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Synthesis of Thienyl-Isoxazolines and in vitro Screening for their Antimicrobial Activity 噻吩基异恶唑啉类化合物的合成及体外抗菌活性筛选
Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p277
C. B. Vagish, N. Renuka, K. Kumar, H. Jayadevappa
A series of thiophene conjugated isoxazoles were efficiently synthesized using a recyclable heterogeneous catalyst Amberlyst-15 in good yields. The synthesized new compounds 5(a-j) were characterized by spectral and elemental analysis and screened in vitro for their antimicrobial potencies. Amongst the synthesized series; compounds 5c and 5j having chloro substitution on both thiophene and aromatic ring exhibited excellent inhibition against the tested species
采用可循环使用的多相催化剂Amberlyst-15合成了一系列噻吩偶联异恶唑,收率高。合成的新化合物5(a-j)通过光谱和元素分析进行了表征,并进行了体外抑菌活性筛选。在合成系列中;化合物5c和5j对噻吩和芳香烃均有氯取代,对被试物种具有良好的抑制作用
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引用次数: 2
Catalyst and Solvent Free Synthesis and Biological Activities of Imidazo[1,2-a]pyridine 咪唑[1,2-a]吡啶的无溶剂合成及生物活性研究
Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p283
G. B. Gundlewad, S. Wagh, B. R. Patil
A series of imidazo[1,2-a]pyridines were synthesized by the reaction of α-chloroacetophenone and 2- aminopyridine under catalyst and solvent free condition. The synthesized compounds were characterized by IR, 1H NMR, 13C NMR and mass spectral data. These imidazo[1,2-a]pyridines were screened for antiinflammatory activity by carrageenan induced rat hind paw edema model. Good anti-inflammatory activity was shown by few compounds. The antibacterial activity was studied against two Grampositive bacteria S. aureus and B. subtilis, two Gram-negative bacteria E. coli and S. typhi and antifungal activity against P. chrysogenum, F. moneliforme, A. flavus and A. niger. All the synthesized compounds were desplayed good antimicrobial and antifungal activities. Some of the compounds were shown higher antibacterial activity than reference drug penicillin.
以α-氯苯乙酮和2-氨基吡啶为原料,在无催化剂和无溶剂条件下合成了一系列咪唑[1,2- A]吡啶。合成的化合物通过IR、1H NMR、13C NMR和质谱数据进行了表征。通过卡拉胶诱导大鼠后足水肿模型,筛选这些咪唑[1,2-a]吡啶类化合物的抗炎活性。少数化合物显示出良好的抗炎活性。研究了其对2种革兰氏阳性菌金黄色葡萄球菌和枯草芽孢杆菌、2种革兰氏阴性菌大肠杆菌和伤寒葡萄球菌的抑菌活性,以及对金黄色葡萄球菌、单念珠菌、黄芽孢杆菌和黑芽孢杆菌的抑菌活性。所有合成的化合物都显示出良好的抗菌和抗真菌活性。其中部分化合物的抑菌活性高于对照药青霉素。
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引用次数: 1
Molecular Docking Studies of Some Natural Products AgainstSARS-CoV-2 Main Protease: Potential Therapeutic Agents for COVID-19 部分抗sars - cov -2主蛋白酶天然产物与新冠病毒潜在治疗剂的分子对接研究
Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p288
Gnanavel Sadhasivam
The severe form of respiratory disease (COVID-19), caused by SARS-COV-2 virus, has evolved into a pandemic is the defining global health crisis of our time and greatest challenge we have faced since second World War. Hence, the current situation demands an immediate need to explore all the possible therapeutic strategies that can be control spread of the diseases. We identified potent COVID-19 Mpro inhibitors based on molecular docking studies on 24 known antiviral natural compounds, which are from medicinal plants and marine sponges. The results revealed that 15 potential COVID-19 main protease inhibitors have been identified among the 24 natural compounds of plants and marine origin. The result further revealed that the selected natural products that has lower free binding energy is Halituline (-8.41 Kcal/mol). As these active compounds were extensively validated by molecular docking, the chance that at least few of these compounds could be bioactive is excellent.
由SARS-COV-2病毒引起的严重呼吸道疾病(COVID-19)已演变成一场大流行,是我们这个时代决定性的全球卫生危机,也是我们自第二次世界大战以来面临的最大挑战。因此,目前的情况迫切需要探索所有可能的治疗策略,以控制疾病的传播。通过对来自药用植物和海洋海绵的24种已知抗病毒天然化合物的分子对接研究,我们发现了有效的COVID-19 Mproinhibitors。结果显示,从24种植物和海洋来源的天然化合物中鉴定出15种潜在的COVID-19主要蛋白酶抑制剂。结果进一步表明,选择的天然产物为Halituline(-8.41 Kcal/mol),其自由结合能较低。由于这些活性化合物通过分子对接得到了广泛的验证,因此这些化合物中至少有少数具有生物活性的可能性很大。
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引用次数: 0
Stability Indicating RP-UPLC Photo-Diode Array basedMethod for Determination of Edoxaban Tosylate 稳定性指示RP-UPLC光电二极管阵列测定Tosylate依多沙班的方法
Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p270
D. Patel, B. Rana, S. Maru, A. Vyas, A. Patel, A.I. Patel, N. K. Patel
The objective of the current study was to develop a specific, precise, accurate and robust gradient stability indicating reversed-phase ultra performance liquid chromatography (RP-UPLC-PDA) assay method and validated for determination of edoxaban tosylate in API. Gradient separation was achieved on an acquity UPLC BEH C18 column (50 mm, 2.1 mm and 1.7 μm) column using mobile phase of acetoitrile:20 mM potassium dihydrogen phosphate, pH 3.0 ± 0.05 adjust with OPA at flow rate of 0.6 mL/min, the injection volume was 1 μL and the detection was carried out of 289 nm by using photodiode array detector. The drug was subjected to oxidation, hydrolysis, photolysis, and heat to apply stress condition. The method was linear in the drug concentration range of 100-300 μg/mL with correlation coefficient of 0.999. Degradation products produced as a result of stress studies did not interfere with detection of edoxaban tosylate and the assay, thus developed stability indicating method can be used for routine analysis in pharmaceutical industry.
本研究的目的是建立一种特异、精确、准确和稳健的梯度稳定性指示反相超高效液相色谱(RP-UPLC-PDA)测定原料药中tosy酸依多沙班的方法,并对其进行验证。色谱柱为UPLC BEH C18 (50 mm、2.1 mm和1.7 μm),流动相为乙二腈:磷酸二氢钾20 mm, pH 3.0±0.05,OPA调节,流速0.6mL/min,进样量为1 μL,光电二极管阵列检测器在289 nm处进行检测。对药物进行氧化、水解、光解、加热等应激反应。该方法在100 ~ 300 μg/mL范围内线性良好,相关系数为0.999。应激研究产生的降解产物不干扰tosy酸乙多沙班的检测和测定,因此所建立的稳定性指示方法可用于制药工业的常规分析。
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引用次数: 1
The Chemical Sciences' Advances on Coronavirus Disease 2019 (COVID-19) 2019冠状病毒病(COVID-19)化学研究进展
Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p286
Shovan Mondal
The novel β-coronavirus (SARS-CoV-2) causes coronavirus disease (COVID-19), which is presently a pandemic affecting numerous nations worldwide including a grim fatality of over 9 lakhs deaths till August, 2020. But even after the 9 months of the outbreak of this deadly disease, there is no particular medication or vaccine so far that can be recommended for the treatment of COVID-19 patients. Therefore, chemists are struggling to understand and dissect the viral structure of this SARS-CoV-2, unwind its pathogenesis and pinpoint its vaccines and therapies as well. In this current study, the author endeavor to sum up the ongoing advances of chemical sciences about COVID-19 focusing mainly on the developments of its therapeutics.
新型β-冠状病毒(SARS-CoV-2)引起的冠状病毒病(COVID-19)目前正在全球许多国家流行,截至2020年8月,死亡人数已超过90万人。但即使在这种致命疾病爆发9个月后,到目前为止,还没有特别的药物或疫苗可以推荐用于治疗COVID-19患者。因此,化学家们正在努力了解和剖析这种SARS-CoV-2的病毒结构,揭示其发病机制,并确定其疫苗和治疗方法。在本研究中,作者试图总结目前关于COVID-19的化学科学进展,主要关注其治疗方法的发展。
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引用次数: 0
RP-UPLC Stability Indicating Assay Method for Simultaneous Estimation ofDextromethorphan Hydrobromide and Chlorpheniramine Maleate in Tablet Dosage Form RP-UPLC稳定性指示法同时测定片剂中氢溴酸右美沙芬和马来酸氯苯那敏的含量
Pub Date : 2020-01-01 DOI: 10.14233/ajomc.2020.ajomc-p269
A. Patel, Nishith K. Patel, A. Vyas, A.B. Patel, A.I. Patel
RP-UPLC method was developed and validated for the determination of chlorpheniramine maleate and dextromethorphan hydrobromide in tablet dosage form. Reverse phase waters acquity UPLC BEH C18 (50 mm × 2.1 mm, 1.7 μm) column using isocratic mobile phase of 0.5 mL 0.1% TFA (trifluroacetic acid) in H2O:CH3CN (70:30 %v/v). The flow rate was 0.2 mL/min and 252 nm wavelength use for detection on PDA detector. The retention time of chlorpheniramine maleate was 1.2 min and 2.2 min for dextromethorphan hydrobromide. Chlorpheniramine maleate and dextromethorphan hydrobromide was subjected to stress conditions including acidic, alkaline, oxidation, photolysis and thermal degradation. The method was validated as per ICH guideline with respect to samples to specificity, precision, accuracy, linearity and robustness.
建立了反相高效液相色谱法测定马来酸氯苯那敏和氢溴酸右美沙芬片剂的含量。反相水acquity UPLCBEH C18 (50 mm × 2.1 mm, 1.7 μm)柱,采用等压流动相0.5 mL 0.1% TFA(三氟乙酸)in H2O:CH3CN (70: 30% v/v)。流速为0.2 mL/min,波长为252 nm,在PDA检测器上检测。马来酸氯苯那敏的保留时间为1.2 min,氢溴酸右美沙芬的保留时间为2.2min。对马来酸氯苯那敏和氢溴酸右美沙芬进行了酸性、碱性、氧化、光解和热降解等胁迫条件的研究。根据ICH指南对样品进行特异性、精密度、准确度、线性和稳健性验证。
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引用次数: 0
Synthesis of Some New 5-Indolylidene-4-thiazolidinone Derivatives of1,2,4-triazole as Potent Antioxidant and Antifungal Agents 新型1,2,4-三唑类5-吲哚吡啶-4-噻唑烷酮衍生物的合成
Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p214
T. Khan, R. Yadav
A series of 1,2,4-triazolyl-4-(5-indolylidene)-thiazolidinone derivatives were synthesized and screenedfor their antifungal and antioxidant activity. Among these synthesized compounds 3d, 3g showinggood antifungal activity and compounds 3b, 3d, 3f and 3h have high % antioxidant activity with lowerIC50 value of 11.21, 20.89, 17.51 and 14.05 respectively. We report the antioxidant potential of the saidclass of compound in which free radical is generated by methelenic and 2nd carbon of thiazolidinonering. The antifungal activity reported against A. niger, C. albicans and A. flavus. The antioxidantactivity of all the synthesized compounds was screened by H2O2, DPPH scavenging and byphosphomolybdenum method with respect to ascorbic acid.
合成了一系列1,2,4-三唑基-4-(5-吲哚吡啶)-噻唑烷酮衍生物,并对其抗真菌和抗氧化活性进行了筛选。合成的化合物3d、3g具有较好的抗真菌活性,化合物3b、3d、3f和3h具有较高的%抗氧化活性,其eric50值较低,分别为11.21、20.89、17.51和14.05。我们报道了该类化合物的抗氧化潜力,其中自由基是由甲基和噻唑烷化的2碳产生的。报道了对黑曲霉、白色念珠菌和黄曲霉的抑菌活性。通过H2O2法、DPPH清除法和超磷钼法对合成化合物的抗坏血酸活性进行了筛选。
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引用次数: 0
Facile Synthesis and Biological Evaluation of Cyclopropyl-PyrazoleHybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents [bmim][PF6]-水双相体系中环丙基吡唑杂合物的快速合成及生物学评价
Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p192
P. C. Burde, A. Rahatgaonkar
3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from correspondingchalcones were synthesized and evaluated for their biological activities. A convenient synthesis of alibrary of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic systemat ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which areimmiscible, has been easily recycled and reused after separation of the products without any noticeablediminution in its activity.
合成了由相应查尔酮衍生的3-环丙基-5-(4-取代)-1-苯基-4,5-二氢- 1h -吡唑,并对其生物活性进行了评价。在1-丁基-3-甲基咪唑六氟磷酸酯-水双相体系中,在常温下方便地合成了这些化合物的文库。离子液体[bmim][PF6]与水不混溶,分离产物后易于回收再利用,活性无明显降低。
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引用次数: 0
Origination Progress and Utility of Selective Estrogen Receptor Modulators in ClinicalPractice as an Efficient Substitute of Estrogen for Treating Hormone Dependent Issues 选择性雌激素受体调节剂作为雌激素的有效替代品治疗激素依赖的起源、进展及临床应用
Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p188
A. Kulshrestha, J. Pandey
The discovery, development and utility of selective estrogen receptor modulators (SERMs) are presentedin this study. As per literature review SERMs used in the treatment of estrogen hormone responsivediseases like osteoporosis, Alzheimer, angiogenesis, hyperlipidemia, coronary heart disease,atherosclerosis, endometriosis, breast cancer, post-menopausal depression, dysfunctional uterinebleeding, gynacomastia, Albright syndrome, ovarian cancer, dyspareunia, cyclical mastalgia,hypogondism and induced ovulation in sub-fertile woman, etc. Basically world wide a large no.compounds available those function as SERMs successfully or under different phase clinical trials ordiscontinued because of unwanted side effects during clinical trials. This work describes the specificreference compounds which have created a substitute of estrogen for treating hormone dependentissues.
本文介绍了选择性雌激素受体调节剂(SERMs)的发现、发展和应用。根据文献综述,SERMs用于治疗雌激素激素反应性疾病,如骨质疏松症、阿尔茨海默病、血管生成、高脂血症、冠心病、动脉粥样硬化、子宫内膜异位症、乳腺癌、绝经后抑郁症、功能失调性子宫出血、女性乳房发育不良、奥尔布赖特综合征、卵巢癌、性交困难、周期性乳房痛、性腺功能减退和诱导排卵等。基本上,世界上有很多化合物成功地或在不同阶段的临床试验中作为serm发挥作用,或在临床试验中因不必要的副作用而停用。这项工作描述了特定的参考化合物,创造了雌激素的替代品,治疗激素依赖问题。
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引用次数: 0
Synthesis, Characterization and Biological Activities of Substituted1-[Benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-ones 取代1-[苯并噻唑-(1H)-2-基]-3-苯基-丙-2-烯-1的合成、表征及生物活性
Pub Date : 2019-10-12 DOI: 10.14233/ajomc.2019.ajomc-p181
C. Anuba, T. Reji
A series of ortho and para substituted 1-[benzothiazol-(1H)-2-yl]-3-phenyl-prop-2-en-1-one derivativeswere synthesized from 2-acetyl benzothiazole and ortho and para-substituted benzaldehye using ethanolas solvent. The synthesized compounds were characterized by UV-visible, FT-IR, 1H NMR and massspectrometry. Antioxidant activities of synthesized compounds have been evaluated by DPPH freeradical scavenging activity using ascorbic acid as standard. The standard solution and 1-[benzothiazol-(1H)-2-yl]-3-phenylprop-2-en-1-ones compounds were prepared with different concentrations.Anticancer activity of 1-[benzothiazol-(1H)-2-yl]-3-phenylprop-2-en-1-one and 1-[benzothiazol-(1H)-2-yl]-3(4-chlorophenyl)prop-2-en-1-one were assigned by MTT assays.
以2-乙酰苯并噻唑和邻苯并甲醛为原料,以乙醇为溶剂合成了一系列邻苯并噻唑-(1H)-2-基]-3-苯基丙烷-2-烯-1- 1衍生物。合成的化合物通过紫外可见光谱、红外光谱、核磁共振氢谱和质谱进行了表征。以抗坏血酸为标准,通过对DPPH自由基的清除活性来评价合成化合物的抗氧化活性。制备了不同浓度的标准溶液和1-[苯并噻唑-(1H)-2-基]-3-苯基丙-2-烯-1-酮化合物。用MTT法测定了1-[苯并噻唑-(1H)-2-基]-3-苯基prop-2-en-1和1-[苯并噻唑-(1H)-2-基]-3(4-氯苯基)prop-2-en-1的抗癌活性。
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引用次数: 0
期刊
Asian Journal of Organic & Medicinal Chemistry
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