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显示 1-30 共 148 条结果 关于 "G2539" 范围 论文
Baomei Wang et al.
Cell reports, 26(6), 1614-1626 (2019-02-07)
β2-integrins promote neutrophil recruitment to infected tissues and are crucial for host defense. Neutrophil recruitment is defective in leukocyte adhesion deficiency type-1 (LAD1), a condition caused by mutations in the CD18 (β2-integrin) gene. Using a model of Citrobacter rodentium (CR)-induced
Sarah E Tulk et al.
Journal of cellular biochemistry, 116(5), 711-720 (2015-02-03)
Vitamin D3 has emerged as an important regulator of the immune system. With metabolic enzymes for vitamin D3 activation and vitamin D receptors (VDR) now identified in a variety of immune cells, the active vitamin D3 metabolite 1,25(OH)2D3, is thought
A Guerra et al.
European journal of medicinal chemistry, 45(3), 930-940 (2009-12-22)
A neural model based on a numerical molecular representation using CODES program to predict oral absorption of any structure is described. This model predicts both high and low-absorbed compounds with a global accuracy level of 74%. CODES/ANN methodology shows promising
Xingchu Gong et al.
International journal of pharmaceutics, 493(1-2), 208-213 (2015-08-01)
An analysis of data collected from 25 sets of diverse pharmaceutical powders has identified that an exponential growth function satisfactorily describes the relationship between tablet brittleness and tablet porosity while a power law function well describes the relationship between tablet
Alaa A-M Abdel-Aziz et al.
European journal of medicinal chemistry, 46(9), 4324-4329 (2011-07-26)
Certain new halogenated cyclic-imides related to N-substituted phthalimide moiety were synthesized. Spacers of one or two carbon atom distances were inserted to connect the N-terminus of the cyclic-imide nuclei to the used heteroaryl groups to evaluate the effect of such
The second generation oral sulfonylureas: glyburide and glipizide.
T Kuhn
American pharmacy, NS28(10), 55-61 (1988-10-01)
Mariel Núñez et al.
BMC pharmacology & toxicology, 14, 6-6 (2013-01-15)
Glibenclamide (Gli) binds to the sulphonylurea receptor (SUR) that is a regulatory subunit of ATP-sensitive potassium channels (KATP channels). Binding of Gli to SUR produces the closure of KATP channels and the inhibition of their activity. This drug is widely
Atul Kumar et al.
Bioorganic & medicinal chemistry, 17(14), 5285-5292 (2009-06-09)
We have designed 1,3-disubstituted-5-membered heteroaromatic ring system as a common core motif from known anti-hyperglycemic agents. Designed compounds were synthesized and screened for in vivo anti-hyperglycemic activity in sucrose loaded model (SLM), sucrose-challenged streptozotocin-induced diabetic rat model (STZ-S) as well
Ya-Jean Wang et al.
Toxicology letters, 223(2), 139-145 (2013-09-10)
Methamphetamine (MA), a highly abused amphetamine-like psychostimulant, has surged in popularity worldwide in the last decade. Repeated MA exposure has been shown to affect the alternative splice variant expression of large conductance Ca(2+)-activated K(+) (BK) channels. It remains unclear whether
David Buttar et al.
Bioorganic & medicinal chemistry, 18(21), 7486-7496 (2010-09-28)
The displacement of probes that bind selectively to subdomains IIA or IIIA on human serum albumin (HSA) by competing compounds has been followed using fluorescence spectroscopy, and has therefore been used to assign a primary binding site for these compounds
Editorial: sulfonylureas differ in effects on ischemic preconditioning--is it time to retire glyburide?
Matthew C Riddle
The Journal of clinical endocrinology and metabolism, 88(2), 528-530 (2003-02-08)
Manthena V S Varma et al.
Journal of medicinal chemistry, 52(15), 4844-4852 (2009-05-19)
Kidney plays an important role in the elimination of drugs, especially with low or negligible hepatic clearance. An analysis of the interrelation of physicochemical properties and the human renal clearance for a data set of 391 drugs or compounds tested
Mariana Torres-Piedra et al.
European journal of medicinal chemistry, 45(6), 2606-2612 (2010-03-30)
The aim of the current study was to investigate the oral antidiabetic activity of six structurally related flavonoids: flavone (1), 3-hydroxyflavone (2), 6-hydroxyflavone (3), 7-hydroxyflavone (4), chrysin (5) and quercetin (6). Normoglycemic and STZ-nicotinamide diabetic rats were treated with these
Carlo Marchetti et al.
Journal of cardiovascular pharmacology, 66(1), 1-8 (2015-04-29)
Sterile inflammation resulting from myocardial injury activates the NLRP3 inflammasome and amplifies the inflammatory response mediating further damage. We used 2 experimental models of ischemic injury (acute myocardial infarction [AMI] with and without reperfusion) and a model of nonischemic injury
[Diagnosis and treatment of type 2 diabetes from the perspective of guidelines].
M Kellerer
Deutsche medizinische Wochenschrift (1946), 139(21), 1114-1115 (2014-05-16)
Gustav Ahlin et al.
Journal of medicinal chemistry, 51(19), 5932-5942 (2008-09-16)
The liver-specific organic cation transport protein (OCT1; SLC22A1) transports several cationic drugs including the antidiabetic drug metformin and the anticancer agents oxaliplatin and imatinib. In this study, we explored the chemical space of registered oral drugs with the aim of
D Saw et al.
Digestive diseases and sciences, 41(2), 322-325 (1996-02-01)
A wide variety of diseases and injuries can cause granulomatous hepatitis, and drug-induced granulomatous hepatitis is a well-described entity. Sulfonylurea derivatives, which are commonly used oral hypoglycemic agents in the treatment of non-insulin-dependent diabetes mellitus, have been implicated in liver
Yi-Ling Hsieh et al.
Journal of pharmaceutical sciences, 103(9), 2724-2735 (2014-02-08)
The aim of this study was to investigate the pH-induced precipitation behavior of four ionizable compounds (papaverine, dipyridamole, glyburide, and warfarin) in the absence and presence of polymers. Polymers selected included nonionic, anionic, and cationic polymers. Precipitates were analyzed immediately
Nandita Sinha et al.
European journal of medicinal chemistry, 46(2), 618-630 (2010-12-28)
A QSAR based predictive model of hERG activity in terms of 'global descriptors' has been developed and evaluated. The QSAR was developed by training 77 compounds covering a wide range of activities and was validated based on an external 'test
Sol Cristians et al.
Journal of natural products, 72(3), 408-413 (2009-01-15)
The CH(2)Cl(2)-MeOH (1:1) extract of the leaves of Hintonia standleyana and H. latiflora caused significant decrease in blood glucose levels in both normal and streptozotozin (STZ)-induced diabetic rats when compared with vehicle-treated groups (p < 0.05). These extracts were not
Ryan Mathias et al.
American journal of physiology. Gastrointestinal and liver physiology, 304(6), G623-G634 (2013-01-01)
Mesenteric lymphatic vessels actively transport lymph, immune cells, fat, and other macromolecules from the intestine via a rhythmical contraction-relaxation process called lymphatic pumping. We have previously demonstrated that mesenteric lymphatic pumping was compromised in the guinea pig model of 2,4,6-trinitrobenzenesulfonic
Sherrie L Aspinall et al.
The American journal of geriatric pharmacotherapy, 9(1), 58-68 (2011-04-05)
The objectives of this study were to describe changes in glyburide prescribing in cohorts that were and were not targeted by a risk reduction project, assess factors associated with glyburide discontinuation, and evaluate changes in glycated hemoglobin (ie, HbA(1c)) levels
Xiafei Wu et al.
IUBMB life, 67(4), 312-321 (2015-04-08)
Hepatic fibrosis is concomitant with liver inflammation, which has been highlighted as significant treatment of chronic liver disease. We previously demonstrated that tetramethylpyrazine (TMP), the effective component of Ligusticum chuanxiong Hort, can inhibit the activation of HSCs and consequential anti-hepatic
McGuinness OP; discussion 51S-53S et al.
The American journal of medicine, 89(2A), 26S-37S (1990-08-20)
Glyburide, along with the other second-generation oral hypoglycemic agent glipizide, has been used as adjunctive therapy for the treatment of non-insulin-dependent diabetes mellitus. After glyburide therapy, basal glycemia and glucose response to a meal are greatly improved. The mechanism for
Atma P Dwivedi et al.
Bioorganic & medicinal chemistry letters, 18(7), 2301-2305 (2008-03-21)
A series of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines were synthesized and evaluated for their antihyperglycemic activity. Compounds 3g and 6d exhibited lowering of postprandial plasma glucose by 30.7%, 23.3% in SLM and 25.6%, 25.4% in STZ models respectively which is significant
A Ahmadi et al.
Drug research, 63(12), 614-619 (2013-07-06)
In this study, new glibenclamide analogues (5a-d) with substituted pharmacological triethoxysilyl propan, allyl and ethoxyphenyl groups for cyclohexyl moiety have been synthesized by condensing sulfonamide (4) with related isocyanate or isothiocyanate's compounds. The newly synthesized drugs were evaluated for their
Giuseppe Ermondi et al.
European journal of medicinal chemistry, 44(5), 1926-1932 (2008-12-27)
The study compares GRIND-based 3D-QSAR and CoMFA [A. Cavalli, E. Poluzzi, F. De Ponti, M. Recanatini, J. Med. Chem, 45(2002), 3844-53] to investigate a biological topic dominated by hydrophobic interactions, e.g. hERG K(+) channel blocking activity. As expected, models are
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
Ramya V Shingalapur et al.
European journal of medicinal chemistry, 45(5), 1753-1759 (2010-02-04)
In seeking broad spectrum pharmacological activities of benzimidazole derivatives, a group of 4-thiazolidinones 5(a-j) and 1,3,4-oxadiazoles 6(a-j) containing 2-mercapto benzimidazole moiety were synthesized and screened for in vivo anticonvulsant activity by Maximal Electroshock (MES) model and antidiabetic activity using Oral
Séverin Slove et al.
Hypertension (Dallas, Tex. : 1979), 62(4), 794-801 (2013-08-07)
Hypertension is a cardiovascular disorder that appears in more than half of the patients with Williams-Beuren syndrome, hemizygous for the elastin gene among 26 to 28 other genes. It was shown that the antihypertensive drug minoxidil, an ATP-dependent potassium channel
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