共查询到20条相似文献,搜索用时 15 毫秒
1.
Yuanyuan Zheng Xuesong Wang Sumei Gao Min Ma Guiming Ren Huabing Liu 《Natural product research》2015,29(19):1804-1810
In the present study, using chalcone as a lead compound, a series of its derivatives (compounds 1–30) were designed and synthesised. Their activity of anti-pathogenic fungi of plants has been evaluated. It is found that these compounds have good antifungal activity against Sclerotinia sclerotiorum, Helminthosprium maydis, Botrytis cinerea, Rhizoctonia solani and Gibberella zeae. Among them, the inhibition of growth for compound 30 against S. sclerotiorum showed 89.9%, with the median effective concentrations (EC50) of 15.4 μg mL? 1. The inhibition of growth for compounds 28, 29 and 30 at a concentration of 100 μg mL? 1 against H. maydis is 90.3%, 90.7% and 91.1%, with EC50 of 15.1, 18.3 and 18.1μg mL? 1, respectively. 相似文献
2.
Qing Jie Zhao Yan Song Hong Gang Hu Shi Chong Yu Qiu Ye Wu School of Pharmary Second Military Medical University Shanghai China 《中国化学快报》2007,18(6):670-672
Twenty-three 1 -(1H-1,2,4-triazole-1 -y1)-2-(2,4-difluorophenyl)-3-(iV-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase. In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole. 相似文献
3.
Shi-Ping Zhu Wen-Ya Wang Kun Fang Zheng-Gang Li Guo-Qiang Dong Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang Chun-Quan Sheng 《中国化学快报》2014,25(2):229-233
The incidence of invasive fungal infections is increasing rapidly. Clinically available antifungal agents suffer from limited efficacy and severe resistance. There is an urgent need to discover antifungal lead compounds with novel chemical scaffold. On the basis of our previously identified tetrahydrocarbazole antifungal leads, the structure-activity relationship was further explored by modifying the scaffold and the side chains. Several targeted compounds showed potent activity against Candida species. Particularly, compound 13i showed better antifungal activity than the lead compound, which can be used as a good starting point for further optimization. 相似文献
4.
A series of heterocycle containing amide derivatives (1–28) were synthesised by the combination of acyl chlorides (1a, 2a) and heterocyclic/homocyclic ring containing amines, and their in vitro antifungal activity was evaluated against five plant pathogenic fungi, namely Gibberella zeae, Helminthosporium maydis, Rhizoctonia solani, Botrytis cinerea and Sclerotinia sclerotiorum. Results of antifungal activity analysis indicated that some of the products showed good to excellent antifungal activity, as compound 2 showed excellent activity against G. zeae and R. solani and potent activity against H. maydi, B. cinerea and S. sclerotiorum, and compounds 1, 8 and 10 also displayed excellent antifungal potential against H. maydi, B. cinerea and S. sclerotiorum and good activity against R. solani when compared with the standard carbendazim. 相似文献
5.
Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase (CYP51) 总被引:1,自引:2,他引:1
Zhi Gang Dan Jun Zhang Shi Chong Yu Hong Gang Hu Xiao Yun Chai Qing Yan Sun Qiu Ye Wu 《中国化学快报》2009,20(8):935-938
A series of 1-(1H-1,2,4-triazole-1-y1)-2-(2,4-difluorophenyl)-3-(N-isoproyl-N-substituted-amino)-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase(CYP51).Their structures were confirmed by MS and ~1H NMR.In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi.The results showed that all title compounds exhibited activity against fungi tested to some extent.Compounds 3c,3d,7a,7b and 7c exhi... 相似文献
6.
Synthesis and fungicidal activity of novel 1,2,4-triazole derivatives containing a pyrimidine moiety
Wen-Neng Wu Yang-Ming Jiang Qiang- Fei Hai-Tang Du 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):1171-1175
AbstractA series of novel 1,2,4-triazole derivatives containing a pyrimidine moiety were synthesized and their fungicidal activities were evaluated. The preliminary biological test indicated that some of the target compounds exhibited moderate to good fungicidal activities against the tested plant pathogenic fungi compared with the commercial agent. Among them, compounds 9n and 9o exhibited excellent antifungal activity against Phompsis sp., with the half-maximal effective concentration (EC50) values of 25.4 and 31.6?μg/mL, which were even better than the commercial agent of Pyrimethanil (32.1?μg/mL). Meanwhile, compound 9o showed better fungicidal activities against B. dothidea and B. cinerea with 40.1 and 55.1?μg/mL, respectively, in comparison with that of commercial Pyrimethanil (57.6 and 62.8?μg/mL). 相似文献
7.
A series of novel 1,3,4-thiadiazole derivatives based on benzisoselenazolone were synthesized and evaluated for their cytotoxicity in vitro against human liver cancer cell SSMC-7721,human breast cancer cell MCF-7 and human lung cancer cell A549 by CCK-8 assay.The results showed mat compounds 7e,7f,7h,7k,71 and 7m displayed good cytotoxicity against MCF-7 cell lines.Compound 71 exhibited the most potent antitumor activities among the tested compounds. 相似文献
8.
A series of structurally novel 1,3,4-oxadiazole thioether derivatives(6a-6z) containing a 6-fluoroquinazolinylpiperidinyl moiety were designed and synthesized using pharmacophore hybrid approach,and their structures were fully characterized by ^1H NMR,13C NMR and HRMS spectra.Among them,the structure of compound 6 d was further corroborated via single-crystal X-ray diffraction analysis.In vitro antibacterial bioassays showed that compounds 6 a,6 g,6 u and 6 v possessed EC50 values of 30.4,30.6,27.5 and 26.0 μg/mL against phytopathogenic bacterium Xanthomonas oryzae pv.oryzae,respectively,which were significantly superior to that of commercially-available bactericide Bismerthiazol(85.1 μg/mL).Moreover,in vitro antifungal bioassays indicated that seven compounds demonstrated broad-spectrum fungicidal acitivties against six types of phytopathogenic fungi at 50 μg/mL.The present work showed the potential of 1,3,4-oxadiazole thioether derivatives carrying a 6-fluoroquinazolinylpiperidinyl moiety as effective antimicrobial agents for crop protection,deserving further investigations in the future. 相似文献
9.
Jian Ta Wang Ying Wang Ji Quan Zhang Xing Cui Yi Zhang Gao Feng Zhu Lei Tang 《中国化学快报》2011,22(4):409-412
A series of diclofenac derivatives were synthesized.The insulin-sensitizing activity of 28 new compounds was evaluated in 3T3- L1 cells.The compounds 10a and 10f exhibited similar insulin-sensitizing activity with positive drug rosiglitazone. 相似文献
10.
Yuan-Yuan Xu An-Ran Qian Xu-Feng Cao Chen-Yu Ling Yong-Bing Cao Rui-Lian Wang Yi-Su Li Yu-She Yang 《中国化学快报》2016,27(5):703-706
A series of novel triazole derivatives containing γ-lactam were designed and synthesized, and their structures were confirmed by ~1H NMR,~(13)CNMR and HRMS. The in vitro antifungal activities of the target compounds were evaluated. The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition,the docking model for 2A and CYP51 was investigated. 相似文献
11.
In order to find novel antifungal agents with good activity and aqueous solubility,a series of SYN-2869 analogues containing a pyridine ring were synthesized and evaluated for their in vitro antifungal activity and water solubility.The results indicated that some compounds showed potent activity against six pathogenic fungi.In particular,the analogue 17a having an isobutyl substitution on the triazolone exhibited significant broad spectrum antifungal activity.In addition,the water solubility of compound 17a was sufficiently improved over SYN-2869. 相似文献
12.
Mei Ren Yun Gen Xu Na Wen Da Yong Zhang Wei Yi Hua 《中国化学快报》2007,18(5):539-541
A series of novel derivatives of ligustrazine linked with substituted benzoyl guanidine were synthesized. These compounds have not been reported in literature, and their chemical structures were confirmed by IR, 1H NMR and MS. The results of NHE1 inhibitory activity test showed that compounds I2, I3, I4, I6, and I7 possess more potent NHE1 inhibitory activity than cariporide. 相似文献
13.
《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
14.
15.
Nine new fluorine-containing phenylimino-thiazolidines derivatives were prepared. The structures of all compounds were confirmed by 1H NMR, mass and high resolution mass spectroscopy. The antifungicidal activities of the title compounds on Phytophthoza capsici L., Pyriculazia ozyzae C., Fusazium spp. at 100 ppm were screened. 相似文献
16.
Nine new fluorine-containing phenylimino-thiazolidines derivatives were prepared. The structures of all compounds were confirmed by NMR, mass and high resolution mass spectroscopy. The antifungicidal activities of the title compounds on Phytophthora capsici L., Pyricularia oryzae C, Fusarium spp. at 100 ppm were screened. 相似文献
17.
A series of novel acylide derivatives have been synthesized from clarithromycin A via a facile procedure. The C-3 modifications involved replacing the natural C-3 cladinosyl group in clarithromycin core with different aryl-piperzine sidechain via chemical synthesis. Meanwhile a distinctive intermediate with 10,11-epoxy moiety was obtained. The structure and stereochemistry of this novel structure were confirmed via NMR and X-ray crystallography. Potential anti-bacterial activities against both Grampositive and Gram-negative bacteria were reported. Because of existence of C10,11-epoxide, these derivatives can be used as intermediates for further structural modification. 相似文献
18.
<正>A series of new 4-substituted benzoxazolone derivatives were synthesized according to a convenient method,their anti-inflammatory and analgesic activities in vivo were evaluated.All of them were new compounds,the structures of all the synthesized compounds were confirmed by ~1H NMR,~(13)C NMR,ESI-MS and HR-MS.Most of the compounds exhibited anti-inflammatory activity. 相似文献
19.
20.
To improve the aqueous solubility of an itraconazole analogue,compound 1(YL-24),a series of novel prodrugs were synthesized.Among these prodrugs,the phosphate disodium salt compound 7 exhibited excellent aqueous solubility(9.8 mg/mL) at near-neutral pH and sufficient stability in buffer solutions, along with favorable pharmacokinetic profiles.In particular,compounds 1 and 7 provided moderate survival efficacy in murine systemic Candida albicans SC5314 infection model,but their efficacy was weaker than that of fluconazole. 相似文献