A2093

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Investigation of possible prophylactic, renoprotective, and cardioprotective effects of thromboprophylactic drugs against ischemia-reperfusion injury.

Sinan Demirtas et al.

The Kaohsiung journal of medical sciences, 31(3), 115-122 (2015-03-07)

The aim of this study was to investigate whether anticoagulant and antiaggregant agents have protective effects against oxidative damage induced by peripheral ischemia-reperfusion (I/R). Groups were created as follows: control group, I/R group (sham group), I/R plus acetylsalicylic acid (Group

The prevalence of gastroduodenal mucosal injuries in aspirin users.

Thirada Thongbai

Journal of the Medical Association of Thailand = Chotmaihet thangphaet, 96(11), 1423-1427 (2014-01-17)

Aspirin is a widely used medication for primary and secondary prevention of cardiovascular and cerebrovascular events. The gastrointestinal risks of aspirin are well known, but the frequency of gastroduodenal mucosal injuries in aspirin users in Thailand is currently unknown. The

Aspirin and clopidogrel drug response in patients undergoing percutaneous coronary intervention: the role of dual drug resistance.

Eli I Lev et al.

Journal of the American College of Cardiology, 47(1), 27-33 (2006-01-03)

We evaluated the response to clopidogrel among aspirin-resistant versus aspirin-sensitive patients undergoing elective coronary stenting. Patients (n = 150) treated with aspirin but not clopidogrel had blood samples drawn at baseline and 24 h after clopidogrel loading. Depending on the

'Bridged' stilbene derivatives as selective cyclooxygenase-1 inhibitors.

Norbert Handler et al.

Bioorganic & medicinal chemistry, 15(18), 6109-6118 (2007-07-03)

Resveratrol ((E)-3,4',5-trihydroxy-stilbene), a phytoalexin found in various plants, shows non-selective cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) inhibition. In order to find more selective COX inhibitors a series of bridged stilbene derivatives was synthesized and evaluated for their ability to inhibit both

NSAID-associated gastrointestinal bleeding: assessing the role of concomitant medications.

Loren Laine

Gastroenterology, 147(4), 730-733 (2014-08-30)

Chocolate consumption and risk of diabetes mellitus in the Physicians' Health Study.

Chisa Matsumoto et al.

The American journal of clinical nutrition, 101(2), 362-367 (2015-02-04)

Previous studies reported beneficial effects of cocoa or chocolate on insulin resistance, oxidative stress, and inflammation, which are important risk factors of type 2 diabetes mellitus (DM). However, it is unclear whether chocolate consumption is associated with risk of DM.

Inhibitory effects of pain relief drugs on neurological enzymes: implications on their potential neurotoxicity to aquatic animals.

Jui-Pin Wu et al.

Environmental toxicology and pharmacology, 39(2), 898-905 (2015-03-25)

Pain relief medications commonly occur in the aquatic environment at measurable levels. While the neurotoxicity of pain relievers to higher vertebrates is currently known, little is known about their effects on aquatic animals. This study investigated the neurotoxicity of pain

A class of novel N-(1-methyl-β-carboline-3-carbonyl)-N'-(aminoacid-acyl)-hydrazines: aromatization leaded design, synthesis, in vitro anti-platelet aggregation/in vivo anti-thrombotic evaluation and 3D QSAR analysis.

Chunyu Li et al.

European journal of medicinal chemistry, 46(11), 5598-5608 (2011-10-11)

High anti-thrombotic activity of aminoacid modified tetrahydro-β-carbolines was generally correlated with a small proximity of the side chain of the aminoacid residue to the carboline-cycle. This paper explored that the aromatization of the tetrahydro-β-carboline-cycle of N-(1-methyl-β-tetrahydrocarboline-3-carbonyl)-N'-(aminoacid-acyl)-hydrazines leaded to N-(1-methyl-β-carboline-3-carbonyl)-N'-(aminoacid-acyl)-hydrazines and

In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.

Esra Bayram et al.

Bioorganic & medicinal chemistry, 16(20), 9101-9105 (2008-09-30)

The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes, hCA I and II, with a series of salicylic acid derivatives was investigated by using the esterase method with 4-nitrophenyl acetate as substrate. IC(50) values for sulfasalazine, diflunisal

Amino acid based enantiomerically pure 3-substituted benzofused heterocycles: A new class of antithrombotic agents.

Jitendra Kumar Mishra et al.

Bioorganic & medicinal chemistry letters, 20(1), 244-247 (2009-11-26)

A diverse group of novel medium ring heterocycles derived from naturally abundant proteinogenic amino acids were evaluated for their potency towards antithrombotic activity. The more potent benzofused oxazepine and oxazocine scaffolds were diversified by incorporating different amino acids at the

Chamazulene carboxylic acid and matricin: a natural profen and its natural prodrug, identified through similarity to synthetic drug substances.

Mai Ramadan et al.

Journal of natural products, 69(7), 1041-1045 (2006-07-29)

Chamazulene carboxylic acid (1) is a natural profen with anti-inflammatory activity and a degradation product of proazulenic sesquiterpene lactones, e.g., matricin. Both 1 and proazulenes occur in chamomile (Matricaria recutita), yarrow (Achillea millefolium), and a few other Asteraceae species. It

10H-Phenothiazines: a new class of enzyme inhibitors for inflammatory diseases.

Y S Sadanandam et al.

European journal of medicinal chemistry, 44(1), 197-202 (2008-04-11)

The phenothiazine nucleus is known for their inhibitory activity towards the regulatory enzymes that are contributing to diseases such as asthma, autoimmune diseases including allergic rheumatoid and encephalomyelitis. In this study a number of substituted phenothiazines were synthesized and screened

Detecting Blending End-Point Using Mean Squares Successive Difference Test and Near-Infrared Spectroscopy.

Milad Khorasani et al.

Journal of pharmaceutical sciences, 104(8), 2541-2549 (2015-06-23)

An algorithm based on mean squares successive difference test applied to near-infrared and principal component analysis scores was developed to monitor and determine the blending profile and to assess the end-point in the statistical stabile phase. Model formulations consisting of

Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.

Dennis J Pelletier et al.

Journal of chemical information and modeling, 47(3), 1196-1205 (2007-04-13)

The identification of phospholipidosis (PPL) during preclinical testing in animals is a recognized problem in the pharmaceutical industry. Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process.

Weighing the risks of perioperative aspirin.

John Serak et al.

World neurosurgery, 82(6), 928-929 (2014-10-15)

Synthetic isoxazole as antiplatelet agent.

Margarita Gutiérrez et al.

Platelets, 25(4), 234-238 (2013-07-12)

Abstract Nine synthetic isoxazoles were evaluated as antiplatelet agents and studied the possible mechanism of more active compound. The initial screening was evaluating all compounds against platelet aggregation assays. The most active compound was isoxazole 8 showing an inhibition of

Synthesis of substituted acridinyl pyrazoline derivatives and their evaluation for anti-inflammatory activity.

Trilok Chandra et al.

European journal of medicinal chemistry, 45(5), 1772-1776 (2010-02-13)

A rapid preparation of compounds (1-24), with the objective of discovering novel and potent anti-inflammatory agent. All the compounds exhibited anti-inflammatory and analgesic activities at the dose 50 mg/kg p.o. The compound 1-(2',4'-Chloroacridine-9'-yl)-3-(5'-pyridine-4-yl)-(1,3,4-oxadiazol-2-yl-thiomethyl)-pyrazole-5-one 24 showed better anti-inflammatory and analgesic activities

Flavonoids inhibit COX-1 and COX-2 enzymes and cytokine/chemokine production in human whole blood.

Daniela Ribeiro et al.

Inflammation, 38(2), 858-870 (2014-08-21)

Cyclooxygenase 2 (COX-2) and the production of cytokines/chemokines are important targets for the modulation of the inflammatory response. Although a large variety of inhibitors of these pathways have been commercialized, some of those inhibitors present severe side effects, governing the

Relationship between aspirin use after diagnosis of colorectal cancer and patient survival: a meta-analysis of observational studies.

X-F Ye et al.

British journal of cancer, 111(11), 2172-2179 (2014-09-03)

Epidemiological evidence suggests that use of aspirin after the diagnosis of colorectal cancer can lengthen survival. However, the supporting data vary between studies, and this hypothesis remains controversial. We conducted a meta-analysis to provide a quantitative assessment of the association

1-Acylthiosemicarbazides, 1,2,4-triazole-5(4H)-thiones, 1,3,4-thiadiazoles and hydrazones containing 5-methyl-2-benzoxazolinones: synthesis, analgesic-anti-inflammatory and antimicrobial activities.

Umut Salgin-Gökşen et al.

Bioorganic & medicinal chemistry, 15(17), 5738-5751 (2007-06-26)

Acetic acid hydrazide containing 5-methyl-2-benzoxazolinone (4) was synthesized by the condensation of 2-(5-methyl-2-benzoxazolinone-3-yl)acetate with hydrazine hydrate. Thiosemicarbazide derivatives (5a-5d) were afforded by the reaction of corresponding compound 4 with substituted isothiocyanates. The cyclization of compounds 5a-5d in the presence of

Ultrastructure and composition of thrombi in coronary and peripheral artery disease: correlations with clinical and laboratory findings.

András Kovács et al.

Thrombosis research, 135(4), 760-766 (2015-02-18)

Fibrin structure and cellular composition of thrombi profoundly affect the clinical outcomes in ischemic coronary and peripheral artery disease. Our study addressed the interrelations of structural features of thrombi and routinely measured laboratory parameters. Thrombi removed by thromboaspiration following acute

Reasons for discontinuation of recommended therapies according to the patients after acute coronary syndromes.

Baris Gencer et al.

European journal of internal medicine, 26(1), 56-62 (2015-01-15)

The prescription of recommended medical therapies is a key factor to improve prognosis after acute coronary syndromes (ACS). However, reasons for cardiovascular therapies discontinuation after hospital discharge are poorly reported in previous studies. We enrolled 3055 consecutive patients hospitalized with

A human ether-á-go-go-related (hERG) ion channel atomistic model generated by long supercomputer molecular dynamics simulations and its use in predicting drug cardiotoxicity.

Anwar Anwar-Mohamed et al.

Toxicology letters, 230(3), 382-392 (2014-08-17)

Acquired cardiac long QT syndrome (LQTS) is a frequent drug-induced toxic event that is often caused through blocking of the human ether-á-go-go-related (hERG) K(+) ion channel. This has led to the removal of several major drugs post-approval and is a

Aspirin as adjuvant therapy for stage III colon cancer: standard of care?

Alfred I Neugut

JAMA internal medicine, 174(5), 739-741 (2014-04-02)

Endovascular repair of arterial iliac vessel wall lesions with a self-expandable nitinol stent graft system.

Birger Mensel et al.

PloS one, 9(8), e103980-e103980 (2014-08-15)

To assess the therapeutic outcome after endovascular repair of iliac arterial lesions (IALs) using a self-expandable Nitinol stent graft system. Between July 2006 and March 2013, 16 patients (13 males, mean age: 68 years) with a self-expandable Nitinol stent graft.

Synthetic derivatives of the alpha- and beta-amyrin triterpenes and their antinociceptive properties.

Cristian Soldi et al.

Bioorganic & medicinal chemistry, 16(6), 3377-3386 (2007-12-28)

Fifteen different derivatives of an alpha- and beta-amyrin mixture were synthesized by acylation with appropriate anhydride or acid chlorides and oxidation in the presence of tert-butyl chromate or PCC. The molecular structures of the obtained compounds were confirmed by means

[Routine platelet aggregation inhibition not useful when using acetylsalicylic acid or clopidogrel].

Miranda C A Kramer et al.

Nederlands tijdschrift voor geneeskunde, 153(5), 190-195 (2009-03-05)

The In Vitro Inhibitory Effect of Sivelestat on Elastase Induced Collagen and Metallopeptidase Expression in Equine Endometrium.

Ana Amaral et al.

Animals : an open access journal from MDPI, 10(5) (2020-05-21)

Neutrophil extracellular traps (NETs) fight endometritis, and elastase (ELA), a protease found in NETs, might induce collagen type I (COL1) accumulation in equine endometrium. Metallopeptidases (MMPs) are involved in extracellular matrix balance. The aim was to evaluate the effects of

Retrograde access to the posterior inferior cerebellar artery in balloon-assisted coiling of posterior inferior cerebellar artery aneurysms.

Sam Heye et al.

Journal of neurointerventional surgery, 7(11), 824-828 (2014-09-28)

Balloon-assisted coil embolization of proximal posterior inferior cerebellar artery (PICA) aneurysms may be limited by the inferiorly oriented, acutely angulated origin of the PICA from the vertebral artery. The aim of this study is to evaluate retrograde access to the

Platelet function testing in transient ischaemic attack and ischaemic stroke: A comprehensive systematic review of the literature.

Soon Tjin Lim et al.

Platelets, 26(5), 402-412 (2015-06-05)

The majority of patients with ischaemic cerebrovascular disease (CVD) are not protected from further vascular events with antiplatelet therapy. Measurement of inhibition of platelet function ex vivo on antiplatelet therapy, using laboratory tests that correlate with the clinical effectiveness of

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