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本文以取代苯甲醛、苯胺及巯基乙酸为原料,合成了一系列2,3-二苯基-4-噻唑酮类衍生物,其结构经~1H NMR和MS确证。抑菌活性试验显示,所有目标化合物表现出中等抑菌活性,其中化合物4g对苹果腐烂病菌的抑菌活性最高,能达到62.7%。构效关系研究表明在2,3-二苯基-4-噻唑酮的苯基上引入甲基能增强活性。 相似文献
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以取代苯硫酚和顺丁烯二酸酐为原料,经迈克尔加成反应制得2-羧基-硫色满酮衍生物(2a~2d); 2a~2d分别与氨基硫脲反应制得2-(5-氨基-1,3,4-噻二唑-2-基)硫色满-4-酮衍生物(3a~3d); 3a~3d与酰氯经酰化反应合成了14个新型的含1,3,4-噻二唑的硫色满酮衍生物(5a~5n),其结构经1H NMR, 13C NMR和HR-ESI-MS表征。采用微量稀释法测定了5a~5n的抗真菌活性。结果表明:部分化合物对絮状表皮癣菌和总状毛霉菌有较好的抑制活性,优于阳性对照药氟康唑。 相似文献
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为寻找具有杀菌活性的三唑类先导化合物,采用活性亚结构拼接方法,将香豆素环和硫醚结构单元引入到三唑类化合物分子中,合成一系列未见文献报道的新型含香豆素环和硫醚结构的三唑类衍生物。经~1H NMR、~(13)C NMR、IR、MS和元素分析对所合成化合物的结构进行了表征。初步生物活性测试表明,部分目标化合物在试验浓度下具有一定的抑菌活性。 相似文献
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新型1,5-二苯基-1,4-戊二烯-3-酮肟酯类化合物的合成及其抑菌活性研究 总被引:1,自引:0,他引:1
以1,5-二苯基-1,4-戊二烯-3-酮肟和酰氯为原料, 合成了15个新型的1,5-二苯基-1,4-戊二烯-3-酮肟酯类化合物, 通过元素分析, IR, 1H NMR, 13C NMR等对其结构进行了表征. 初步生物活性试验结果表明, 在50 mg•L-1浓度下, 化合物3i和3o对小麦赤霉病菌抑制率分别为51.1%和 53.4%, 与对照药剂恶霉灵抑制活性相当. 相似文献
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本文以2-硫代乙内酰脲、取代苯甲醛、碘甲烷、吡啶甲胺等为原料,经Knoevenagel缩合、甲基化和取代反应,合成了一系列5-取代苯亚甲基-2-[(吡啶-3-基)甲氨基]-1H-咪唑-4(5H)-酮(3a~3i),其结构经IR、~1H NMR、~13C NMR和HRMS确证。初步抑菌活性试验表明,在药剂浓度为100μg/m L时,目标化合物对灰霉菌均有中等抑制活性,抑制率为69.5%~83.2%;在相同浓度下大部分化合物对菌核菌有较高的抑制活性,抑制率为87.9%~100%,其活性高于对照药三唑酮和百菌清。 相似文献
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M. E. Azab E. A. Kassab M. A. El-Hashash R. S. Ali 《Phosphorus, sulfur, and silicon and the related elements》2013,188(3):610-625
2-Phenylamino-6,8-dibromo-4H-3,1-benzoxazinone has been reacted with nitrogen nucleophiles, such as hydrazine hydrate, amines, and formamide, yielding 4(3H)quinazolinone derivatives; and with sulfur nucleophiles producing the corresponding thioesters. The behavior of aminoquinazolinone and 4(3H)quinazolinone towards some carbon electrophiles under different conditions has been studied. 相似文献
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FENGRun-liang GONGPing FANGLin HONGWei 《高等学校化学研究》2005,21(2):177-182
Ten new erythromycin antibacterial agents containing amidino group were designed and synthesized from erythromycin via oximation, reduction and condensation. Their structures were confirmed by MS and ^13C NMR; the synthetic condition(reaction medium)was explored; and their in vtiro antibacterial activities were tested. Compound HMA-3 showed antibacterial activity against staphylococcus aureus, which is equivalent to that of erythromycin A. Compounds HMA-8 and HMA-4 also showed an antibacterial activitiy. But no compound showed bactericidal activity. 相似文献
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A convenient synthesis of 3-substituted pyrazole derivatives by a mixed anhydride method using i-butylchloroformate and N-methylmorpholine at ?20 °C in tetrahydrofuran and study of in vitro antibacterial activities of the prepared compounds against Staphylococcus epidermidis, Bacillus subtilis, Pseudomonas aeruginosa, and Proteus valguris by agar-diffusion method were carried out. The results suggested that the products 4a, 4b, and 4c exhibited moderate to feeble inhibition against all test bacteria at greater concentration but 4d was best against Staphylococcus epidermidis (22 mm) and worst against Pseudomonas aeruginosa (16 mm) at the greatest concentration (2.5 mg/ml), and the activities decreased with decrease in concentration. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.] 相似文献
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以苯胺为原料,通过肟化、环合生成二氢吲哚-2,3-二酮,再对其进行N-烷基化、亲核加成和磺酰化反应得到目标化合物5a~5g和7a~7e。通过1H NMR、13C NMR确认其结构。采用噻唑蓝(MTT)法测试了目标化合物对乳腺癌细胞MDA-MB-231、鼠黑色素瘤细胞B16、鼠结肠癌细胞CT26三种肿瘤细胞的体外抑制活性。结果表明,化合物7d、7e具有明显的肿瘤细胞毒活性,其中化合物7d对MDA-MB-231的细胞毒活性比阳性药五氟尿嘧啶更强,IC50为4.63±0.14μmol/L。本文结果可为进一步研究具有肿瘤细胞毒活性的吲哚酮类衍生物提供参考。 相似文献
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ZHAI Xin ZHAO Yan-fang WANG Jia HONG Wei HUANG Liang GONG Ping 《高等学校化学研究》2006,22(4):459-464
IntroductionOxazolidinones, exemplified by linezolid, are anovel class of totally synthetic antibacterial agents withactivities against a variety of clinically important sus-ceptible and resistant Gram-positive pathogenic bacteriasuch as methicillin-resis… 相似文献
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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
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XU Boxuan DING Xiudong WU Yachuang CUI Lei QIAN Ping WANG Di ZHAO Yanfang 《高等学校化学研究》2018,34(1):51-56
A series of novel oxazolidinone derivatives containing nitro heteroaromatic moiety was synthesized and characterized by means of 1H NMR and MS spectra. All target compounds were evaluated for their in vitro antibacterial activities against S.au 29213, methicillin-resistant Staphylococcus aureus(MRSA) and vancomycin-resistant Enterococcus(VRE) by minimum inhibitory concentration(MIC) assay. Most of them exhibited antibacterial activity against S. au 29213, MRSA and VRE. Among them, compounds 10e and 10f displayed better activity than the control. 相似文献