磺胺的噻二嗪硫酮衍生物的合成及抑菌活性研究

利用药物化学骈合理原理设计并合成了一系列新的３，５－二取代１，３，５－噻二嗪－２－硫酮类化合物，基结构被红外光谱与紫外光谱及元素分析所证实，抑菌活性试验显示良好的抑菌活性。     

噻二嗪硫酮衍生物的合成及抑菌活性研究

合成了４种新的３－苯基－５－取代的－四氢－２Ｈ－１，３，５－二噻一嗪－２－硫酮类化合物，其结构被红外光怀紫外光谱及元素分析所证实，并进行了初步抑菌活性试验。     

磺胺的噻二嗪硫酮衍生物的合成及抑菌活性研究

利用药物化学骈合原理设计并合成了一系列新的3,5-二取代1,3,5-噻二嗪-2-硫酮类化合物,其结构被红外光谱与紫外光谱及元素分析所证实,抑菌活性试验显示了良好的抑菌活性.     

噻二嗪硫酮类抑菌衍生物的合成

通过用相应的脂肪胺与氢氧化钾、二硫化碳反应 ,然后加入甲醛和对氨基苯甲酸 ,共合成了5个新的 1 ,3 ,5 噻二嗪 2 硫酮类抑菌化合物 ,并对这 5个化合物进行了元素分析和紫外、红外、氢核磁的谱图分析 ,且与结构相符     

噻二嗪硫酮衍生物的抗微生物活性

为筛选新的杀菌，抑霉药物，本文报导了１５种标准化合物对６种细菌和２种霉菌的生物活性，结果显示此类化合物对所试细菌的抑菌环直径多在１５ｍｍ以上，其中Ｎｏ３和Ｎｏ４的抑菌环直径均在２０ｍｍ以上；说明此类化合物有较强的生物活性，相比而言，对革兰氏阳性菌的抑制作用稍弱于对革兰氏阴性菌的作用，而对霉菌的作用较弱，表明有望从此类化合物中筛选出临床的新型抗菌药物。     

噻二嗪硫酮衍生物的抗微生物活性

为筛选新的杀菌、抑霉药物,本文报导了１５种标题化合物对６种细菌和２种霉茵的生物活性。结果显示此类化合物对所试细菌的抑菌环直径多在１５ｍｍ以上,其中Ｎｏ３和Ｎｏ４的抑菌环直径均在２０ｍｍ以上;说明此类化合物有较强的生物活性,相比而言,对革兰氏阳性菌的抑制作用稍弱于对革兰氏阴件菌的作用．而对霉菌的作用则较弱。表明有望从此类化合物中筛选出可用于临床的新型抗菌药物。关键词     

硫色满酮Mannich碱衍生物的合成及其抗真菌活性

设计并合成了 12个硫色满酮的Mannich碱衍生物 ,12个化合物均未见文献报道 ,其结构经红外光谱、核磁共振氢谱及元素分析结果证实 .体外抑菌试验表明 :12个化合物均有不同程度的抑菌活性 ,其中化合物 (1)与对照品克霉唑相当 .     

四氢-2H-1,3,5-噻二嗪-2-硫酮类化合物的合成与抗菌活性

报道10个四氢-2H-1,3,5-噻二嗪-2-硫酮类化合物的合成与体外抗菌试验,其中7个化合物为新化合物。经元素分析、紫外光谱、红外光谱及核磁共振氢谱等确证它们的结构,并试验它们对6种细菌和2种霉菌的生物活性。结果显示此类化合物的抗菌活性显著强于临床上正在使用的磺胺嘧啶钠注射液,而稍弱于诺氟沙星注射液。对革兰氏阴性菌的抑制作用强于对革兰氏阳性菌的作用,对霉菌的活性很弱。     

硫色酮衍生物1,1—二氧化物的合成及其抑真菌活性的研究

报道了硫色酮衍生物１，１－二氧化物的合成路线，合成了七个化合物，测定了它们的抗真菌活性，结果表明，对供试的五种真菌均有不同程度的抗菌活性。     

6，8—二氯硫色满酮衍生物的合成及抗真菌活性

本文设计并合成了一系列6,8－二氯硫色满酮衍生物,其中12个为未见文献报道的新化合物,对所合成的化合物进行了体外抑菌活性试验,其结果表明某些化合物对6种供试真菌有较好的抑制作用。     

红霉素衍生物的合成及抗菌活性

目的设计、合成红霉素4″-氨基甲酸酯衍生物,研究其抗菌活性。方法以阿奇霉素为起始原料,经1, 1′-羰基二咪唑处理以及胺解反应、曼尼希反应制备目标化合物,并以金黄葡萄球菌为试验菌进行体外抗菌活性研究。结果共合成了9个目标化合物,其结构经IR、13C NMR、1HNMR和元素分析得以证实,经体外抗菌活性试验发现化合物F-3和F-4显示较好抗金黄色葡萄球菌活性,所有化合物无体外杀菌活性。结论说明吡咯烷基或哌啶基可能有利于提高抗菌活性。     

3-取代-5-羧苯基-四氢-1,3,5-噻二嗪-2-硫酮类化合物的合成

报道了6个新的具抗菌活性的3-取代-5-羧苯基-四氢-1,3,5-噻二嗪-2-硫酮化合物的合成,即用不同的伯胺与氢氧化钾和二硫化碳反应,再与甲醛和对氨基苯甲酸作用而得.     

Synthesis and Antifungal Activities of New Pyrazole Derivatives via 1,3-dipolar Cycloaddition Reaction

A series of cycloadducts--pyrazoles via 1,3-dipolar cycloaddition reactions of generated nitrilimines with N-(4-chloro-2-fluorophenyl)maleimide were described. The novel compounds synthesized were characterized by ¹H NMR, MS, and elemental analysis. The fungicidal tests showed that most of the title compounds exhibit significant fungicidal activities against Corynespora cassiicola.     

Synthesis and Biological Activities of Some Benzimidazolone Derivatives

The reaction of 5-nitrobenzimidazolone with phenoxyethyl bromide in presence of potassium carbonate in dimethyl formamide obtained 6-nitro-1,3-bis(2-phenoxyethyl)-1,3-dihydro-2H-benzimidazol-2-one. It was reduced using stannous chloride to get 6-amino -1,3-bis(2-phenoxyethyl)-1, 3-dihydro-2H-benzimidazol -2-one, which was further treated with aromatic sulphonyl chloride to obtain benzimidazolone derivatives, 6a-k. These compounds were tested for antibacterial, antituberculosis and antifungal activity. Most of them have shown very good activity against some gram positive and gram negative microorganisms and fungal strains. Some of them have shown moderate activity against Mycobacterium tuberculosis.     

Synthesis and Antimicrobial Activity of 5-Imidazolinone Derivatives

Several 4-arylidene-2-phenyl-1-(2,4,5-trichlorophenyl)-1H-imidazol-5(4H)-ones (4a-q), N-(4-benzylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-4-chlorobenzamides (5a-o) and N-(4-benzylidene-5-oxo-2-phenyl-4,5-dihydroimidazol-1-yl)-2,4-dichlorobenzamides (6a-m) were prepared. All newly synthesized compounds have been tested for their antibacterial activity against gram (+)ve and gram (−)ve bacteria and also on different strains of fungi. Introduction of OH, OCH₃, NO₂, Cl and Br groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.     

Synthesis and Antimicrobial Activity of Some New Quinazolin-4(3H)-one Derivatives

A new series of 6-iodo-2-phenylquinazolin-4(3H)-one derivatives was prepared and screened for antimicrobial activity. The thioureide derivatives 4–6, the carbohydrazide derivatives 19–21 and 24 displayed excellent broad-spectrum antimicrobial activity. Some compounds showed moderate activity against Candida albicans and Pseudomonas aeruginosa. None of the tested compounds was as active as the reference standard drugs ampicillin and clotrimazole. The detailed synthesis, antimicrobial activity, and the minimum inhibitory concentrations (MIC) are reported.     

2, 3-Bis(5-alkyl-2-thiono-1, 3, 5-thiadiazin-3-yl) propionic acid: one-pot domino synthesis and antimicrobial activity

In a search for promising antibacterial and antifungal compounds, two new series of 2, 3-bis(5-alkyl-2-thiono-1, 3, 5-thiadiazin-3-yl)propionic acid 1 and their corresponding N, N-dimethylpropionamide 6 have been synthesized. The reaction of 2, 3-diaminopropionate 3, carbon disulfide, formaldehyde, and the appropriate alkyl amines furnished the title compound 1. N, N-dimethylpropionamides 6 were obtained by the reaction of 1 with dimethyl amine in the presence of POCl(3). The newly prepared compounds were screened in vitro against certain strains of Gram-positive and Gram-negative bacteria and compared with nalidixic acid and ciprofloxacin. Moreover, the title compounds were tested for their antifungal activity in vitro against Candida albicans, phytopathogenic, Penicillum expansum and Trichoderma hazianum, and aflatoxin-producing Aspergillus flavus. These compounds exhibit varied activity against the tested pathogenic bacteria and remarkable inhibitory effects on growth or sporulation of some of the tested fungal species.     

新型巯基蛋白酶抑制剂THTT衍生物的抗微生物活性

目的：研制针对各种耐药病原微生物的有效新药，合成一类新的含有四氢－2H－1，3，5－噻二嗪－2－硫酸环的化合物（Tetrahydro-2H-1,3,5-thiadiazine-2-thione,THTT)，并研究其抗微生物活性。方法：用5种G^ 菌和1种对10种新合成的化合物进行了生物活性实验。结果：大部分化合物对供试菌株均具有不同程度的抑制作用，对常见肠道菌如大肠杆菌，志贺菌对甲型副伤寒沙门菌，伤寒沙门菌的力活性较好；而对G^ 菌的金黄色葡萄球菌的力活性最强。其中化合物1，7，8，9，11，13抗菌活性较好。与阳性对照药物磺胺嘧啶钠注射液相比，10种化合物的抗菌活性均强于对照物。但是，铜绿假单胞菌对10种化合物均不敏感。结论：大部分化合物对所选常见致病菌有较好的抑菌活性，同时表明有较宽的抗菌谱，该类化合物值得进一步深入研究。     

Synthesis of Pyrimidine Incorporated Piperazine Derivatives and their Antimicrobial Activity

Thiophene substituted chalcones (1a-e) were cyclised with thiourea in presence of potassium hydroxide to get 4-substituted-6-(thiophen-2-yl)pyrimidine-2-thiols (2a-e) which were then stirred with methyl iodide to obtain 4-substituted-2-(methylsulfanyl)-6-(thiophen-2-yl)pyrimidines (3a-e). Compounds (3a-e) were refluxed with different N-methylpiperazine and N-phenylpiperazine to afford 4-substituted-2-(4-methylpiperazin-1-yl)-6-(thiophen-2-yl)pyrimidines (4a-e) and 4-substituted-2-(4-phenylpiperazin-1-yl)-6-(thiophen-2-yl)pyrimidines (5a-e). The structures of all the newly synthesised compounds 4b, 4d, 5a and 5b showed good antibacterial activity at 40μg/mlconcentration. Compounds 4a, 4d, 4e, 5c and 5e showed significant antifungal activity at 40 μg/ml concentration compared with standard drugs.