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Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry最新文献

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Spiro-heterocycles: A convenient synthesis and antimicrobial activity of some 3-(5-aryl/aryloxymethyl-1,3,4-thiadiazol-2-yl)-spiro-cyclohexane-1',2-thiazolidin-4-ones 螺环杂环:3-(5-芳基/芳基甲基-1,3,4-噻二唑-2-基)-螺环己烷-1′,2-噻唑烷-4-酮的简便合成及其抑菌活性
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-18 DOI: 10.56042/ijcb.v60i11.50058
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引用次数: 1
Synthesis, characterization and biological evaluation of some 2-arylbenzoxazole acetic acid derivatives as potential anticancer agents 潜在抗癌药物2-芳基苯并恶唑乙酸衍生物的合成、表征及生物学评价
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-18 DOI: 10.56042/ijcb.v60i11.33016
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引用次数: 0
Derivatization and biological activity studies of 3-chloro-3-chlorosulfenyl spiro tetrahydropyran/tetrahydrothiopyran-4,2'-chroman-4'-one 3-氯-3-氯磺酰基螺旋四氢吡喃/四氢硫吡喃-4,2'-铬-4'- 1的衍生化及生物活性研究
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-18 DOI: 10.56042/ijcb.v60i11.33135
M. Hegab, Hala E M Tolana, E. Morsya, Alaa M Salehb, Farouk A Gada, Farouk M. E. Abdel-Megeida
The adducts 4a,b-7a , b have been obtained either by reducing α -chloro- β -oxosulfenyl chlorides 2a,b with iodide ion in the presence of dienes namely, 2-methyl-1,3-butadiene (isoperene), 2,3-dimethyl-1,3-butadiene, 1,2,3,4-tetrachlorocyclopentadiene, or 1,3-cyclohexadiene, respectively; or by thermolysis of oxadithiin derivatives 3a,b in the presence of the same aforementioned dienes presumably via the formation of the same intermediate A in both cases of compounds 2a,b and 3a,b . It is observed that α -chloro- β -oxosulfenyl chlorides 2a,b undergo straight forward substitution with potassium cyanide to give 8a,b . Direct oxidation of 2a,b with H 2 O 2 /AcOH affords 3,3-dichloropyran-4-ones 9a,b , while conversion of 2a,b to the sulfonamides 10a,b followed by oxidation provides 3-chloropyranones 11a,b . Antioxidant and antimicrobial evaluation of compounds 4a,b-6a,b shows moderate activiy. MIC of the derivative 6b reveals a remarkable inhibition of the pathogenic gram positive bacteria ( Staphylococcus aureus ) as well as gram negative E coli .
加合物4a,b-7a,b是在二烯即2-甲基-1,3-丁二烯(异戊二烯),2,3-二甲基-1,3-丁二烯,1,2,3,4-四氯环戊二烯或1,3-环己二烯存在的情况下,用碘离子还原α -氯- β -氧亚砜酰氯2a,b得到的;或者在上述相同的二烯存在的情况下,通过氧化二硫肽衍生物3a,b的热裂解,大概是通过在化合物2a,b和3a,b的两种情况下形成相同的中间体A。观察到α -氯- β -氧亚砜酰氯2a,b与氰化钾直接取代得到8a,b。2a,b与h2o2 /AcOH直接氧化得到3,3-二氯吡喃-4- 1 9a,b,而2a,b转化为磺酰胺10a,b,然后氧化得到3-氯吡喃酮11a,b。化合物4a、b、6a、b的抗氧化和抗菌活性评价为中等。衍生物6b的MIC显示对致病性革兰氏阳性菌(金黄色葡萄球菌)和革兰氏阴性大肠杆菌有显著的抑制作用。
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引用次数: 0
Synthesis and antimicrobial evaluation of benzothiazole linked isoxazole Schiff bases 苯并噻唑类异恶唑席夫碱的合成及抗菌性能评价
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-18 DOI: 10.56042/ijcb.v60i11.54954
G. Mallikarjun, A. Raju, J. Yadav
A new series of benzothiazole linked isoxazole Schiff base derivatives have been prepared and characterized by suitable spectroscopic methods via 1 H and 13 C NMR, ESI-MS and IR spectra. These compounds have been further screened for their antimicrobial activity against a panel of microorganisms. Among them, compounds 12d , 12g and 12l demonstrate promising antimicrobial activity against all the tested strains with MIC values ranging between 3.9 – 62.5 µg/mL. Further, compounds 12d , 12g and 12l exhibit promising antifungal activity with MIC values ranging between 7.8 – 32.5 µg/mL. Further studies are underway for determining the antifungal molecular mechanisms of these potential compounds.
制备了一系列新的苯并噻唑类异恶唑希夫碱衍生物,并通过1h和13c NMR、ESI-MS和IR光谱对其进行了表征。这些化合物已被进一步筛选其对一组微生物的抗菌活性。其中化合物12d、12g和12l对所有被试菌株均表现出良好的抑菌活性,MIC值在3.9 ~ 62.5µg/mL之间。此外,化合物12d、12g和12l表现出良好的抗真菌活性,MIC值在7.8 - 32.5µg/mL之间。进一步的研究正在进行中,以确定这些潜在化合物的抗真菌分子机制。
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引用次数: 0
Production and identification of intricate bioactive oligosaccharides from Nyctanthesarbor-tristis leaves by a combination of enzymatic, HPAEC and MALDI-TOF-MS techniques 利用酶促、HPAEC和MALDI-TOF-MS技术合成和鉴定龙参叶中复杂的生物活性低聚糖
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-18 DOI: 10.56042/ijcb.v60i11.33379
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引用次数: 0
Ultrasonicated synthesis of some potent antimicrobial aryl sulphonamides 一些强效抗菌芳基磺胺类药物的超声合成
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-01 DOI: 10.56042/ijcb.v60i10.32409
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引用次数: 0
An efficient naphthalimide based receptor for selective detection of Hg2+and Pb2+ions 一种高效的基于萘酰亚胺的Hg2+和Pb2+离子选择性检测受体
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-01 DOI: 10.56042/ijcb.v60i10.31793
Pramod D Jawale Patila, Sopan M Wagalgavea, Mohammad Al Kobaisid, Shailesh S Birajdara, Rajesh S Bhosalef, Rajita D Inglec, R. Pawarc, Sheshanath V Bhosalee, S. Bhosale
Pramod D Jawale Patil, Sopan M Wagalgave, Mohammad Al Kobaisi, Shailesh S Birajdar, Rajesh S Bhosale, Rajita D Ingle, Rajendra P Pawar, Sheshanath V Bhosale & Sidhanath V Bhosale* a Polymers and Functional Materials Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500 007, India b Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201 002, India c Department of Chemistry, Deogiri College, Aurangabad 431 005, India d Department of Chemistry and Biotechnology, FSET, Swinburne University of Technology, Hawthorn VIC 3122, Australia e School of Chemical Sciences, Goa University, Taleigao Plateau, Goa 403 206, India f Department of Chemistry, Indrashil University, Kadi, Mehsana 382 740, India E-mail: bhosale@iict.res.in
Pramod D Jawale Patil, Sopan M Wagalgave, Mohammad Al Kobaisi, Shailesh S Birajdar, Rajesh S Bhosale, Rajita D Ingle, Rajendra P Pawar, Sheshanath V Bhosale & Sidhanath V Bhosale* a聚合物和功能材料部,csir -印度化学技术研究所,海得拉巴500007,印度;科学与创新研究学院(AcSIR), Ghaziabad 201002,印度;2 .果阿大学化学科学学院,塔莱高高原,果阿403 206;2 .英德拉希尔大学化学系,梅哈萨纳卡迪382 740,印度e -mail: bhosale@iict.res.in
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引用次数: 0
A convenient metal free approach towards the synthesis of dihydropyrimidones mediated by achiral nicotinic acid without solvent 非手性烟酸无溶剂合成二氢嘧啶酮的一种便捷的无金属方法
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-01 DOI: 10.56042/ijcb.v60i10.48917
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引用次数: 1
Tomato fruit extract: an environmentally benign catalytic medium for the synthesis of isoxazoles derivatives 番茄果实提取物:一种合成异恶唑衍生物的环保型催化介质
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-01 DOI: 10.56042/ijcb.v60i10.32325
B. Popatkar, Ankita A Mane, G. Meshram
One-pot multicomponent reaction between aromatic aldehyde, hydroxylamine hydrochloride and ethyl acetoacetate/ methyl acetoacetate for the synthesis of isoxazoles derivatives by employing tomato fruit extract as a catalytic medium has been developed. Tomato fruit extract was found to be a favorable catalytic medium for the synthesis of titled compounds. Mild reaction condition, ease of separation, moderate to high yield of the product, and short reaction time makes this method more attractive over earlier reported methods for the synthesis of isoxazoles derivatives.
以番茄果实提取物为催化介质,采用芳香醛、盐酸羟胺和乙酸乙酯/乙酸甲酯一锅多组分反应合成了异恶唑类化合物。发现番茄果实提取物是合成标题化合物的良好催化介质。该方法具有反应条件温和、易于分离、产率中高、反应时间短等优点,较已有报道的合成异恶唑衍生物的方法更具吸引力。
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引用次数: 1
Synthesis and biological evaluation of azetidinone derivatives with pyrazolone moiety 吡唑啉酮类氮杂二酮衍生物的合成及生物学评价
IF 0.5 4区 化学 Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2021-11-01 DOI: 10.56042/ijcb.v60i10.32090
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引用次数: 0
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Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry
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