IntroductionIt is well known that carbohydrates play importantroles in a wide variety of biological processes[1], suchas cell adhesion to the extracellular matrix and cell sig-naling. They can also act as the ligands for growth fac-tors[2,3].Substituted t… 相似文献
Three novel series of 5-substituted sulfonylurea derivatives were designed and synthesized via introducing a triazole or oxadiazole ring at the 5th position of the benzene ring in classical sulfonylurea herbicides. All the target compounds were confirmed by means of 1H nuclear magnetic resonance(NMR), 13C NMR and elemental analysis. The bioassay results show that the target compounds containing an oxadiazole ring at the 5th position display moderate to excellent herbicidal activities against Brassica campestris and Amaranthus retroflexus under soil treatment. Especially, compounds zdk20, zdk21 and zdk22 possess 98.6%, 96.5% and 94.5% inhibition rates, respectively, against Amaranthus retroflexus at a concentration of 75 g/ha(1 ha=1×104 m2) under soil treatment, which approach to those of the commercial herbicide chlorsulfuron. 相似文献
Novel [1,2,4]triazole derivatives were synthesized via various synthetic pathways. Among which were different substituted [1,2,4]triazole analogues that were synthesized, in addition to various fused [1,2,4]triazolo[1,5‐a]pyrimidine derivatives, [1,2,4]triazolo[1,5‐a][1,3,5]triazines, and [1,2,4]triazolo[5,1‐c][1,2,4]triazines. Besides, benzo[h][1,2,4]triazolo[5,1‐b]quinazolines, [1,2,4]triazolo‐[5,1‐b]quinazoline, [1,2,4]triazolo[1,5‐a]quinazoline and [1,2,4]triazolo[5,1‐d][1,2,3,5]tetrazine derivatives were also synthesized. The newly synthesized compounds were evaluated for their in vitro anticancer activity against liver cancer HepG2 and breast cancer MCF7 cell lines compared with the reference drug doxorubicin. Compounds 4 , 7 , 15 , 17 , 28 , 34 , and 47 were found to exert promising anticancer activity against HepG2 cell line showing IC50 values ranging from 17.69 to 25.4 μM/L, while compounds 7 , 14a , 17 , 28 , and 34 showed significant activity against MCF7 cell line with IC50 values ranging from 17.69 to 27.09 μM/L. 相似文献
Russian Journal of Organic Chemistry - A tetraazacrown ether, 4,9-di(prop-2-yn-1-yl)-1,4,9,12-tetraazacyclohexadecane-2,11-dione, bearing propargyl groups on two nitrogens was synthesized starting... 相似文献
A series of new andrographolide‐1,2,3‐triazole derivatives, 3a , 3b , 3c , 3d , 3e , 3f , 3g , 3h , 3i , 3j , 3k , were synthesized from a natural bioactive labdane type diterpenoid, andrographolide. All the derivatives were screened against human cancer cell lines MCF7, MDA‐MB‐231, COLO205, HepG2, K562, Hela, and HEK293 to evaluate their cytotoxic activity. All the compounds showed anticancer activity selectively against K562 cell line, with IC50 values ranging from 8.00 to 17.11 µM, and are inactive against the rest of the cell lines. Compounds 3c and 3d showed significant cytotoxicity among the synthesized derivatives. The in silico docking studies revealed compounds 3b and 3d with high binding affinity against the cancer target, transient receptor potential vanilloid 1. 相似文献
Novel unsymmetrical bis‐heterocyclic compounds encompassing triazole and isoxazole moieties were synthesized by employing 1,3‐dipolar cycloaddition/click chemistry approach using 5‐butynyl‐1,2,3‐triazoles and 5‐butynyl isoxazoles. 相似文献
We report on the modification of the polyelectrolytes poly(L ‐glutamic acid) (PGA), poly(acrylic acid) (PAA), and poly(L ‐lysine) (PLL) with side groups bearing phosphorylcholine (PC) groups. Two different side chains were synthesized from monoamino tri‐ or tetraethylene glycol, both with PC group linked to the OH end: the tert‐butyloxycarbonyl protected compounds BOCNH(EO)nPC (n = 2, 3) and the succinylated compound SucNH(EO)3PC. BOCNH(EO)nPC was deprotected and the resulting amine was condensed with PGA or PAA and SucNH(EO)3PC was directly coupled to PLL. Degrees of substitution as high as 80% were obtained with the method described. These polyelectrolytes are potential candidates to fabricate multilayers with protein repellent properties.
A series of novel pinanyl pyrimidine amine derivatives (1e~1n) and camphoryl pyrimidine amine derivatives (2b~2f) bearing bicyclic monoterpene moieties were designed and synthesized from natural and renewable nopinone and camphor. All chemical structures of target compounds were characterized by 1H NMR, 13C NMR and HRMS spectra analyses, and the antimicrobial activities were evaluated. The results indicated that most compounds showed considerable antibacterial and antifungal activities against Klebsiella pneumoniae, Streptococcus pneumoniae, Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Methicillin-Resistant Staphylococcus aureus (MRSA), Bacillus cereus and Candida albicans. Among them, 1f showed potent antibacterial activity against all tested bacteria, 1i exhibited excellent inhibition against Streptococcus pneumoniae (1 μg/mL) and Escherichia coli (1 μg/mL), which was better than the control drug amikacin (2 μg/mL). As to antifungal activity against Candida albicans (C. albicans), compound 1l showed comparable activity (16 μg/mL) to the control drug ketoconazole. Furthermore, five active compounds with better antimicrobial activities also showed anti-inflammatory potencies against mouse mononuclear macrophages leukemia cells (RAW). Especially, 1f (IC50 = 1.37 μM) and 2f (IC50 = 1.87μM) are more potent than the control drug aspirin (IC50 = 1.91 μM). 相似文献
The reactive 1 : 1 intermediate produced in the reaction between triphenylphosphine and diisopropyl azodicarboxylate has been trapped by isocyanates or isothiocyanates to yield 1,2,4‐triazole derivatives 2 (Scheme 1). The structures of the highly functionalized compounds 2 were corroborated spectroscopically (IR, 1H‐ and 13C‐NMR, EI‐MS) and by elemental analyses. A mechanism for this type of cyclization is proposed (Scheme 2). 相似文献
Several heterocyclic systems such as 1,2,3‐triazoles ( 5–9 ), pyrimidotriazoles ( 10–13 ), benzothiazole ( 16 ), thiazolo ( 17 ), and pyrimidinone derivative ( 18 ) was obtained from 4‐aminobenzophenone ( 1 ) and the appropriate reagents. 相似文献
The phthalonitrile (3) and triazole substituted metallo phthalocyanines (MPc) (4–7) were prepared. The novel compounds were characterized with spectroscopic data. Electrochemical analyses of metallophthalocyanines (4–7) bearing triazole substituents were performed to investigate redox activity of phthalocyanines (Pcs) ring. While incorporation of Ni2+ and Cu2+ cations in the Pc core only influenced peak positions of Pc ring processes, Co2+ and Cl1?Fe3+ cations of CoPc and FePc gave extra redox couples to the Pc based ones. Releasing the axial Cl1? anion on Fe3+ cation of FePc during the reduction reactions complicated the redox responses. Redox reactions of Co2+ and Fe3+ metal centers also considerable influenced spectral and color responses of these complexes. 相似文献
The synthesis of novel substituted 3-p-nitro-phenyliminocoumarins and corresponding N-ureaiminocoumarins is described. The condensation of these materials with oxalyl chloride leads to the corresponding N-parabanic iminocoumarins, which have not previously been described, in moderate or good yields and high selectivity. The structures were characterized by Fourier transform infrared, 1H and 13C NMR, and elemental analysis.
The authors acknowledge the Ministry of Higher Education, Scientific Research, and Technology in Tunisia for their financial support. They also thank Pr. Rachid El Gharbi for his useful discussions about this work. 相似文献
An efficient route to synthesize the target compounds was developed. Fifteen new 5‐[4′‐(5‐isoxazol‐4‐aryl‐1,2,4‐triazol‐3‐yl‐sulfanylmethyl)‐biphenyl‐2‐yl]‐tetrazoles derivatives were synthesized. The structures of the new compounds synthesized were confirmed by elemental analyses and spectral data. 相似文献
2‐Bromoacetyl‐3‐phenyl‐1,3,4‐thiadiazole derivative was synthesized and reacted with a number of heterocyclic amines to give a series of fused imidazole derivatives. Also, reaction of 2‐bromoacetyl‐3‐phenyl‐1,3,4‐thiadiazole with o‐phenylene diamine and 2‐aminothiophenol yielded the respective products. Moreover, reaction of 2‐bromoacetyl‐3‐phenyl‐1,3,4‐thiadiazole with thiourea, thiosemicarbazide, thiocarbahydrazide gave the respective thiazoles. The structures of all the novel products were elucidated on the basis of elemental analysis and spectral data. In addition, the biological activity of the newly synthesized compounds was evaluated, and the results obtained indicate their potency as anti‐inflammatory, analgesic, and anti‐ulcer agents. The binding mechanism of the most active compounds was studied using MOE to analyze the molecular interactions. 相似文献
Based on our previous studies of 3D-QSAR, 38 novel objective compounds belonging to 4 series were designed and successfully synthesized directed by the idea of reconstructing the structure of non-pharmacophores while reserving essential ones in triazoles. In vitro pilot studies on their antifungal activities showed that most compounds have inhibitory effects on C.albicans and some inhibit S.cerevisiae also. The effects on C.albicans of 5 compounds are more potent than or equal to that of fluconazole or itraconazole. 相似文献
One‐pot synthesis of heterocycle fused‐triazole analogs from the corresponding aldehydes and heteroarylhydrazines is demonstrated. Transformation of hydrazones to the desired systems was achieved by employing the oxidative cyclization with catalytic CuBr2 and oxone. This reaction condition is mild and selective, and a wide range of functional groups were able to sustain. An array of biologically important triazolopyridines, triazolopyridazines, triazolopyrimidines, and triazoloquinolines were obtained in fairly good yield. 相似文献