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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >3D-QSAR study, synthesis and biological evaluation of p-hydroxy benzohydrazide derivatives as antimicrobial agents
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3D-QSAR study, synthesis and biological evaluation of p-hydroxy benzohydrazide derivatives as antimicrobial agents

机译：对羟基苯甲酰肼衍生物作为抗微生物剂的3D-QSAR研究，合成和生物学评估

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Series of compounds N’-[(3-Substituted alkyl/aryl)-4-(substituted aryl)-1,3-thiazol-2-ylidene]-4- hydroxybenzohydrazide (10-37) were designed via 3D-QSAR studies. These compounds were synthesized by reacting compounds (3-9) with various substituted phenacyl bromides in presence of sodium acetate. Good yield of compounds (10-37) were obtained by established reaction. Structure of newly synthesized compounds were evaluated on the basis of spectral data. These compounds (10-37) were tested in vitro against species of grampositive bacteria, Staphylococcus aureus (ATCC 3750) and Bacillus subtilis (ATCC 6633), and gram-negative bacteria, Salmonella typhi (NCTC 786) and Escherchia coli (ATCC 25922). The minimum inhibitory concentration (MIC) was determined by the tube dilution technique using modified Muller-Hinton agar culture medium. Among the compounds tested, the compound (23) N'-[4-(2,4-dichlorophenyl)-3-(4-nitrophenyl)-1,3-thiazol-2(3H)-ylidene]- 4-hydroxybenzohydrazide had shown highest antimicrobial activity against gram-positive and gram-negative organisms while other compounds (19) N'-[3-(4-chlorophenyl)-4-(2,4-dichlorophenyl)-1,3-thiazol-2(3H)-ylidene]-4- hydroxybenzohydrazide, (16) N'-[4-(2-chloro-4-methylphenyl)-3-(4-fluorophenyl)-1,3-thiazol-2(3H)-ylidene]-4- hydroxybenzohydrazide and (25) N'-[4-(2-chloro-4-hydroxyphenyl)-3-(4-nitrophenyl)-1,3-thiazol-2(3H)-ylidene]-4- hydroxybenzohydrazide, also showed good antimicrobial activity against gram-positive and gram-negative organisms. The results of antimicrobial activity were compared with standard antibiotics (ampicillin, penicillin-G, chloramphenicol).
机译：通过3D-QSAR研究设计了一系列N'-[（3-取代烷基/芳基）-4-（取代的芳基）-1,3-噻唑-2-亚烷基] -4-羟基苯甲酰肼（10-37）。这些化合物是通过在乙酸钠存在下使化合物（3-9）与各种取代的苯甲酰溴反应来合成的。通过确定的反应获得良好产率的化合物（10-37）。根据光谱数据评估新合成化合物的结构。这些化合物（10-37）在体外针对革兰氏阳性菌，金黄色葡萄球菌（ATCC 3750）和枯草芽孢杆菌（ATCC 6633）以及革兰氏阴性菌，鼠伤寒沙门氏菌（NCTC 786）和大肠杆菌（ATCC 25922）进行了测试。使用改良的Muller-Hinton琼脂培养基，通过试管稀释技术确定最小抑菌浓度（MIC）。在测试的化合物中，化合物（23）N'-[4-（2,4-二氯苯基）-3-（4-硝基苯基）-1,3-噻唑-2（3H）-亚烷基] -4-羟基苯甲酰肼具有对革兰氏阳性和革兰氏阴性生物显示最高的抗菌活性，而其他化合物（19）N'-[3-（4-氯苯基）-4-（2,4-二氯苯基）-1,3-噻唑-2（3H） ）-亚烷基] -4-羟基苯甲酰肼，（16）N'-[4-（2-氯-4-甲基苯基）-3-（4-氟苯基）-1,3-噻唑-2（3H）-亚烷基]- 4-羟基苯并肼和（25）N'-[4-（2-氯-4-羟基苯基）-3-（4-硝基苯基）-1,3-噻唑-2（3H）-亚烷基] -4-羟基苯并肼对革兰氏阳性和革兰氏阴性生物显示出良好的抗菌活性。将抗菌活性的结果与标准抗生素（氨苄青霉素，青霉素-G，氯霉素）进行比较。

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