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1.
A series of novel quinazolin-4(3H)-one derivatives (6a–6y) containing a 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole moiety were designed and synthesized, and their structures were fully characterized by 1H NMR, 13C NMR, HRMS and IR spectra. Among them, the structure of compound 6u was unambiguously confirmed via single crystal X-ray diffraction analysis. The obtained bioassay results showed that compounds 6h, 6k, 6l and 6y had the EC50 (half-maximal effective concentration) values of 34.8, 28.2, 41.5 and 42.5 μg/mL against the phytopathogenic bacterium Xanthomonas oryzae pv. oryzae (Xoo), respectively, which were significantly better than commercial bactericide Bismerthiazol (EC50 = 95.8 μg/mL). Additionally, compounds 6a and 6b exhibited the strong inhibition activity against the pathogen Xanthomonas axonopodis pv. citri (Xac). 相似文献
2.
Mustapha C. Mandewale Bapu Thorat Y. Nivid Ram Jadhav Aarti Nagarsekar Ramesh Yamgar 《Journal of Saudi Chemical Society》2018,22(2):218-228
The quinoline hydrazone ligands were synthesized through multi-step reactions. The 2-hydroxy-3-formylquinoline derivatives (1a–1c) were prepared from acetanilide derivatives as starting materials using Vilsmeier–Haack reaction. Then the condensation of 2-hydroxy-3-formylquinoline derivatives with hydrazide derivatives (2a–2c) yielded quinoline hydrazone ligands (3a–3i). The synthesis of a new series of Zn(II) complexes carried out by refluxing with these quinoline hydrazone ligands (3a–3i) is reported. The molecular structures of the ligands (3a–3i) and the Zn complexes were characterized by elemental analysis and spectral studies like FT-IR, 1H and 13C NMR, MS, UV–Visible and fluorescence. The preliminary results of antituberculosis study showed that most of the Zn(II) complexes 4a–4i demonstrated very good antituberculosis activity while the ligands 3a–3i showed moderate activity. Among the tested compounds 4e and 4g were found to be most active with minimum inhibitory concentration (MIC) of 8.00 μM and 7.42 μM respectively against Mycobacterium tuberculosis (H37 RV strain) ATCC No-27294 which is comparable to “first and second line” drugs used to treat tuberculosis. 相似文献
3.
《Arabian Journal of Chemistry》2020,13(1):120-133
A rapid, simple and highly efficient method for the synthesis of a variety of 2-aryl-benzimidazoles, 2-aryl-benzothiazoles and quinoxalines has been developed using Koser’s reagent [PhI(OH)OTs] as catalyst. The present work highlights the potential of Koser's reagent ([PhI(OH)OTs]) for the synthesis of benzimidazoles, benzothiazoles and quinoxalines, etc. Short reaction time, high yields, importantly low catalyst loading, broad substrate scope and scalability are the salient features of this methodology. Particularly, this method has been employed successfully to synthesize highly structured indole-benzimidazole and quinoxaline-6-carboxamide derivatives as well as biologically important benzimidazole-imidazo[1,2-a]pyridine conjugates in moderate to good yields. These remarkable features make the present methodology a valid contribution to the existing precedents for the synthesis of benzimidazoles, etc. In the MTT assay, benzimidazole-imidazo[1,2-a]pyridine conjugates 3s, 3t and 3v were found to be active on MCF-7 (IC50 values of 5.10 ± 0.10, 8.23 ± 0.02, and 10.75 ± 0.03 µM, respectively) and MDA-MB-231 cell lines (IC50 values of 10.83 ± 0.13, 7.68 ± 0.05, and 7.87 ± 0.24 µM, respectively). Flow-cytometry analysis revealed that the treatment of MCF-7 cells with compound 3s showed moderate effect on the progression of G0/G1 phase of the cell cycle. 相似文献
4.
《Arabian Journal of Chemistry》2020,13(6):5593-5604
The present study aims to introduce three known and three new stable polycyclic aromatic compounds synthesized. With MALDI-Mass, 1H and 13C NMR spectroscopy, all new compounds were characterized. In the DMF solution were carried out the electrochemical and photophysical properties of the polyaromatic compounds. The compounds are highly fluorescent showing green-red emission when excited at one single wavelength. For the compound 3, it was shown that the highest Stokes Shift (191 nm) appeared which may be due to the excited state energy transfer. The compounds also indicated the blue-orange region of the electromagnetic spectrum strong emission bands. Additionally, compounds 1, 3, 4, and 5 were investigated for their in vitro cytotoxic activities against PC-3 prostate cancer cells, L-929 non-cancerous cells, and MDA-MB-231 breast cancer for 24 h, 48 h and 72 h. The results obtained from the experiment demonstrated that compounds had different cytotoxic activity against cell lines. Compound 3 was indicated to be inactive against L-929 cells and MDA-MB-231 cancer cells, whereas compounds 1, 4 and 5 indicated a dose and time-dependent cytotoxic activity against PC-3, MDA-MB-231, and L-929 cell lines. It was found that the most sensitive cells to compound 5 were MDA-MB-231 human breast cancer cells. Additionally, it became clear that compounds 1 and 3 had significant selectivity for human PC-3 prostate cancer cells, and compounds 1, 4 and 5 had considerable selectivity for human MDA-MB-231 breast cancer cells. Also, the quantum chemical examinations of six organic compounds were conducted at the B3LYP/6-31G level in the gas phase and water. According to calculated results, compound 5 was found to be the best candidate for NLO applications. 相似文献
5.
Gustav Komlaga Grégory Genta-Jouve Sandrine Cojean Rita A. Dickson Merlin L.K. Mensah Philippe M. Loiseau Pierre Champy Mehdi A. Beniddir 《Tetrahedron letters》2017,58(38):3754-3756
The chemical investigation of the antimalarial plant Phyllanthus fraternus G. L. Webster (Phyllanthaceae) resulted in the discovery of the Securinega alkaloid (+)-allonorsecurinine (1), previously reported as a synthetic compound, together with the known ent-norsecurinine (2), nirurine (3), bubbialine (4), epibubbialine (5) and the lignan phyllanthin (6). The structure and absolute configuration of the new compound were elucidated on the basis of extensive spectroscopic analysis, optical rotation, and GIAO NMR shift calculation followed by CP3 analysis. The antiplasmodial activity of these compounds was evaluated against chloroquine-resistant (W2) and -sensitive (3D7) strains of Plasmodium falciparum. Among them, ent-norsecurinine (2) and (+)-allonorsecurinine (1) showed the strongest activity (IC50: 1.14 ± 0.32 and 2.57 ± 0.53 µM) respectively, against W2 but one of the weakest against 3D7. 相似文献
6.
Chiral [(1R)-10-(N,N-diethylsulfamoyl)isobornyl] 2H-azirine 1 [Timén, A. S.; Somfai, P. J. Org. Chem. 2003, 9958–9963; Timén, A. S.; Fisher, A.; Somfai, P. Chem. Commun. 2003, 1150–1151]. was combined to a number of 1,4-disubstituted-2-aza-1,3-dienes 2a–g [Alves, M. J.; Durães, M. M.; Gil Fortes, A. Tetrahedron 2004, 6541–6553] to give cycloadducts 8a–g as major isomers. High to good diastereofacial differentiation of the two faces of the azirine is observed when R1,R2 = Ar 2a–e; diastereoselectivity drops drastically when R1 = Me or H 2f,g. Cycloaddition of the azirine 1 to E,E-1,4-diacetoxy-1,3-butadiene shows complete diastereoselectivity giving cycloadduct 11a. 相似文献
7.
Two xanthanolide-type dimmers, namely Mogolide D (4) and Mogolide E (5) are isolated from the aerial parts of Xanthium mogolium Kitag plant collected from Heilongjiang province, China. The dimmers’ relative structures are elucidated on the basis of HRESIMS, IR spectrum and NMR spectroscopy. The absolute configurations of them are assigned with ECD spectra. The biosynthetic pathway of the two dimmers is also proposed. Besides, Mogolide D (4) and Mogolide E (5) are tested against MDA-MB-231 breast cancer cell line with IC50 8.46 μM and 19.20 μM, respectively. 相似文献
8.
Hongjian Wang Kai Lv Xiaoning Li Bo Wang Apeng Wang Zeyu Tao Yunhe Geng Bin Wang Menghao Huang Mingliang Liu Huiyuan Guo Yu Lu 《中国化学快报》2019,30(2):413-416
We report herein the design and synthesis of a series of novel nitrobenzamide derivatives. Results reveal that many of them display considerable in vitro antitubercular activity. Four N-benzyl or N- (pyridine-2-yl)methyl 3,5-dinitrobenzamides A6, All, Cl and C4 have not only the same excellent MIC values of0.016 μg/mL against both drug-sensitive MTB strain H37 Rv and two drug-resistant clinical isolates as PBTZ169 and the lead 1, but also acceptable safety indices (SI 1500), opening a new direction for further development. 相似文献
9.
《Arabian Journal of Chemistry》2014,7(6):994-999
A series of 2-(phenyl)-2-(morpholin-4-yl)-N-phenylacetamide I–VII were synthesized by Mannich base method. Synthesized compounds I–VII were confirmed by IR, 1H NMR, 13C NMR, mass and elemental analyses. Synthesized compounds I–VII were screened for antibacterial activity against various bacterial strains and compared with standard Ciprofloxacin at concentration 100 μg/mL and for antifungal activity against various fungal strains and compared with Clotrimazole at concentration 100 μg/mL; particularly 3-(4-chlorophenyl)-3-(morp holin-4-yl)-N-phenylpropanamide lll that has high antibacterial activity against Streptococcus epidermidis was compared with standard Ciprofloxacin. 相似文献
10.
《Arabian Journal of Chemistry》2020,13(1):377-392
A series of diazenyl schiff bases have been synthesized by reaction of salicylaldehyde containing azo dyes with various substituted aniline derivatives in the presence of acetic acid as catalyst. The structures of diazenyl derivatives were determined by FTIR, UV–vis, 1H NMR, 13C NMR, CHN analysis, fluorimetric and mass spectroscopic studies. The synthesized derivatives were screened for their in vitro antimicrobial activity against various Gram-positive (S. aureus, B. subtilis, B. cereus), Gram-negative (S. typhi, S. enterica, E. coli, P. aeruginosa) bacterial and fungal (C. albicans, A. niger and A. fumigatus) strains, using cefadroxil (antibacterial) and fluconazole (antifungal) as standard drugs. The diazenyl schiff bases were also screened for their cytotoxicity against human colorectal carcinoma cell line (HCT-116) using 5-fluorouracil as standard drug by Sulforhodamine-B Stain (SRB) assay. The schiff bases exhibited significant activity toward both Gram-positive, Gram-negative bacterial and fungal strains. Most of the synthesized derivatives showed high activity against S. enterica. 4-((2,5-Dichlorophenyl)diazenyl)-2-((3-bromophenylimino)methyl)phenol (SBN-40) was found to be very active against S. aureus, B. cereus and E. coli, with MIC = 0.69 (µM/ml × 102). The compound 4-((2-bromophenyl)diazenyl)-2-((4-nitrophenylimino)methyl)phenol (SBN-13) possessed comparable activity (IC50 = 7.5 µg/ml) to the standard drug 5-fluorouracil (IC50 = 3.0 µg/ml) against human colorectal carcinoma cell line (HCT-116). 相似文献
11.
Synthesis and biological evaluation of novel 1,2,4-triazole containing 1,2,3-thiadiazole derivatives
Yue-Dong Li Wu-Tao Mao Zhi-Jin Fan Juan-Juan Li Zhen Fang Xiao-Tian Ji Xue-Wen Hua Guang-Ning Zong Feng-Yun Li Chao-Lun Liu Jian-Hua Yu 《中国化学快报》2013,24(12):1134-1136
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. 相似文献
12.
Yan-Jiao Wang Da-Gui Zhou Fang-Cheng He Ji-Xiang Chen Yong-Zhong Chen Xiu-Hai Gan De-Yu Hu Bao-An Song 《中国化学快报》2018,29(1):127-130
A series of novel chalcone derivatives containing purine group was synthesized and evaluated for their antiviral activities against cucumber mosaic virus and tobacco mosaic virus. Compound 3o exhibited remarkable antiviral activities and strong combining capacity to tobacco mosaic virus coat protein. 相似文献
13.
Employing the intermediate derivatization method (IDM), a series of 1,3,4-oxadiazole derivatives containing arylpyrazoloxyl moiety were designed and synthesized. In vitro bioassays showed that these compounds have moderate to significant fungicidal activity against rice sheath blight and sorghum anthracnose. Furthermore, compound 20 is a promising fungicide for further development. 相似文献
14.
《Journal of organometallic chemistry》2007,692(1-3):635-644
Novel imidazolylethynyl-zinc-porphyrin 1a and its meso,meso-linked bisporphyrin 5M were synthesized effectively by the reaction of the corresponding bromoporphyrins and 2-imidazolylethyne in the presence of palladium-arsenic catalyst. The complementary coordination of monomer 1a into dimer 2a was observed by 1H NMR and UV–Vis spectroscopy. Self-association constant of 1a to 2a in CHCl3 (including 0.5% ethanol) was determined as 1.84 × 107 M−1 by UV–Vis titration of 2a with N-methylimidazole. UV–Vis absorption and fluorescence spectra of 1a, 2a, monomer 5M, and its polymer 5P were compared. 相似文献
15.
Jianxun Zhu Xiaofeng Lu Xiaona Fan Ruibo Wu Hongjuan Diao Rongmin Yu Hanhong Xu Jiachen Zi 《中国化学快报》2018,29(8):1261-1263
Azadiramide A (1), a new salannin-class limonoid alkaloid, inhibits growth of human breast cancer MDA-MB-231 cell line with IC50 value of 2.70±0.63 μmol/L. 相似文献
16.
Thi Dao Phi Huong Doan Thi Mai Van Hieu Tran Van Loi Vu Bich Ngan Truong Tuan Anh Tran Van Minh Chau Van Cuong Pham 《Tetrahedron letters》2017,58(19):1830-1833
A series of bengamide E analogues were prepared from the corresponding polyketide chain and amino acids via amide coupling reactions. Opening of the polyketide chain lactone ring with α-aminolactams was successfully achieved under microwave irradiation in the presence of sodium 2-ethyl hexanoate. A cytotoxic activity evaluation against a panel of cancer cell lines (KB, HepG-2, Lu-1, MCF-7, HL-60 and Hela) indicated that the 2′R analogues were generally more cytotoxic than the 2′S analogues. Additionally, several analogues exhibited selective inhibition against various cancer cell lines: compounds 32a and 32b selectively inhibited MCF-7 cells, while 33b and 35b were more sensitive toward Lu-1 and HepG-2, respectively. Notably, some of the synthetic analogues possess cytotoxic activities with IC50 values less than 1 µM. 相似文献
17.
《Tetrahedron: Asymmetry》2014,25(22):1456-1465
A method using (S)-(+)-2-methoxy-2-(1-naphthyl)propionic acid 1 (MαNP acid) has been applied to acetylene alcohols 4–14 to determine their absolute configurations by 1H NMR anisotropy and/or X-ray crystallography. Diastereomeric MαNP esters prepared from racemic acetylene alcohols and (S)-(+)-MαNP acid 1 were easily separable by HPLC on silica gel. From the 1H NMR anisotropy Δδ data of separated diastereomeric MαNP esters {Δδ = δ (R,X) − δ(S,X) = δ(2nd fr.) − δ(1st fr.)}, the absolute configurations of the first eluted esters were determined. This MαNP acid method has been successfully applied to various acetylene alcohols 4–12 and 14. In the case of MαNP esters 21b, 24a, and 26a, their absolute configurations were unambiguously determined by X-ray crystallography, which confirmed the absolute configuration assignments performed by 1H NMR anisotropy. These acetylene alcohol MαNP esters can serve as key intermediates for the synthesis of enantiopure aliphatic chain alcohols with established absolute configurations as described in Part 2 of this series. 相似文献
18.
Truc T.T. Duong Truong N.V. Do Hai X. Nguyen Tho H. Le Phu H. Dang Nhan T. Nguyen Tuyen N.T. Nguyen Thao D. Nguyen Mai T.T. Nguyen 《Tetrahedron letters》2017,58(23):2280-2283
Two new neolignans, named rebaneolignan A (1) and B (2), were isolated from the stem of Mangifera reba (Anacardiaceae), together with six known compounds (3–8). Their structures were elucidated on the basis of NMR spectroscopic analysis and the absolute configurations of 1 and 2 were determined by NOESY and CD data. All isolated compounds were found to possess more potent inhibitory activity, with IC50 values ranging from 28.5 to 162.8 µM, than the positive control acarbose (IC50, 214.5 µM). Plausible biosynthetic pathways for the formation of 1 and 2 were proposed based on the oxidative β-5′ coupling reactions. 相似文献
19.
The carbosilanes RMe2Si(CH2)xSiH3, [R = 2-Th (1a, 2a), 4-Me-2-Th (3a, 4a), 2-Fu (5a, 6a), 5-Me-2-Fu (7a, 8a); x = 2 and 3], with primary SiH3 end groups undergo a facile dehydropolymerization under ambient conditions (50 °C, 48 h) in presence of Cp2TiCl2/2.2 n-BuLi catalyst to afford the corresponding poly(hydrosilane)s 1–8 bearing carbosilyl side chains appended with thienyl/furyl groups. These have been characterized by GPC, IR, multinuclear (1H, 13C{1H}, 29Si{1H}) NMR, UV and PL spectral studies. 相似文献
20.
Hüseyin Ünver Zeliha Hayvali 《Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy》2010,75(2):782-788
Two new nickel(II) [Ni(L)2] and copper(II) [Cu(L)2] complexes have been synthesized with bidentate NO donor Schiff base ligand (2-{(Z)-[furan-2-ylmethyl]imino]methyl}-6-methoxyphenol) (HL) and both complexes Ni(L)2 and Cu(L)2 have been characterized by elemental analyses, IR, UV–vis, 1H, 13C NMR, mass spectroscopy and room temperature magnetic susceptibility measurement. The tautomeric equilibria (phenol-imine, O–H?N and keto-amine, O?H–N forms) have been systemetically studied by using UV–vis absorption spectra for the ligand HL. The UV–vis spectra of this ligand HL were recorded and commented in polar, non-polar, acidic and basic media. The crystal structures of these complexes have also been determined by using X-ray crystallographic techniques. The complexes Ni(L)2 and Cu(L)2 crystallize in the monoclinic space group P21/n and P21/c with unit cell parameters: a = 10.4552(3) Å and 12.1667(4) Å, b = 8.0121(3) Å and 10.4792(3) Å, c = 13.9625(4) Å and 129.6616(3)Å, V = 1155.22(6) Å3 and 1155.22(6) Å3, Dx = 1.493 and 1.476 g cm?3 and Z = 2 and 2, respectively. The crystal structures were solved by direct methods and refined by full-matrix least squares to a find R = 0.0377 and 0.0336 of for 2340 and 2402 observed reflections, respectively. 相似文献