Showing 1-30 of 33 resultados for "P56100"
Michael Groll et al.
Structure (London, England : 1993), 14(3), 451-456 (2006-03-15)
The dipeptide boronic acid bortezomib, also termed VELCADE, is a proteasome inhibitor now in use for the treatment of multiple myeloma, and its use for the treatment of other malignancies is being explored. We determined the crystal structure of the...
Beatriz E Bolívar et al.
Chembiochem : a European journal of chemical biology, 18(10), 931-940 (2017-02-22)
Pyrazinamide (PZA), an essential constituent of short-course tuberculosis chemotherapy, binds weakly but selectively to Sirtuin 6 (SIRT6). Despite the structural similarities between nicotinamide (NAM), PZA, and pyrazinoic acid (POA), these inhibitors modulate SIRT6 by different mechanisms and through different binding sites...
Wanliang Shi et al.
Science (New York, N.Y.), 333(6049), 1630-1632 (2011-08-13)
Pyrazinamide (PZA) is a first-line tuberculosis drug that plays a unique role in shortening the duration of tuberculosis chemotherapy. PZA is hydrolyzed intracellularly to pyrazinoic acid (POA) by pyrazinamidase (PZase, encoded by pncA), an enzyme frequently lost in PZA-resistant strains...
Michael J Munchhof et al.
Bioorganic & medicinal chemistry letters, 19(5), 1428-1430 (2009-02-03)
Recently, we disclosed a series of potent pyrimidine benzamide-based thrombopoietin receptor agonists. Unfortunately, the structural features required for the desired activity conferred physicochemical properties that were not favorable for the development of an oral agent. The physical properties of the...
Anthony D Baughn et al.
Antimicrobial agents and chemotherapy, 54(12), 5323-5328 (2010-09-30)
The pyrazinamide (PZA) analog 5-chloropyrazinamide (5-Cl PZA) is active against mycobacterial species, including PZA-resistant strains of Mycobacterium tuberculosis. In M. smegmatis, overexpression of the type 1 fatty acid synthase (FAS I) confers resistance to 5-Cl PZA, a potent FAS I...
Oren Zimhony et al.
Antimicrobial agents and chemotherapy, 51(2), 752-754 (2006-11-15)
The activity of different analogs of pyrazinamide on Mycobacterium tuberculosis fatty acid synthase type I (FASI) in replicating bacilli was studied. Palmitic acid biosynthesis was diminished by 96% in bacilli treated with n-propyl pyrazinoate, 94% in bacilli treated with 5-chloro-pyrazinamide...
Marta Filipa Simões et al.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 37(3-4), 257-263 (2009-06-06)
Pyrazinamide (PZA) is active against M. tuberculosis and is a first line agent for the treatment of human tuberculosis. PZA is itself a prodrug that requires activation by a pyrazinamidase to form its active metabolite pyrazinoic acid (POA). Since the...
Jhy-Wen Wu et al.
Drug metabolism and disposition: the biological fate of chemicals, 35(9), 1603-1610 (2007-06-02)
Pyrazinamide (PZA) is widely used in combination with other drugs in chemotherapy for tuberculosis. However, the dose-related liver injury is the main adverse effect of PZA and its metabolite [pyrazinoic acid (PA)]. Silibinin is the main flavonoid extracted from milk...
H J Kim et al.
The international journal of tuberculosis and lung disease : the official journal of the International Union against Tuberculosis and Lung Disease, 16(1), 98-103 (2012-01-13)
Pyrazinamide (PZA), one of the most effective anti-tuberculosis drugs, becomes toxic to Mycobacterium tuberculosis when converted to pyrazinoic acid by pyrazinamidase (PZase). PZA resistance is caused mainly by the loss of enzyme activity by mutation. To investigate the patterns of...
Takashi Iwanaga et al.
The Journal of pharmacology and experimental therapeutics, 320(1), 211-217 (2006-10-18)
Serum uric acid (SUA) is currently recognized as a risk factor for cardiovascular disease. It has been reported that an angiotensin II receptor blocker (ARB), losartan, decreases SUA level, whereas other ARBs, such as candesartan, have no lowering effect. Because...
João P S Fernandes et al.
Archiv der Pharmazie, 343(2), 91-97 (2010-01-26)
Tuberculosis is an infection caused mainly by Mycobacterium tuberculosis. A first-line antimycobacterial drug is pyrazinamide (PZA), which acts partially as a prodrug activated by a pyrazinamidase releasing the active agent, pyrazinoic acid (POA). As pyrazinoic acid presents some difficulty to...
Mirko Zimic et al.
Microbial drug resistance (Larchmont, N.Y.), 18(4), 372-375 (2012-03-01)
Pyrazinamide (PZA) is an important drug in the treatment of tuberculosis. Microbiological methods of PZA susceptibility testing are controversial and have low reproducibility. After conversion of PZA into pyrazinoic acid (POA) by the bacterial pyrazinamidase enzyme, the drug is expelled...
Y Sheeena Mary et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 71(2), 725-730 (2008-03-21)
A substituted amide of pyrazine-2-carboxylic acid was prepared and the IR spectrum is recorded and analysed. The vibrational frequencies and corresponding vibrational assignments are examined theoretically using the Gaussian03 set of quantum chemistry codes. Predicted infrared and Raman intensities are...
W Ebeid et al.
Die Pharmazie, 70(6), 368-373 (2015-07-21)
A capillary zone electrophoresis method was developed for the simultaneous determination of valsartan (VAL), amlodipine besylate (AML) and hydrochlorothiazide (HCZ) in their combined tablets. Separation was achieved on a fused silica capillary by applying a potential of 15 kV (positive...
Manas Sutradhar et al.
Dalton transactions (Cambridge, England : 2003), 42(33), 11791-11803 (2013-05-02)
A new binuclear oxovanadium(V) complex [{VO(OEt)(EtOH)}2L] (1) where H4L is bis(2-hydroxybenzylidene)terephthalohydrazide has been synthesized and fully characterized. The combination of 1 with pyrazine-2-carboxylic acid (PCA; a cocatalyst) affords a catalytic system for the efficient oxidation of saturated hydrocarbons, RH, with...
Halimah Sayahi et al.
Bioorganic & medicinal chemistry letters, 21(16), 4804-4807 (2011-07-22)
Pyrazinamide (PZA), an essential component of short-course anti-tuberculosis chemotherapy, was shown by Saturation Transfer Difference (STD) NMR methods to act as a competitive inhibitor of NADPH binding to purified Mycobacterium tuberculosis fatty acid synthase I (FAS I). Both PZA and...
Mary Margaret Wade et al.
Journal of medical microbiology, 53(Pt 8), 769-773 (2004-07-24)
Pyrazinamide (PZA) is an unconventional front line tuberculosis drug characterized by high in vivo sterilizing activity, but poor in vitro activity. This disparity in PZA activity may reflect differences between the in vivo tissue environment and in vitro culture conditions....
Stefania Tanase et al.
Dalton transactions (Cambridge, England : 2003), (15)(15), 2026-2033 (2008-04-03)
The reactivity towards H(2)O(2) of the complexes [Fe(pca)(2)(py)(2)].py (1) and Na(2){[Fe(pca(3))](2)O}.2H(2)O.CH(3)CN (2) (where pca(-) is pyrazine-2-carboxylate) and their catalytic activity in the oxidation of hydrocarbons is reported. Addition of H(2)O(2) to 1 results in the formation of a dinuclear Fe(III)-(mu-O)-Fe(III)...
Masanobu Sato et al.
Biochimica et biophysica acta, 1808(6), 1441-1447 (2010-11-16)
Uric acid transporter URAT1 contributes significantly to reabsorption of uric acid in humans to maintain a constant serum uric acid (SUA) level. Since alteration of SUA level is associated with various diseases, it is important to clarify the mechanism of...
Bruce A Ellsworth et al.
Bioorganic & medicinal chemistry letters, 17(14), 3978-3982 (2007-05-22)
Structure-activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via inclusion of hydroxyl-containing sidechains. This structural modification sufficiently improved ADME properties of an orally inactive series such that food intake...
Iwao Akashi et al.
The Journal of pharmacy and pharmacology, 61(4), 473-478 (2009-03-21)
The protective effects of coffee-derived compounds on lipopolysaccharide/D-galactosamine (LPS/D-GalN) induced acute liver injury in rats were investigated. Wistar rats were orally administered saline (control) or one of the test compounds (caffeine, chlorogenic acid, trigonelline, nicotinic acid or eight pyrazinoic acids)...
Mirko Zimic et al.
Tuberculosis (Edinburgh, Scotland), 92(1), 84-91 (2011-10-19)
Pyrazinamide is one of the most important drugs in the treatment of latent Mycobacterium tuberculosis infection. The emergence of strains resistant to pyrazinamide represents an important public health problem, as both first- and second-line treatment regimens include pyrazinamide. The accepted...
Martin Dolezal et al.
Current pharmaceutical design, 17(32), 3506-3514 (2011-11-15)
Design, results of in vitro antimycobacterial evaluation, and study of structure-activity relationships of various pyrazinecarboxylic acid reversible derivatives are presented. This review deals with some pyrazinamide analogues/prodrugs derived from Nphenylpyrazine- 2-carboxamides (1), arylaminopyrazine-2,5-dicarbonitriles (2), aryl/alkylsulphanylpyrazines (3,4), and aroylpyrazines (5) effecting...
Ping Lu et al.
Antimicrobial agents and chemotherapy, 55(11), 5354-5357 (2011-08-31)
Pyrazinoic acid, the active form of the first-line antituberculosis drug pyrazinamide, decreased the proton motive force and respiratory ATP synthesis rates in subcellular mycobacterial membrane assays. Pyrazinoic acid also significantly lowered cellular ATP levels in Mycobacterium bovis BCG. These results...
Rustam Z Khaliullin et al.
The journal of physical chemistry. B, 109(38), 17984-17992 (2006-07-21)
Experimental studies by Shul'pin and co-workers have shown that vanadate anions in combination with pyrazine-2-carboxylic acid (PCA identical with pcaH) produce an exceptionally active complex that promotes the oxidation of alkanes and other organic molecules. Reaction of this complex with...
Wolfgang Holzer et al.
Magnetic resonance in chemistry : MRC, 47(7), 617-624 (2009-04-30)
NMR spectroscopic studies are undertaken with derivatives of 2-pyrazinecarboxylic acid. Complete and unambiguous assignment of chemical shifts ((1)H, (13)C, (15)N) and coupling constants ((1)H,(1)H; (13)C,(1)H; (15)N,(1)H) is achieved by combined application of various 1D and 2D NMR spectroscopic techniques. Unequivocal...
Shirou Itagaki et al.
European journal of pharmacology, 518(2-3), 83-89 (2005-08-09)
The purpose of this study was to elucidate the transporter-mediated secretion systems for phenolsulfonphthalein in brush-border membranes. In human and rat renal brush-border membranes, a potential-sensitive transport system has been shown to be involved in the efflux of organic anions....
Tawfik Gharbaoui et al.
Bioorganic & medicinal chemistry letters, 17(17), 4914-4919 (2007-06-26)
A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series...
Mohamed Abdel-Aziz et al.
European journal of medicinal chemistry, 45(8), 3384-3388 (2010-05-22)
A series of pyrazine-2-carboxylic acid hydrazide derivatives were synthesized and screened for their activity against Mycobacterium tuberculosis. The results show that pyrazine-2-carboxylic acid hydrazide-hydrazone derivatives 3a-l were less active than pyrazinamide. In contrast, the N(4)-ethyl-N(1)-pyrazinoyl-thiosemicarbazide 4 showed the highest activity...
Microbiology. Pyrazinamide--old TB drug finds new target.
Stewart T Cole
Science (New York, N.Y.), 333(6049), 1583-1584 (2011-09-17)

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