Synthesis of tetrazole containing 1,2,3-thiadiazole derivatives via U-4CR and their anti-TMV activity

A series of novel tetrazole containing 1,2,3-thiadiazole derivatives were designed and synthesized via Ugi reaction. Their structures were confirmed by melting points, IR, 1H NMR, and HRMS (ESI). Preliminary bioassay indicated that most target compounds exhibited very good direct anti-TMV activity at 100 μg/mL, which was equal to or higher than that of ribavirin. Among them, compounds 4b, 4c and 4i also showed equivalent protection effect to ribavirin in vivo at 100 μg/mL.     

Synthesis and biological evaluation of novel 1,2,4-triazole containing 1,2,3-thiadiazole derivatives

A series of novel 1,2,4-triazoles containing 1,2,3-thiadiazole derivatives were designed and synthesized. Their structures were confirmed by melting points, IR, 1H NMR, and elemental analysis and ESI-MS or HRMS. Preliminary bioassays indicated that these compounds exhibited very good insecticidal activity against Aphis laburni at 100 μg/mL, with mortality no less than 95%. Compounds 6a, 6c, 6f, 61 showed higher curative activity against TMV and compound 6h showed a higher induction effects against TMV in vivo at 100 μg/mL. Collectively, our data demonstrate a new strategy for control of insects and viruses.     

Synthesis and characterization of new hexahelicene derivatives

The synthesis and structural characterization of a new hexahelicene derivative 2 is reported. This compound features a new type of structure bearing a bromine atom and a methoxy group. Suitable crystals of the latter indicate that its conformation closely resembles that of the unsubstituted [6]helicene, whose idealized symmetry is C2. This 3-bromo-14-methoxyhexahelicene was subjected to lithiation/phosphinilation and yielded the new 3-methoxy-14-(diphenylphosphino)hexahelicene 3.     

Synthesis,characterization and antimicrobial activity of some new biquinoline derivatives containing a thiazole moiety

A series of new biquinoline derivatives containing a thiazole moiety were synthesized by a one-pot,base-catalyzed cyclocondensation reaction of 2-chloro-3-formyl quinoline,malononitrile and enaminone.All the synthesized compounds were characterized by elemental analysis,FT-IR,¹H NMR and ¹³C NMR data.All the synthesized compounds were screened against three bacterial pathogens,namely Bacillus cereus,B.substilis and Escherichia coli and for antifungal activity against three fungal pathogens,Aspergillus niger,Fusarium oxisporum and Rhizopus using the disc diffusion method.     

Synthesis of some substituted 1,2,4-triazole and 1,3,4-thiadiazole derivatives

New S-substituted 1,2,4-triazole and 1,3,4-thiadiazole derivatives have been prepared. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 11, pp. 1712–1715, November, 2008.     

Synthesis of 2-Naphthylselenoacetic Acid Dialkylamides from 4-(2-Naphthyl)-1,2,3-selenadiazole

Russian Journal of General Chemistry - Under the action of potassium hydroxide, 4-(2-naphthyl)-1,2,3-selenadiazole readily decomposes with the evolution of nitrogen and the formation of potassium...     

Synthesis and characterization of novel benzaldehyde derivatives containing 1,3,4-thiadiazole

In the work discussed in this paper, a series of novel benzaldehyde derivatives containing 1,3,4-thiadiazole were prepared in high yield from 4-fluorobenzaldehyde and 2-amino-5-substituted-1,3,4-thiadiazole. The products were characterized by determination of melting point, elemental analysis, and UV–visible, IR, ¹H NMR, and ¹³C NMR spectroscopy. The fluorescence properties of the compounds were also studied by recording their fluorescence emission spectra.     

Synthesis of new hetarylazoindole dyes from some 2-aminothiazole derivatives

A new series of heterocyclic disperse dyes were prepared by diazotization of some 2-aminothiazole derivatives and subsequent coupling with indole compounds. The dyes were characterized by UV-Vis, FT-IR, ¹H NMR, and mass spectra (LC-MS). Solvent effects on their visible absorption spectra were estimated. The color of the dyes is discussed with respect to the substituent therein. The effects of acids and bases on the visible absorption maxima of the dyes are also reported. Replacement of methyl group in the 4-position of the thiazole ring by phenyl group leads to red shift of the absorption maximum due to π-electron-donating properties of the phenyl group, while weak electron-withdrawing chlorine or bromine atom in the para-position of the phenyl group in the 2-amino-4-phenylthiazole fragment induce a small blue shift relative to 2-amino-4-phenylthiazole derivatives. Introduction of an electron-withdrawing 4-nitrophenylsulfonyl group into the thiazole ring produces bathochromic shift of the absorption maximum in all solvents. Published in Russian in Zhurnal Organicheskoi Khimii, 2008, Vol. 44, No. 4, pp. 592–599. The text was submitted by the authors in English.     

Synthesis and characterization of some nitrogen heterocycles from d-galactose derivatives

The tetrazoles 5-(6′-acetamido-6′-deoxy-1′,2′:3′,4′-di-O-isopropylidene-D-glycero-α-D-galactohexopyranos-6′-yl)tetrazole ( 1 ) and 5-(6′-acetamido-6′-deoxy-1′,2′:3′,4′–di-O-isopropylidene-L-glycero-α-D-galacto-hexopyranos-6′-yl)-tetrazole ( 2 ) were synthesized by the 1,3-dipolar cycloaddition reaction of the epimeric α-acetamidonitriles 5 and 6 , respectively, with sodium azide. Reaction of tetrazole 1 with acetic anhydride in the presence of pyridine afforded the N-acetyl-1,3,4-oxadiazole derivative 3 and the N-acetylacetamido-1,3,4-oxadiazole derivative 7 . The N-acetylacetamido-1,3,4-oxadiazole derivative ( 8 ) was isolated when the tetrazole 2 was allowed to react under the same conditions. The physical and spectroscopic data of the five new compounds 1, 2, 3, 7 and 8 are presented.     

联二烯丁基硫醚衍生物合成呋喃的反应

本文报道以联二烯丁基硫醚为起始物的呋喃衍生物的合成方法.实验结果表明,β-联二烯丁基硫醚醇在氢化钠的作用下以很高的收率环化生成一个苯硫基离去的呋喃产物,β-联二烯丁基硫醚醛与外加亲核试剂作用后能得到多一个取代的类似呋喃产物,而β-联二烯丁基硫醚酮在P2O5的促进下也能环化生成呋喃衍生物.     

Synthesis and cytotoxicity studies of new 1,2,4-thiadiazole derivatives and their zinc complexes

A new polyfunctional ligand of the thiadiazole family was synthesized. Cytotoxic properties with respect to leukemic cell lines, radiation stability, predicted permeability through the blood–brain barrier and cardiotoxicity of the new ligand and its precursor were determined. New zinc complexes with N-{2-[5-(3-chloro-4-methylphenylamino)-1,2,4-thiadiazol-3-yl]-1-methylethyl}-N-(2,2,6,6-tetramethylpiperidin-4-yl)-amine as the ligand have been obtained.     

Synthesis, electropolymerization and electrochemical characterization of some new acrylate substituted thiophene derivatives

In this work, three new acrylate substituted thiophene monomers, (3-thienyl) methylacrylate, 6-(3-thienyl)methoxy-hexylacrylate and 11-(3-thienyl)methoxy-undecylacrylate were synthesized and electropolymerized. Electrochemical polymerisation by a potential step technique leads to the formation of an electroactive film on a Pt electrode in each case. The polymerization involves evidently only the thiophene ring, as no sign of polyacrylate formation could be detected. The oxidation of each polymer was studied by in situ external reflectance FTIR spectroscopy, which showed several bands assigned to (bi)polaron type charge carriers in the region 1500–1000 cm⁻¹. The evolution of the conductivity was studied in situ by the contact electric resistance technique. The conductivity of poly(3-thienyl methacrylate) was found to be higher in aqueous solutions than in acetonitrile. The surface of poly((3-thienyl) methacrylate) was found to have a granular structure observed for many polythiophenes, as studied by atomic force microscopy (AFM).     

Synthesis,spectroscopic characterization and Antibacterial screening of some new cefotaxime sodium derivatives

Biologically active compounds with heteroaromatic ring system of cefotaxime sodium have been synthesized via aminomethylation reaction. The aminomethylation of cefotaxime sodium with various biologically potent sulphonamides/secondary amines was carried out and then characterized by elemental analysis and spectral studies – IR, ¹H NMR, ¹³C NMR, Powder X-ray diffraction and Scanning Electron Microscopy. The compounds were screened for their antibacterial activity against various pathogenic bacteria at varying concentrations. The antibacterial activity of cefotaxime sodium derivatives was compared with parent sulphonamides. The toxicity of synthesized cefotaxime sodium derivatives was ascertained by LD₅₀ test.     

Synthesis and characterization of some important indazolyl derivatives

A series of some important indazolyl derivatives of pyrazoles, diazepines, thiopyrimidines, thiazines and chromones were synthesized and characterized with the help of spectral data. Some of the synthesized compounds are tested for antimicrobial and antioxidant activities.     

3,5-二甲氧基苯乙烯环酮类化合物的合成及表征

研发环氧合酶(COSX)/5-脂氧酶(5-LOX)双重抑制剂是降低非甾体抗炎药胃肠道(GI)副作用的有效途径之一[1]。大多数二叔丁基苯酚类化合物具有较强的COX/5-LOX双重抑制作用,例如达布飞龙甲磺酸盐(darbufelone mesilate)用于治疗类风湿性关节炎和骨关节炎,GI不良反应小且长效,目前处     

Lewis acid promoted aldol reaction of fluorinated silyl enol ethers from new fluoroacetylsilane derivatives

New fluorinated silyl enol ethers with various trialkylsilyl groups were synthesized. Various fluorinated β-hydroxy ketones were synthesized by Lewis acid promoted aldol reaction of silyl enol ethers with diverse aldehydes. Reactivity of various trialkylsilyloxy groups toward Lewis acid was also studied.     

Synthesis,characterization, and antimicrobial activity of new bis-1,2,3-triazol-H-yl-substituted 2-arylbenzimidazoles

New bis-1,2,3-triazol-H-yl-substituted 2-aryl benzimidazoles VIa-VIp were synthesized from O- and N-bis-propargyl substituted 2-arylbenzimidazoles using “click chemistry.” The newly synthesized compounds were characterized by IR, NMR, and mass spectra. These compounds were screened for their activity against bacterial and fungal organisms.     

Synthesis of new functional derivatives of pyrazolidine from 1-acetyl-3-methyl-5-nitromethyl-2-phenylpyrazolidine

3-Nitromethylpyrazolidine reacts with derivatives of unsaturated acids and reducing agents with the formation of polyfunctional compounds of the pyrazolidine nucleus. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 9, pp. 1365–1369, September, 2006.