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Adamantane

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61. Novel Guanidine Compound against Multidrug-Resistant Cystic Fibrosis-Associated Bacterial Species Full Text available with Trip Pro

; these derivatives were studied as antimicrobial agents against Gram-positive, Gram-negative, and a panel of drug-resistant clinical isolates recovered from patients with CF. One novel compound, a guanidine derivative bearing adamantane-1-carbonyl and 2-bromo-4,6-difluouro-phenyl substituents (H-BDF), showed potent bactericidal activity against the strains tested, at levels generally higher than those exhibited by tobramycin, ceftazimide and meropenem. The role that different substituents exert

2018 Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

62. Blockade of soluble epoxide hydrolase attenuates post-ischemic neuronal hyperexcitation and confers resilience against stroke with TrkB activation Full Text available with Trip Pro

a permanent middle cerebral artery occlusion (MCAO) model in adult wild-type mice with the sEH inhibitor 12-(3-adamantan-1-yl-ureido)dodecanoic acid (AUDA) post-treatment and in sEH knockout (sEH KO) mice. We found that sensorimotor recovery was significantly enhanced after MCAO in both AUDA-treated and sEH KO mice, with decreased sEH activity and brain infarction. Decreased post-ischemic long-term potentiation (iLTP) was observed in an ex vivo hippocampal oxygen-glucose deprivation model. Tropomyosin

2018 Scientific reports

63. A Supramolecular Approach for Liver Radioembolization Full Text available with Trip Pro

adamantane and cyclodextrin was employed in an in vivo pre-targeting set-up. Adamantane (guest)-functionalized macro albumin aggregates (MAA-Ad; d = 18 μm) and (radiolabeled) Cy5 and β-cyclodextrin (host)-containing PIBMA polymers (99mTc-Cy50.5CD10PIBMA39; MW ~ 18.8 kDa) functioned as the reactive pair. Following liver or lung embolization with (99mTc)-MAA-Ad or (99mTc)-MAA (control), the utility of the pre-targeting concept was evaluated after intravenous administration of 99mTc-Cy50.5CD10PIBMA39 (...) , for the first time, this data demonstrates that the formation of supramolecular interactions between cyclodextrin and adamantane can be used to drive complex formation in the chemically challenging in vivo environment. Conclusion: The in vivo distribution pattern of the cyclodextrin host could be guided by the pre-administration of the adamantane guest, thereby creating a direct link between the scout-scan (MAA-Ad) and delivery of therapy.

2018 Theranostics

64. Soluble epoxide hydrolase inhibitors, t-AUCB, downregulated miR-133 in a mouse model of myocardial infarction Full Text available with Trip Pro

assumed that the beneficial effects of sEHIs might also relate to the regulation of miR-133.A mouse model of myocardial infarction (MI) was established by ligating the coronary artery. The sEHI t-AUCB (trans-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid) was administered daily for 7 days before MI. Myocardial infarct size and cardiac function was assessed at 24 h post-MI. The miRNA expression profiles of sham and MI mice treated with or without t-AUCB were determined by microarray

2018 Lipids in health and disease

65. Palmitic Acid Methyl Ester and Its Relation to Control of Tone of Human Visceral Arteries and Rat Aortas by Perivascular Adipose Tissue Full Text available with Trip Pro

. These effects were abolished by XE991 (30 μM), but not 4-aminopyridine (2 mM) or NDGA (10 μM), a lipoxygenases inhibitor. The cytochrome P450 epoxygenase inhibitor 17-octadecynoic acid (ODYA 10 μM) and the soluble epoxide hydrolase inhibitor 12-(3-adamantan-1-ylureido)-dodecanoic acid (AUDA 10 μM) slightly decreased PAME relaxations. PAME up to 10 μM failed to induce relaxations of PVAT-removed human mesenteric arteries. 5-HT induced endogenous PAME release from rat peri-aortic adipose tissue, but not from

2018 Frontiers in physiology

66. Genetic and antigenic characterization of influenza A(H3N2) in Cameroon during the 2014-2016 influenza seasons. Full Text available with Trip Pro

to adamantanes. There was drift in influenza A(H3N2) dominant epitopes B (2014 and 2015) to epitopes A (2016) with a theoretical efficiency in vaccine ranging from low to moderate. The presence of several antigenic site mutations among H3N2 virus strains between 2014-2016 influenza seasons in Cameroon confirms the progressing evolution of circulating H3N2 strains.

2017 PLoS ONE

67. New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum. Full Text available with Trip Pro

. Ring survival and mature stage survival assays were performed against artemisinin-resistant and artemisinin-sensitive P. falciparum strains. Cytotoxicity was evaluated against mammalian cell lines V79 and HepG2, using the MTT assay.The synthesis and anti-malarial activity of 21 new endoperoxide-derived compounds is reported, where the peroxide pharmacophore is part of a trioxolane (ozonide) or a tetraoxane moiety, flanked by adamantane and a substituted cyclohexyl ring. Eight compounds exhibited

2018 Malaria journal

68. Modelling the emergence of influenza drug resistance: The roles of surface proteins, the immune response and antiviral mechanisms. Full Text available with Trip Pro

. We specifically examine three factors and their effect on the emergence of drug-resistant mutants: antiviral mechanism, the immune response, and surface proteins. We find that adamantanes, because they act at the start of the replication cycle to prevent infection, are less likely to produce drug-resistant mutants than NAIs, which act at the end of the replication cycle. A mismatch between surface proteins and internal RNA results in drug-resistant mutants being less likely to emerge

2017 PLoS ONE

69. Advances in the Development of PET Ligands Targeting Histone Deacetylases for the Assessment of Neurodegenerative Diseases Full Text available with Trip Pro

and evaluated using various assays including in vitro HDAC binding assays and PET imaging in rodents and non-human primates. Although most compounds do not readily cross the blood-brain barrier, adamantane-conjugated radioligands tend to show good brain uptake. Until now, only one HDAC radioligand has been tested clinically in a brain PET study. Further PET imaging studies to clarify age-related and disease-related changes in HDACs in disease models and humans will increase our understanding of the roles

2018 Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

70. A chemical genetic screen reveals that iminosugar inhibitors of plant glucosylceramide synthase inhibit root growth in Arabidopsis and cereals Full Text available with Trip Pro

in both systems, N-5-(adamantane-1-yl-ethoxy)pentyl- L-ido-deoxynojirimycin (L-ido-AEP-DNJ), inhibited root growth in agar plate assays by 92% and 96% in Arabidopsis and Tef respectively, at 10 µM concentration. Phenocopying the effect of L-ido-AEP-DNJ with the commercial inhibitor (PDMP) implicated glucosylceramide synthase as the target responsible for root growth inhibition. L-ido-AEP-DNJ was twenty-fold more potent than PDMP. Liquid chromatography-mass spectrometry (LC-MS) analysis

2018 Scientific reports

71. Vildagliptin (Galvus®) 50 mg tablets

of the All Wales Medicines Strategy Group (AWMSG). AWMSG Secretariat Assessment Report Advice No. 0213. 2013 Authors' conclusions Vildagliptin (Galvus®) is recommended as an option for use within NHS Wales for the treatment of type 2 diabetes mellitus as monotherapy in patients inadequately controlled by diet and exercise alone and for whom metformin is inappropriate due to contraindications or intolerance. Final publication URL Indexing Status Subject indexing assigned by CRD MeSH Adamantane; Diabetes

2013 Health Technology Assessment (HTA) Database.

72. [Addendum to Commission A12-16 Saxagliptin/metformin]

Auftrag A12-16 (Saxagliptin/Metformin). [Addendum to Commission A12-16 Saxagliptin/metformin] Cologne: Institut fuer Qualitaet und Wirtschaftlichkeit im Gesundheitswesen (IQWiG). IQWiG-Berichte 161. 2013 Final publication URL Additional data URL Indexing Status Subject indexing assigned by CRD MeSH Adamantane; Dipeptides; Dipeptidyl-Peptidase IV Inhibitors; Drug Combinations; Hypoglycemic Agentss; Metformin Language Published German Country of organisation Germany English summary There is no English

2013 Health Technology Assessment (HTA) Database.

73. [Saxagliptine/metformin (drug combination) - Benefit assessment according to § 35a Social Code Book V (dossier assessment)]

. 2013 Final publication URL Additional data URL Indexing Status Subject indexing assigned by CRD MeSH Adamantane; Dipeptides; Drug Therapy, Combination; Humans; Hypoglycemic Agents; Metformin; Thiazolidinediones Language Published German Country of organisation Germany English summary There is no English language summary available. Address for correspondence IQWiG, Im Mediapark 8, DE-50670 Cologne, GERMANY, Tel: +49 (0) 221 - 35685 - 0, Fax: +49 (0) 221 - 35685 - 1 Email: berichte@iqwig.de

2013 Health Technology Assessment (HTA) Database.

74. Vildagliptin (Galvus®) 50 mg tablets

of the All Wales Medicines Strategy Group (AWMSG). AWMSG Secretariat Assessment Report Advice No. 3012. 2012 Authors' conclusions Vildagliptin (Galvus®) 50 mg tablets are recommended as an option for use within NHS Wales for the treatment of type 2 diabetes in patients with moderate or severe renal impairment. Final publication URL Indexing Status Subject indexing assigned by CRD MeSH Adamantane; Blood Glucose; Diabetes Mellitus, Type 2; Dipeptidyl-Peptidase IV Inhibitors; Humans; Nitriles; Pyrrolidines

2012 Health Technology Assessment (HTA) Database.

75. Genetic deletion or pharmacological inhibition of soluble epoxide hydrolase reduces brain damage and attenuates neuroinflammation after intracerebral hemorrhage Full Text available with Trip Pro

. The present study investigated the involvement of sEH in ICH-induced neuroinflammation, brain damage, and functional deficits using a mouse ICH model and microglial cultures.ICH was induced by injecting collagenase in both wild-type (WT) C57BL/6 mice and sEH knockout (KO) mice. WT mice were injected intracerebroventricularly with 12-(3-adamantan-1-yl-ureido)-dodecanoic acid (AUDA), a selective sEH inhibitor, 30 min before ICH. Expression of sEH in the hemorrhagic hemisphere was examined

2017 Journal of neuroinflammation

76. Structure–Activity Studies of N‐Butyl‐1‐deoxynojirimycin (NB‐DNJ) Analogues: Discovery of Potent and Selective Aminocyclopentitol Inhibitors of GBA1 and GBA2 Full Text available with Trip Pro

and C5 hydroxy groups present in DNJ/NB-DGJ (N-butyldeoxygalactojirimycin) showed no inhibitory activity for CGT or GBA2. Inversion of stereochemistry at C4 of N-(n-butyl)- and N-(n-nonyl)-DGJ (compounds 24) also led to a loss of activity in these assays. The aminocyclopentitols N-(n-butyl)- (35 a), N-(n-nonyl)-4-amino-5-(hydroxymethyl)cyclopentane- (35 b), and N-(1-(pentyloxy)methyl)adamantan-1-yl)-1,2,3-triol (35 f), were found to be selective inhibitors of GBA1 and GBA2 that did not inhibit CGT (...) (>1 mm), with the exception of 35 f, which inhibited CGT with an IC50 value of 1 mm. The N-butyl analogue 35 a was 100-fold selective for inhibiting GBA1 over GBA2 (Ki values of 32 nm and 3.3 μm for GBA1 and GBA2, respectively). The N-nonyl analogue 35 b displayed a Ki value of ≪14 nm for GBA1 inhibition and a Ki of 43 nm for GBA2. The N-(1-(pentyloxy)methyl)adamantan-1-yl) derivative 35 f had Ki values of ≈16 and 14 nm for GBA1 and GBA2, respectively. The related N-bis-substituted

2017 ChemMedChem

77. Active maintenance of endothelial cells prevents kidney fibrosis Full Text available with Trip Pro

Active maintenance of endothelial cells prevents kidney fibrosis Soluble epoxide hydrolase (sEH) expressed by endothelial cells catalyzes the metabolism of epoxyeicosatrienoic acids (EETs), which are vasoactive agents.We used a unilateral ureteral obstruction mouse model of kidney fibrosis to determine whether inhibition of sEH activity reduces fibrosis, the final common pathway for chronic kidney disease.sEH activity was inhibited by continuous release of the inhibitor 12-(3-adamantan-1

2017 Kidney research and clinical practice

78. Drug Delivery and Nanoformulations for the Cardiovascular System Full Text available with Trip Pro

receptor agonist (CGS 21680), CYP-epoxygenases inhibitor (N-(methylsulfonyl)-2-(2-propynyloxy)-benzenehexanamide, trans-4-[4-(3-adamantan-1-ylureido)cyclohexyloxy] benzoic acid), soluble epoxide hydrolase inhibitor (N-methylsulfonyl-12,12-dibromododec-11-enamide), PPARγ agonist (rosiglitazone) and PPARγ antagonist (T0070907)], nanoparticles, peptides, and siRNA to the cardiovascular system. Effective formulations of nanoproducts have significant potential to overcome physiological barriers and improve

2017 Research & reviews. Drug delivery

79. Dynamic Mechano-Regulation of Myoblast Cells on Supramolecular Hydrogels Cross-Linked by Reversible Host-Guest Interactions Full Text available with Trip Pro

Dynamic Mechano-Regulation of Myoblast Cells on Supramolecular Hydrogels Cross-Linked by Reversible Host-Guest Interactions A new class of supramolecular hydrogels, cross-linked by host-guest interactions between β-cyclodextrin (βCD) and adamantane, were designed for the dynamic regulation of cell-substrate interactions. The initial substrate elasticity can be optimized by selecting the molar fraction of host- and guest monomers for the target cells. Moreover, owing to the reversible nature

2017 Scientific reports

80. Oriented, molecularly imprinted cavities with dual binding sites for highly sensitive and selective recognition of cortisol Full Text available with Trip Pro

attached at the 3-carbonyl group of cortisol via an oxime linkage and an adamantane carboxylate moiety coupled with the 21-hydroxyl group. TM1 was orientationally immobilized on a β-cyclodextrin (β-CD)-grafted gold-coated sensor chip by inclusion of the adamantane moiety of TM1, followed by copolymerization of a hydrophilic comonomer, 2-methacryloyloxyethyl phosphorylcholine, with or without a cross-linker, N,N'-methylenebisacrylamide. Subsequent cleavage of the oxime linkage leaves the imprinted

2017 Royal Society Open Science

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