Research Progress on Synthesis of Superoxide Dismutase Mimics

Research on the synthesis of superoxide dismutase mimics by chemical and biologi-cal synthetic methods were reviewed.The advantages and limitations were analyzed.A prospect for the future development of superoxide dismutase mimics is proposed.

Synthesis,Crystal,Computational Study and Biological Activity of N-(1-(2,4-Dichlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)-4-(N,N-dipropylsulfamoyl)benzamide

The title compound N-（1-（2,4-dichlorophenyl）-1 H-pyrazolo[3,4-d]pyrimidin-4-yl）-4-（N,N-dipropylsulfamoyl）benzamide was synthesized by the condensation of 4-（dipropylsulfamoyl）benzoic acid with 1-（2,4-dichlorophenyl）-1 H-pyrazolo[3,4-d]pyrimidin-4-amine. This intermediate was prepared from 5-amino-1-（2,4-dichlorophenyl）-1 H-pyrazole-4-carbonitrile by the condensation with triethyl orthoformate and then cyclisation with ammonium hydroxide solution in tetrahydrofuran at room temperature. The crystal structure of the title compound was determined. The optimized geometric bond lengths and bond angles obtained by using density functional theory（DFT） have been compared with X-ray diffraction values. In addition, the preliminary biological test showed that the compound possesses distinct effective inhibition on the proliferation of some cancer cell lines.

STUDIES ON THE SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-ARYLOXYACETYL-4-AROYLTHIOSEMICARBAZIDE DERIVATIVES

A series of new 1-aryloxyacetyl-4-aroylthiosemicarbazides were synthesized by means of solid-liguid phase transfer catalysis. The promoting effects of these new compounds on wheat growth were observed.

Synthesis and Biological Activities of 10-Substituted 9-Aryl-3,4,6,7,9,10-hexahydroacridine-1,8(2H,5H)-diones

A series of 10-substituted 9-aryl-3,4,6,7,9,10-hexahydroacridine-1,8（2H,5H）-dione derivatives 2 were synthesized by a two-step reaction.All the compounds were characterized by IR,MS,and ^1H NMR.Crystals of 1a and 2c were obtained and determined by X-ray single-crystal diffraction.Crystal data of 1a：C_（20）H_（22）O_5,orthorhombic system,space group Pbcn,a = 15.8888（19）,b = 18.228（2）,c = 11.6926（13） A,V = 3386.4（7） A^3,Z = 8,F（000） = 1456,Dc = 1.343 g/cm^3,R = 0.0456 and w R = 0.1600.Crystal data of 2c：C_（26）H_（24） Cl NO_3,monoclinic system,space group P2_1/n,a = 8.628（2）,b = 10.912（3）,c = 22.425（7） A,β = 90.786（4）°,V = 2111.1（10） A^3,Z = 4,F（000） = 912,D_c = 1.365 g/cm^3,R = 0.0613,and w R = 0.1196.The results of biological experiments show that compounds 2b and 2c could inhibit the proliferation of Hep G2 cells.

Synthesis,Crystal Structure and Anti-fungal Activity of 2-(4-Chlorophenyl)-(1,3-dimethyl-2,3-dihydro-1H)-perimidine

The title compound 2-（4-chlorophenyl）-1,3-dimethyl-2,3-dihydro-1H-perimidine（C（19）H（17）ClN2） was synthesized and characterized by elemental analysis, ^1H NMR, HRMS and single-crystal X-ray diffraction. The crystal of the title compound belongs to orthorhombic system,space group Pnma with a = 11.385（2）, b = 12.170（2）, c = 11.210（2）A, V = 1553.2（5）A^3, Z = 4, Dc =1.321 g/cm^3, m（Mo-Ka） = 0.244 mm^-1, F（000） = 648, S = 1.309, R = 0.0400 and w R（I 〉 2s（I）） =0.1065. X-ray diffraction results showed that the molecular structure is highly symmetric and the new-formed N-heterocyclic ring is non-planar. In addition, the biological experiment showed that the title compound showed inhibitory activities against fungi with varied potencies.

Syntheses,Crystal Structures and Biological Activities of the 2-Oxo-butyric Acid Salicylacylhydrazone Dibenzyltin Complexes

2-Oxo-butyric acid salicylacylhydrazone dibenzyltin（IV） complexes 1 {[o-OHC6H4（O）C=N-N=C（Et）COO]（CH3OH）[（C6H5CH2）2Sn]}2 and 2 {[o-OH-C6H4（O）C=N-N=C（Et）-COO]（CH3OH）[（2,4-Cl2C6H3CH2）2Sn]}2 have been synthesized. The complexes were characterized by IR, 1H, 13C and 119Sn NMR spectra, elemental analysis and thermal stability analysis, and the crystal structures were determined by X-ray diffraction. The crystal of complex 1 belongs to triclinic system, space group P1 with a = 8.9121（6）, b = 10.3875（7）, c = 14.5658（10） ？, α = 89.534（5）, β = 86.790（5）, γ = 70.103（6）°, Z = 1, V = 1265.85（15） ？3, Dc = 1.488 Mg·m^（-3）, m（Mo Kα） = 1.047 mm-1, F（000） = 576, R = 0.0466 and w R = 0.1054. The crystal of complex 2 belongs to monoclinic system, space group P21/n, a = 12.7165（10）, b = 17.8466（14）, c = 12.8538（10） ？, β = 95.1310（10）°, Z = 2, V = 2905.4（4） ？~3, Dc = 1.612 Mg·m^（-3）, m（Mo Kα） = 1.286 mm-1, F（000） = 1408, R = 0.0369 and w R = 0.0958. In vitro antitumor activities of both complexes were evaluated by the 3-（4,5-dimethylthiazoly-2-yl）-2,5-diphenyltetrazolium bromide（MTT） assay against three human cancer cell lines（NCI-H460, HepG2, MCF7） and one human cell line（HL7702）. Two complexes exhibited strong antitumor activity, and then they were expected after further chemical optimization of candidate compounds as anti-cancer drugs. The interaction between complexes and calf thymus DNA were studied by EB fluorescent probe. The interactions of the two complexes with calf thymus DNA were intercalation.

Synthesis,Crystal Structure,Thermal Stability and Anti-tumor Activity In Vitro of Bis(tricyclohexyltin) Pimelicarboxylate

Bis（tricyclohexyltin） pimelicarboxylate, [（CH2）5（CO2SnCy3）2] （1）, has been synthesized by the reaction of tricyclohexyltin hydroxide with pimelic acid and characterized by means of 1R, 1H and 13C NMR, elemental analysis and X-ray diffraction. Complex 1 crystallizes in triclinic space group Pi with a = 11.569（3）, b = 12.0419（2）, c = 17.3988（4） A, α = 81.4310（10）, β = 79.8270（10）, ）, = 69.7060（10）°, V = 2227.60（9） A3, Z = 2, C43H7604Sn2, Mr = 894.42, Dc = 1.333 g.cm-3, μ = 1.157 mm-1, F（000） = 932, GOOF = 1.339, the final R = 0.0452 and wR = 0.1333 for 6709 observed reflections （1〉 2σ（I）. Complex 1 shows discrete dimeric structures and the tin atoms have a distorted tetrahedral geometry. The 1D chain structure of complex 1 is formed by intermolecular Sn…O interactions. Complex 1 displays good thermal stability under 553 K and has selective antibacterial property. Complex 1 is strong in vitro anti-tumor activity against five human tumor cell lines, Colo205, HepG2, MCF-7, Hela and NCI-H460, and is significantly higher than that in the clinical use of carboplatin.

Design,synthesis and biological evaluation of novel non-azole derivatives as potential antifungal agents

A series of 3-substituted quinazolinones,2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in vitro.The new compounds revealed excellent in vitro antifungal activity with broad spectrum.The structure-activity relationships（SARs） of the derivatives were analyzed.Compound 9A2 exhibits better antifungal activity against 5 tested fungi in vitro than fluconazole,especially against Trichophyton rubrum and Microsporum gypseum.This study provides a series of novel lead compounds for the development of non-azole antifungal agents.

Synthesis and biological evaluation of novel phenothiazine derivatives as non-peptide arginine vasopressin V2 receptor antagonists

A series of novel phenothiazine derivatives was synthesized and tested for arginine vasopressin receptor antagonist activity. They were synthesized as novel arginine vasopressin receptor antagonists from phenothiazine as a scaffold via successive acylation, reduction and acylation reactions. Their structures were characterized by ^1H NMR, ^13C NMR and HRMS, and biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay indicated that several compounds are potent selective V2 receptor antagonists. Compounds with promising binding affinity to V2 receptors were selected to conduct the in vivo diuretic studies on Sprague-Dawley rats. Among them, 1n, 1r, It and 1v exhibited excellent diuretic activity, especially 1 r and 1v. Therefore, 1 r and 1v are potent novel AVP V2 receptor antagonist candidates.

A Systematic Review on Antituberculosis Drug Discovery and Antimycobacterial Potential of Biologically Synthesized Silver Nanoparticles:Overview and Future Perspectives

Rapid emergence and quick evolution of drug-resistant and aggressive mycobacterial strains have resulted in the present antimycobacterial drug crisis and the persistence of tuberculosis as a major public health problem.Green/biological nanotechnologies constitute an interesting area of research for discovering antimycobacterial agents.This review focused on the biological(green)synthesis of silver nanoparticles(AgNPs)as an alternative source of antimycobacterial agents.Data for this study were searched and screened from three electronic databases(Google Scholar,PubMed and ScienceDirect)following the Preferred Reporting Items for Systematic Reviews and Meta-analyses flowchart.Data from in total 17 eligible studieswere reported in this systematic review.Twelve of the 17 studies used plants to fabricate AgNPs,whereas the remaining five studies used microorganisms(bacteria and/or fungi).Silver as part of silver nitrate(AgNO3)was themetal precursor reported for the synthesis of AgNPs in these studies.Silver nanoparticles were mostly spherical,with sizes ranging from12 to140nm.Resultsbasedon minimum inhibitory concentrations varied between studies and were divided into three groups:(i)those more effective than the antibiotic(controls),(ii)those more effective than plant extracts,and(iii)those less effective than the antibiotic controls.In addition,little or no cytotoxicity effects were reported.Silver nanoparticles were also shown to be highly specific or selective toward mycobacterial strains.This systematic review highlights the antimycobacterial potential of biologically synthesized AgNPs,underscoring the possibility of discovering/developing new antimycobacterial agents using biological synthesis approaches with less toxicity and high selectivity.

Gold-catalyzed oxazoles synthesis and their relevant antiproliferative activities

Nine 5-aryl-2-methyloxazole derivatives were synthesized via gold-catalyzed alkyne oxidation. All of the compounds have been screened for their antiproliferative activities against MCF-7 cell （human breast carcinoma）, A549 cell （human lung carcinoma） and Hela cell （human cervical carcinoma） lines in vitro. The results revealed that compounds 1b, 1c and 1d exhibited strong inhibitory activities against the MCF-7 cell lines （with ICso values of 4.6, 9.7 and 2.2 μmol/L, respectively）.