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Tao Zhuang, Wen Zhang, Longji Cao, Kai He, Yu Wang, Jing Li, Liang Chen, Bifeng Liu, Guisen Zhang
Olanzapine is a marketed antipsychotic agent for treatment of both positive and negative symptoms of schizophrenia. The chemical synthesis of olanzapine drug substance involved the reaction of thienobenzodiazepine hydrochloride with N-methylpiperazine. During the manufacture of olanzapine, two unknown impurities were present in pilot batches in the range of 0.08-0.22% based upon HPLC analysis. These unknown impurities were enriched from the mother liquor of reaction by preparative HPLC, and characterized by UV, FT-IR, LC-MS/TOF, 1D-NMR (1H, 13C, DEPT), 2D-NMR (1H-1H COSY, HSQC, HMBC, ROESY) and single-crystal X-ray diffraction analysis...
January 31, 2018: Journal of Pharmaceutical and Biomedical Analysis
Neeraj Kumar, Subba Rao Devineni, Prasad Reddy Gajjala, Shailendra Kumar Dubey, Pramod Kumar
One unknown impurity (Imp-II) during the analysis of laboratory batches of isoproterenol hydrochloride was detected in the level ranging from 0.04% to 0.12% by high performance liquid chromatography with UV detection. The unknown impurity structure was proposed as 4-[2-(propan-2-ylamino)ethyl]benzene-1,2-diol (Imp-II) using the liquid chromatography--mass spectrophotometry (LC--MS) analysis. Imp-II was isolated by semi-preparative liquid chromatography from the impurity-enriched reaction crude sample. Its proposed structure was confirmed by nuclear magnetic spectroscopy such as 1H, 13C, DEPT (1D NMR), HSQC (2D NMR) and infrared spectroscopy (IR), and retention time and purity with HPLC followed by the chemical synthesis...
December 2017: Journal of Pharmaceutical Analysis
Phoebe F Lamie, John N Philoppes, Lucie Rárová
A new series of 1,2-diaryl-4-substituted-benzylidene-5(4H)-imidazolone derivatives 4a-l was synthesized. Their structures were confirmed by different spectroscopic techniques (IR, 1 H NMR, DEPT-Q NMR, and mass spectroscopy) and elemental analyses. Their cytotoxic activities in vitro were evaluated against breast, ovarian, and liver cancer cell lines and also normal human skin fibroblasts. Cyclooxygenase (COX)-1, COX-2 and lipoxygenase (LOX) inhibitory activities were measured. The synthesized compounds showed selectivity toward COX-2 rather than COX-1, and the IC50 values (0...
February 5, 2018: Archiv der Pharmazie
Sebile Işık Büyükekşi, Abdurrahman Şengül, Seda Erdönmez, Ahmet Altındal, Efe Baturhan Orman, Ali Rıza Özkaya
In this study, a bis-chelating bridging perylene diimide ditopic ligand, namely N,N'-di(1,10-phenanthroline)-1,6,7,12-tetrakis-(4-methoxyphenoxy)perylene tetracarboxylic acid diimide (1), was synthesized and characterized. Further reactions of 1 with d8 metal ions such as Pt(ii) and Pd(ii) having preferential square-planar geometry afforded the novel triads [(Cl2)M(ii)-(1)-M(ii)(Cl2)] where M(ii) = Pt(ii) (2), and Pd(ii) (3), respectively. The isolated triads and the key precursor were fully characterized by FT-IR, 1D-NMR (1H NMR and 13C DEPT NMR), 2D-NMR (1H-1H COSY, 1H-13C HSQC, 1H-13C HMBC), MALDI-TOF mass and UV/Vis spectroscopy...
January 31, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Tomoko M Nakanishi
Immediately after the Fukushima nuclear power plant accident, a team of 40-50 researchers at the Graduate School of Agricultural and Life Sciences at the University of Tokyo began to analyze the behavior of radioactive materials in the fallout regions. The fallout has remained in situ and become strongly adsorbed within the soil over time. 137Cs was found to bind strongly to the fine clay, weathered biotite, and organic matter in the soil; therefore, it has not mobilized from mountainous regions, even after heavy rainfall...
2018: Proceedings of the Japan Academy. Series B, Physical and Biological Sciences
Zdenek Provaznik, Andreas Holzamer, Daniele Camboni, Leopold Rupprecht, Markus Resch, Sigrid Wittmann, Christof Schmid, Bernhard Floerchinger
Background: Less invasive procedures have replaced open surgical treatment in many cardiovascular disorders. During these interventions, iatrogenic cardiac perforation may ensue, which is a severe complication and requires immediate diagnostic assessment and treatment. Methods: From March 2011 to April 2016, all patients referred to the Dept. of Cardio-thoracic Surgery with the diagnosis of iatrogenic perforation of myocardial wall or great vessels were included into the retrospective study...
December 2017: Journal of Thoracic Disease
C Kelly, M A Roett, K McCrory, A Coutinho, N Bhuyan, M Alavi, T Ho, C Stisher, A Bentley, M A Roett, P M Diller, A Davis, M A Roett
No abstract text is available yet for this article.
January 2018: Annals of Family Medicine
Harry Glorikian, Richard Jeremy Warburg, Kelly Moore, Jennifer Malinowski
The development of molecular diagnostics is a complex endeavor, with multiple regulatory pathways to consider and numerous approaches to development and commercialization. Companion diagnostics, devices which are "essential for the safe and effective use of a corresponding drug or diagnostic product" (see U.S. Food & Drug Administration, In Vitro Diagnostics - Companion Diagnostics, U.S. Dept. of Health & Human Services(2016), available at
December 9, 2017: Expert Opinion on Therapeutic Patents
Yu Jin, Xiaohai Liu, Lu Gao, Xiaopeng Guo, Qiang Wang, Xinjie Bao, Kan Deng, Yong Yao, Ming Feng, Wei Lian, Renzhi Wang, Qiwen Yang, Yao Wang, Bing Xing
OBJECTIVE: To investigate the incidence, bacteriological features, and risk factors of post- transsphenoidal surgery (TSS) meningitis and/or bacteremia. METHODS: This retrospective study included 3242 patients who underwent TSS for pituitary adenoma at the Dept. of Neurosurgery of Peking Union Medical College Hospital between January 2012 and December 2016. Clinical data for patients with and without post-TSS meningitis and/or bacteremia were compared and analyzed...
November 27, 2017: World Neurosurgery
Tugba Gungor, Gulden Yetis, Ferah Cömert Onder, Esra Tokay, Tugba Taşkın Tok, Ayhan Celik, Mehmet Ay, Feray Kockar
BACKGROUND: Directed Enzyme Prodrug Therapy (DEPT) as an alternative method against conventional cancer treatments, in which the non-toxic prodrug is converted to highly cytotoxic derivative, has attracted an ample attentions in recent years for cancer therapy studies. OBJECTIVE: The metabolite profile, cell cytotoxicity and molecular modeling interactions of a series of nitro benzamides with Ssap-NtrB were investigated in this study. METHOD: A series of nitro-substituted benzamide prodrugs (1-4) were synthesized and firstly investigated their enzymatic reduction by Ssap-NtrB (S...
November 29, 2017: Medicinal Chemistry
Shou-Bai Liu, Wen-Li Mei, Hui-Qin Chen, Jun Wang, Zhu-Nian Wang, Hao-Fu Dai
Six new compounds (1-4, 8, 10), along with six known limonoids (5-7, 9, 11, 12), were isolated from the roots of Trichilia sinensis. Their structures were elucidated on the basis of extensive spectroscopic methods including (1)H NMR, (13)C NMR, DEPT, HSQC, HMBC, (1)H-(1)H COSY and ROESY experiments, as well as by comparison with the literature. All the compounds were evaluated for cytotoxicities against K562, SGC-7901 and BEL-7402 cell lines. Compounds 2, 7, 10, 11, and 12 showed weak inhibitory activity to the selected cell lines...
November 23, 2017: Archives of Pharmacal Research
Mansour S Al-Said, Nasir A Siddiqui, Mohamed Ahmed Mukhair, Mohammad K Parvez, Perwez Alam, Mohd Ali, Anzarul Haque
Suaeda monoica Forssk. ex J.F. Gmel (Chenopodiaceae), a mangrove herb, is distributed in tropical Africa, Arabian Peninsula, India, Pakistan, Palestine and Jordan. The plant parts are used to treat sore throat, hepatitis, wounds, rheumatism, paralysis, asthma, snakebites, skin disease and ulcer. Two new phytoconstituents characterized as 13,17-octahydropentalene-4,4,10,23-tetramethyl-17,21-diisopropyl-tetradecahydrocyclo-[a]-phenanthrene-(14), 20(23), 21(30)-trien-5α-ol (SMC-3) and [1,4,4-trimethyl-cyclopent-1(5)-enyl]-9,10,17,21-tetramethyl-9α-ol-16α (17α)-epoxy heptadecan-6,10-dione (SMC-4) belong to the class norsesquaterpenol and monocyclic triterpenoid, respectively, along with two known compounds 3-epi-lupeol (SMC-1) and 4-cyclopentylpyrocatechol (SMC-2) have been isolated from the ethanol extract of aerial parts of S...
November 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Usama Shaheen, Nagwa Abdelkader Shoeib, Abeer Temraz, Mohamed I S Abdelhady
Background: Dipterygium glaucum Decne. herb is one of the common traditional plants with multiple medicinal uses. Objective: To isolate the major constituents and to investigate the antioxidant, antimicrobial, and cytotoxic activities of this herb. Materials and Methods: Methanolic extract of D. glaucum herb was fractionated using n-hexane, dichloromethane, and n-butanol. Butanol fraction was chromatographed using column chromatography and preparative thin layer chromatography to isolate the major constituents...
October 2017: Pharmacognosy Magazine
Hui Wang, Yanhua Chang, Hui Liang
OBJECTIVE: To analyze the clinical effect of tamsulosin and Solifenacin in the treatment of benign prostatic hyperplasia in combination with overactive bladder and its safety. Another objective was to investigate the clinical effect and safety of mega dose of tamsulosin in the treatment of benign prostatic hyperplasia in combination with overactive bladder. METHODS: One hundred and twenty-four patients who were admitted to the Dept. of Urology at Binzhou People's Hospital, , China with confirmed benign prostatic hyperplasia (BPH) with overactive bladder were randomly divided into two groups...
July 2017: Pakistan Journal of Medical Sciences Quarterly
Mazhar Hussain, Habib-Ur-Rehman, Lubna Akhtar
BACKGROUND AND OBJECTIVE: NAFLD affecting up to 30% of the population globally. Drug treatment options are limited with disappointing results. The dietary supplementation in the form of green tea is another option. Our objective was toinvestigate the effect of Green tea extract (GTE) supplementation on various parameters innon-alcoholicfatty liver disease (NAFLD) patients. METHODS: This study was conducted Dept. of Medicineof Sheikh Zayed Medical College/Hospital, Rahim Yar Khan from 15 April 2016 to 15 July 2016...
July 2017: Pakistan Journal of Medical Sciences Quarterly
Dan-Na Chen, Ya-Ping Wu, Yue-Juan Chen, Wen-Jian Liu, Jing-Xian Wang, Feng He, Lin Jiang
Two new stilbenoids, named 2,3 -dimethoxyl-7-hydroxyl-1,4-phenanthrenedione (1) and 2-methoxyl-3-methyl-7-hydroxyl-9,10-dihydro-1,4-phenanthrenedione (2), together with two known stilbenoids including densiflorol B (3) and ephemeranthoquinone (4), were isolated from aerial parts of Flickingeria fimbriata (Bl.) Hawkes. The structures of two new compounds were elucidated by extensive spectroscopic analysis, including HRESIMS, (1)H and (13)C NMR, DEPT, HMBC, COSY, HMQC, NOESY. All the compounds were obtained from this genus for the first time...
October 24, 2017: Journal of Asian Natural Products Research
Dimel K Bhuva, Jitendra H Vachhani
INTRODUCTION: Repeated blood transfusions can result in the production of alloantibodies against one or more red cell antigens, which complicates subsequent transfusions. Aims: The study was done to find incidence of various red cell alloantibodies; to determine the type of alloantibody; to identify the factors such as frequency of transfusion, splenectomy status, donor ethnicity and gender and their association with the development of antibody in repeatedly transfused patients. MATERIALS AND METHODS: This study was carried out in Dept...
July 2017: Asian Journal of Transfusion Science
Yawei Zhang, Lina Yang, Dongmei Wang, Dengwu Li
Chemical and structure properties of Ethanol lignin (EL), alkali lignin (AL), milled wood lignin (MWL) and cellulase enzymatic lignin (CEL) extracted from acorn shell of Quercus variabilis Bl. were studied by GPC, TG, SEM, FT-IR, (13)C NMR, DEPT-135 NMR, 2D-HSQC and functional groups measurement. Results indicated that AL had a lower quantity of ArOH (2.19mmol/g) in four lignin samples. TG results proved the existence of a less thermally stable domain within the lignin polymer. SEM, FT-IR, (13)C NMR, DEPT-135 NMR and 2D-HSQC confirmed the lignin structural characters of the extracted samples, it was found that the relative content of β-O-4' linkage in MWL (51...
September 25, 2017: International Journal of Biological Macromolecules
Paolo De Santis, Irene Lamanna, Nicolas Mavroudakis, Benjamin Legros, Jean-Louis Vincent, Jacques Creteur, Fabio Silvio Taccone
AIM: Few data are available on the use of brainstem auditory evoked potentials (BAEPs) in combination with other electrophysiological tools to assess prognosis of comatose survivors from cardiac arrest (CA). METHODS: Retrospective analysis of data from all adult patients (>18years of age) admitted to our Dept of Intensive Care after CA over a 6-year period who were comatose (Glasgow Coma Scale <9) on admission, had been treated with targeted temperature management and had BAEP testing...
November 2017: Resuscitation
M B Bharathi, J Rajendra Prasad, K Satish
The role of Drug-induced sleep endoscopy as a selection tool for surgical management of obstructive sleep apnoea syndrome. SOURCE OF DATA: Polysomnography proved OSA patients, who are planned for surgery in dept. of ENT AND HEAD& NECK, JSS Hospital, Mysore. STUDY DESIGN: A prospective clinical study. METHOD: 30 Polysomnography proved OSA patients, age between 20 and 60 years have been selected for Drug Induced Sleep Endoscopy (DISE) after taking informed consent for proposed surgery...
September 2017: Indian Journal of Otolaryngology and Head and Neck Surgery
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