dihydropyrazol-3-one afforded the compounds 20a,b, 22, 23, 27 and 28 respectively. The structure of the newly synthesized compounds has been confirmed by elemental analysis and spectra data. The antimicrobial activities of the some newly synthesized compounds were measured and showed that most of them have high

Two homologous INDOLE-3-ACETAIVHDE (IAM) HYDROLASE genes are required for the auxin effects of IAM in Arabidopsis

Indole-3-acetamide(IAM)is the first confirmed auxin biosynthetic intermediate in some plant pathogenic bacteria.Exogenously applied IAM or production of IAM by overexpressing the bacterial iaaM gene in Arabidopsis causes auxin overproduction phenotypes.However,it is still inconclusive whether plants use IAM as a key precursor for auxin biosynthesis.Herein,we reported the isolation IAM HYDROLASE 1(IAMH1)gene in Arabidopsis from a forward genetic screen for IAM-insensitive mutants that display normal auxin sensitivities.IAMH1 has a close homolog named IAMH2 that is located right next to IAMH1on chromosomeⅣin Arabidopsis.We generated iamh1 iamh2 double mutants using our CRISPR/Cas9gene editing technology.We showed that disruption of the IAMH genes rendered Arabidopsis plants resistant to IAM treatments and also suppressed the iaaM overexpression phenotypes,suggesting that IAMH1 and IAMH2 are the main enzymes responsible for converting IAM into indole-3-acetic acid(IAA)in Arabidopsis.The iamh double mutants did not display obvious developmental defects,indicating that IAM does not play a major role in auxin biosynthesis under normal growth conditions.Our findings provide a solid foundation for clarifying the roles of IAM in auxin biosynthesis and plant development.

Synthesis and characterization of poly(2,5-diyl pyrrole-2-pyrrolyl methine)semiconductor copolymer

The proposed technique to synthesise poly {（2,5-diyl pyrrole）（2-pyrrolyl methine）}（PPPM） copolymer by condensation of pyrrole and pyrrole-2-carboxaldehyde monomers catalyzed by Maghnite-H＋ is introduced.The protons are exchanged with Maghnite-H＋, which is available in the form of a montmorillonite silicate clay sheet. The effect of several parameters such as time and temperature of copolymerization, [pyrrole]/[pyrrole-2-carboxaldehyde] molar ratio, amount of Maghnite-H＋, and solvent on the produced poly（2,5-diyl pyrrole-2-pyrrolyl methine） semiconductor copolymer material（yield%） was investigated. The synthesized PPPM copolymer was characterized using nuclear magnetic resonance, Fourier transform infrared, and ultraviolet-visible spectroscopy.The results show that the synthesized copolymer using the copolymerization technique is a real organic copolymer consisting of two monomers units（i.e, pyrrole and pyrrole-2-carboxaldehyde）. Also, the synthesized copolymer is more soluble than polypyrrole in most of the commonly used organic solvents. Hence, copolymerization of pyrrole with pyrrole-2-carboxaldehyde will overcome the insolubility of polypyrrole. In addition, the resultant copolymer exhibits good film formability. The produced copolymer has several potential applications in the field of rechargeable batteries, sensors, capacitors, light emitting diodes, optical displays, and solar cells.