Pharmaceutical Chemistry Journal最新文献

Radiocomplexation, Quality Control and Bioevaluation of [99mTc]tricarbonyl Rolipram for Brain Imaging in Mice 用于小鼠脑成像的[99m锝]三羰基罗利普仑的放射性络合、质量控制和生物评估

IF 0.8 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-10 DOI: 10.1007/s11094-024-03190-2

M. Sanad, H. Eyssa, S. M. Abd-elhaliem, A. B. Farag, S. A. Bassem

引用次数: 0

Radiocomplexation, Quality Control and Bioevaluation of [99mTc]tricarbonyl Rolipram for Brain Imaging in Mice 用于小鼠脑成像的[99m锝]三羰基罗利普仑的放射性络合、质量控制和生物评估

IF 0.8 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-10 DOI: 10.1007/s11094-024-03190-2

M. Sanad, H. Eyssa, S. M. Abd-elhaliem, A. B. Farag, S. A. Bassem

引用次数: 0

Synthesis of Benzoic Acid Esters and Their Antimicrobial Activity 苯甲酸酯的合成及其抗菌活性

IF 0.8 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-09 DOI: 10.1007/s11094-024-03186-y

N. V. Groza, T. A. Yarkova, N. N. Gessler, A. V. Rozumiy

引用次数: 0

Cytotoxic and Antioxidant Activity of a Series of 4-Methylene-1,3-Dioxolane Acetals 一系列 4-亚甲基-1,3-二氧戊环乙酸酯的细胞毒性和抗氧化活性

IF 0.8 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-09 DOI: 10.1007/s11094-024-03187-x

G. Z. Raskildina, D. V. Ishmetova, S. A. Sokov, A. A. Golovanov

引用次数: 0

Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning 将 99MTc-Montelukast 放射性合成作为肺部扫描的新型潜在放射性药物模型

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-07 DOI: 10.1007/s11094-024-03179-x

M. A. Motaleb, I. T. Ibrahim, H. A. Shweeta, S. M. Abd El-Halem

{"title":"Radiosynthesis of 99MTc-Montelukast as a Novel Potential Radiopharmaceutical Model for Lung Scanning","authors":"M. A. Motaleb, I. T. Ibrahim, H. A. Shweeta, S. M. Abd El-Halem","doi":"10.1007/s11094-024-03179-x","DOIUrl":"https://doi.org/10.1007/s11094-024-03179-x","url":null,"abstract":"Montelukast, a leukotriene receptor antagonist with a high affinity and selectivity for the cysteinyl leukotriene receptor type-1, was radiolabeled with 99mTc using a direct tagging procedure. The processing parameters—amounts of both montelukast and reducing agent, pH of the reaction mixture, reaction temperature, time of reaction, and in vitro stability of the 99mTc-montelukast complex—were thoroughly investigated. The 99mTc-montelukast complex had a percent radiolabeling yield of 92 ± 0.23 and an in vitro stability of 6 hours. According to biological distribution studies, the maximum uptake of 99mTc-montelukast complex for the lungs was 35.89 ± 1.03 % injected activity/gm tissue at 15 minutes following injection and remained high in the lungs for another hour (15.88 ± 0.39%), whereas the washout of mice organs appeared to primarily occur via the urinary tract. Because the 99mTc-montelukast complex is not a blood product, it is safer. To summarize, the 99mTc-montelukast complex is a new radiopharmaceutical that might be utilized for perfusion imaging of the lungs that is both safer and more useful.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.9,"publicationDate":"2024-08-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948674","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

High-Performance Liquid Chromatography Assay for Ondansetron in Bulk and Pharmaceutical Formulations 散装和药物制剂中昂丹司琼的高效液相色谱分析

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-06 DOI: 10.1007/s11094-024-03195-x

Saba Razzak, Somia Gul

{"title":"High-Performance Liquid Chromatography Assay for Ondansetron in Bulk and Pharmaceutical Formulations","authors":"Saba Razzak, Somia Gul","doi":"10.1007/s11094-024-03195-x","DOIUrl":"https://doi.org/10.1007/s11094-024-03195-x","url":null,"abstract":"Ondansetron (OND), a serotonin type-3 receptor antagonist exhibits antiemetic activity by blocking both centrally as well as peripherally. It is one of the most common empiric options for the treatment of nausea and vomiting of different etiologies such as chemotherapy-induced nausea vomiting (CINV), radiation-induced NV, postoperative NV as well as off-labeled drugs used in pregnancy. For the quantitative determination of ondansetron in bulk and pharmaceutical dosage form, a simple reversed-phase HPLC method was successfully developed and validated. Nucleodur 100 – 10 C18 column (216 mm, 4.6 mm, and 5 μm) was used. The solvent system was methanol: water: acetonitrile (80:15:5, v/v/v), whose pH was adjusted to 2.8 by using a few drops of ortho-phosphoric acid, delivered at a flow rate of 1ml/min. Eluents were detected at a wavelength of 308 nm. The proposed method was found to be specific, sensitive and linear (R2 > 0.9999) within a desired range of 0.15 – 5 μg/ml, accurate (99.61 – 100.23%), precise (0.004 – 0.2%), and showed good robustness and ruggedness. The limit of detection and quantification was 0.27 μg/ml and 0.8 μg/ml, respectively. A statistically paired sample t-test for the analysis of precision was employed. The proposed method was applied to different marketed formulations.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948676","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Attenuation of Cardiomyocyte Hypertrophy Via Inhalation of Isosteviol-Loaded Exosome in Mice 在小鼠体内吸入异甾烷醇外泌体可减轻心肌细胞肥大

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-06 DOI: 10.1007/s11094-024-03183-1

Haihua Guo, Meng Li, Changhong Ke, Yue Lin, Zizhao Zhai, Guanlin Wang, Suqing Zhao, Tingyuan Pang

{"title":"Attenuation of Cardiomyocyte Hypertrophy Via Inhalation of Isosteviol-Loaded Exosome in Mice","authors":"Haihua Guo, Meng Li, Changhong Ke, Yue Lin, Zizhao Zhai, Guanlin Wang, Suqing Zhao, Tingyuan Pang","doi":"10.1007/s11094-024-03183-1","DOIUrl":"https://doi.org/10.1007/s11094-024-03183-1","url":null,"abstract":"Isosteviol has been investigated with a cardio-treating effect on cardiomyocyte hypertrophy. However, its hydrophilicity suppressed its efficient cellular uptake for targeting the heart. Exosomes were seen as delivery vesicles with excellent histocompatibility; thus, an isosteviol-loaded exosome (Istv-exo) was prepared for cardiopulmonary delivery in this study. For in vivo evaluation, the Istv-exo and isosteviol saline solution was used for inhalation or intragastric administration on Sprague–Dawley rats for an assay of dynamic distribution. The higher biodistribution of Istv-exo in the lung and heart has been confirmed by the dynamic content curve. Istv-exo/isosteviol solution was administered by inhalation/intragastrically to Myh6-/- mice, a cardiomyocyte hypertrophy model, to explore the therapeutic effect. The heart function of the mice was measured using echocardiography and in situ imaging was used to analyze the morphology of the heart. The higher level of left ventricular internal dimension, ejection fraction, and cardiac output in echocardiography indicated that Istv-exo enhanced improvement of myocardial function. The attenuation of cardiomyocyte hypertrophy in mice treated with inhalation of Istv-exo determined that it contributed to the reversal of pathological hypertrophy phenotypes. Wheat germ agglutinin staining confirmed that cardiomyocyte hypertrophy was reversed to varying degrees in the Istv-exo, intragastrical isosteviol, and positive control groups. Hematoxylin and eosin staining exhibited the enlarging left ventricular and thinning ventricular wall of the treated mice. Drastically less collagen fiber was observed in the positive control group and Istv-exo group. The inhalation administration of isosteviol-loaded exosomes may be better in therapy for cardiomyocyte hypertrophy than intragastric usage of isosteviol.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948677","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

An Efficient Catalyst-Free One-Pot Synthesis and In Vitro Biological Activity Evaluation of Novel Isoquinoline Derivatives of Fatty Acids 新型脂肪酸异喹啉衍生物的高效无催化剂一锅合成及体外生物活性评估

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-06 DOI: 10.1007/s11094-024-03189-9

Razieh Rahimizadeh, Akbar Mobinikhaledi, Hassan Moghanian, Mahta Mobinikhaledi, Seyedeh sara Kashaninejad

{"title":"An Efficient Catalyst-Free One-Pot Synthesis and In Vitro Biological Activity Evaluation of Novel Isoquinoline Derivatives of Fatty Acids","authors":"Razieh Rahimizadeh, Akbar Mobinikhaledi, Hassan Moghanian, Mahta Mobinikhaledi, Seyedeh sara Kashaninejad","doi":"10.1007/s11094-024-03189-9","DOIUrl":"https://doi.org/10.1007/s11094-024-03189-9","url":null,"abstract":"There is good evidence that fatty acid derivatives have antibacterial activity and represent a promising approach to developing the next generation of antibacterial agents. In the present work, some new isoquinolin derivatives were synthesized via the Betti reaction. Three-component reaction of aryl aldehydes, 2,7-naphthalenediol and ammonium carboxylate of fatty acids with different chains in EtOH under reflux conditions offered related isoquinolin compounds in good to excellent yields. Some advantages of this procedure are short reaction times, free catalyst, high yield of products and easy work-up. The structure of synthesized compounds was characterized by IR, 1H, and 13C NMR data as well as microanalysis results. In addition, these novel materials were evaluated for their biological activities against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) bacteria. The obtained data confirm that isoquinolin derivatives 4c, 4e, 4f, 4g, 4m, 4n, 4p, 4q exert excellent antimicrobial activity against these tested bacterial strains.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.9,"publicationDate":"2024-08-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948675","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Protective Effects of Raspberry Ketone against Isoproterenol-Induced Cardiac Hypertrophy in Wistar Rats 覆盆子酮对异丙肾上腺素诱导的 Wistar 大鼠心肌肥大的保护作用

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03181-3

Vasim Khan, Sumit Sharma, Aamir khan, Uma Bhandari, Syed Ehtaishamul Haque

{"title":"Protective Effects of Raspberry Ketone against Isoproterenol-Induced Cardiac Hypertrophy in Wistar Rats","authors":"Vasim Khan, Sumit Sharma, Aamir khan, Uma Bhandari, Syed Ehtaishamul Haque","doi":"10.1007/s11094-024-03181-3","DOIUrl":"https://doi.org/10.1007/s11094-024-03181-3","url":null,"abstract":"Raspberry ketone (RK) is an active constituent obtained from Rubus idaeus (Rosaceae), which has been traditionally used against diabetes, hypertension, etc. The objective of this study was to assess the cardioprotective effect of RK against isoproterenol (ISO)-induced cardiac hypertrophy in Wistar rats. Rats were arbitrarily divided into six groups and were treated daily with raspberry ketone (100 and 200 mg/kg), fenofibrate (80 mg/kg) and propranolol (10 mg/kg) along with ISO (3 mg/kg, subcutaneously) for 28 days. Twenty-four hours after the last dose administration, serum and heart tissue samples from the animals were taken and their hemodynamic (blood pressure, heart rate], biochemical (CK-MB, LDH, troponin-T, PPAR-α, apolipoprotein C III, c-reactive protein, total cholesterol, triglycerides, high-density lipoprotein, low-density lipoprotein, very-low-density lipoprotein, malondialdehyde, reduced glutathione, superoxide dismutase, catalase, Na+-K+-ATPase, total antioxidant capacity, and nitric oxide), histopathological, and immunohistochemical (caspase-3, nuclear factor-κB, tumor necrosis factor-α) analysis was performed along with gravimetric analysis. Administration of ISO significantly altered the cardiac integrity and physiology and these changes were significantly averted by the administration of RK (100 and 200 mg/kg). These results were also found to be comparable with those of the standard drugs, fenofibrate and propranolol. The assessment of cardiac morphology by histopathological and immunohistochemical analysis further validated these results. This study thus demonstrated that RK at doses of 100 and 200 mg/kg showed a dose-dependent decrease in inflammation, oxidative stress, and dyslipidemia against ISO-induced cardiac hypertrophy in Wistar rats, which could be due to agonistic action of RK at PPAR-α receptor subtype.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.9,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948508","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Effect of 2-ethyl-6-methylpyridinol-3-yl-thiooctanoate and its Non-Esterified Components on the Behavior of Rats in an Elevated Plus Maze 2-乙基-6-甲基吡啶醇-3-基硫代辛酸酯及其非酯化成分对大鼠在高架正迷宫中行为的影响

IF 0.9 4区医学

Pharmaceutical Chemistry Journal Pub Date : 2024-08-03 DOI: 10.1007/s11094-024-03178-y

I. A. Volchegorskii, S. I. Grobovoi, A. I. Sinitskii, I. Y. Miroshnichenko, L. M. Rassokhina, R. R. Mihajlov

{"title":"Effect of 2-ethyl-6-methylpyridinol-3-yl-thiooctanoate and its Non-Esterified Components on the Behavior of Rats in an Elevated Plus Maze","authors":"I. A. Volchegorskii, S. I. Grobovoi, A. I. Sinitskii, I. Y. Miroshnichenko, L. M. Rassokhina, R. R. Mihajlov","doi":"10.1007/s11094-024-03178-y","DOIUrl":"https://doi.org/10.1007/s11094-024-03178-y","url":null,"abstract":"The effect of thioctic acid (TA), 2-ethyl-6-methyl-3-hydroxypyridine hydrochloride (emoxypine), and their ester derivative (2-ethyl-6-methylpyridinol-3-yl-thiooctanoate, thioxypine) on the behavior of rats in an elevated plus maze (EPM) was studied. Intraperitoneal administration (three times) of TA, emoxypine, and their equimolar mixture in single doses of 36.25, 72.5, and 145 μmol/kg enhanced individual manifestations of anxious behavior in the EPM but did not cause full-blown anxiogenic effects. Similar pro-anxiogenic effects were observed when TA was administered in a dose of 36.25 μmol/kg and emoxypine in doses of 72.5 and 145 μmol/kg. The equimolar mixture of the non-esterified components of thioxypine had a pro-anxiogenic effect in doses of 36.25 and 72.5 μmol/kg. Combination of TA and 2-ethyl-6-methyl-3-hydroxypyridine into the ester potentiated their pro-anxiogenic activity, which manifested as an extensive anxiogenic effect of thioxypine when administered three times in a dose of 145 μmol/kg.","PeriodicalId":19990,"journal":{"name":"Pharmaceutical Chemistry Journal","volume":null,"pages":null},"PeriodicalIF":0.9,"publicationDate":"2024-08-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141948506","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0