ライフサイエンスコーパス: nitroimidazole

1 sequential four-drug regimens that include a nitroimidazole.

2 ory proteins that directly interact with the nitroimidazole.

3 belonging to both assemblages A and B, after nitroimidazole.

4 f the hypoxic cell marker pentafluorinated 2-nitroimidazole.

5 n be monitored by measuring the binding of 2-nitroimidazoles.

6 cephalosporins, penicillins, amphenicols and nitroimidazoles.

7 teins that are known to confer resistance to nitroimidazoles.

8 aching over 70% for most of the considered 5-nitroimidazoles.

9 wide range of substituted aryl halides and 4-nitroimidazoles.

10 ted in patients with giardiasis treated with nitroimidazoles.

11 of structure-based optimization of improved nitroimidazoles.

12 alize MIC results in this series of bicyclic nitroimidazoles.

13 btle structural variations in these bicyclic nitroimidazoles.

14 f refractory giardiasis after treatment with nitroimidazoles.

15 is hypothesis, we synthesized a 10B-enriched nitroimidazole, 1-2[(undecahydro-closo-dodecaborato)thio

16 By using the hypoxic marker 2-(2-nitroimidazole-1[H]-y1)-N-(2,2,3,3,3-pentafluoropropyl)-

17 isolates showed high levels of resistance to Nitroimidazoles (100%) and Penicillins (93.3%), with non

18 le (10), 1-(2'-deoxy-beta-D-ribofuranosyl)-4-nitroimidazole (11) and 1-(2'-deoxy-beta-D-ribofuranosyl

19 alpha-D-[5-fluoro-5-deoxyarabinofuranosyl]-2-nitroimidazole [(18)F-FAZA]).

20 g(-1)) and the recommended concentration for nitroimidazole (3.00 mug kg(-1)), respectively.

21 ric Ru(II)(kappa(4)-bda)L(2) complexes L = 5-nitroimidazole (5) and 5-bromo-N-methylimidazole (6), th

22 t has been developed for the extraction of 5-nitroimidazole (5-NDZ) drugs in milk samples previous to

23 dia lamblia, are commonly treated with the 5-nitroimidazole (5-NI) metronidazole (Mz), and yet treatm

24 Metronidazole and other 5-nitroimidazoles (5-NI) are among the most effective anti

25 beta-D-erythro-pentofuranosyl)-5-guanidino-4-nitroimidazole (6a) was synthesized by an independent ro

26 In the first step, 2-nitroimidazole (8) is coupled with 10 to yield intermedi

27 s, 97-109% for 4 nitrofurans, 84-115% for 10 nitroimidazoles, 89-114% for 3 phenicols, 86-111% for 3

28 , fluoroquinolones (11), sulphonamides (17), nitroimidazoles (9), amphenicols (2), cephalosporins (7)

29 In contrast, 5-guanidino-4-nitroimidazole, a product of the oxidation of guanine in

30 be used as potential biomarkers of illicit 5-nitroimidazole abuse.

31 The fluorinated nitroimidazoles all showed radiotracer uptake increasing

32 rmation of the nitro products, 5-guanidino-4-nitroimidazole and 8-nitroguanine adducts.

33 ared from zinc(II) nitrate and mixtures of 2-nitroimidazole and five different functionalized imidazo

34 In particular, hyperpolarized nitroimidazole and its derivatives have powerful potenti

35 have synthesized analogues of both 4- and 5-nitroimidazoles and explored their antitubercular activi

36 search: beta-lactam, lincosamide, macrolide, nitroimidazole, and tetracycline.

37 ven patients were recruited and treated with nitroimidazoles, and in 14 of 71 (20%) of patients follo

38 d with single-dose therapy of an appropriate nitroimidazole antibiotic, but women who are also infect

39 th useful diagnostic tools for IHRs due to 5-nitroimidazole antibiotics and can be used as supplement

40 nt studies of azathioprine/6-mercaptopurine, nitroimidazole antibiotics, and infliximab have broadene

41 e hypersensitivity reactions (IHRs) due to 5-nitroimidazole antibiotics.

42 The CYP3A inhibitors used in the study were nitroimidazole antifungal agents, diltiazem, verapamil,

43 Pretomanid is a nitroimidazole antimicrobial active against drug-resista

44 previously shown to mediate resistance to 5-nitroimidazole antimicrobial agents in B. fragilis strai

45 te that 2-aminoimidazolone and 5-guanidino-4-nitroimidazole are potent sources of mutations in vivo.

46 Nitroimidazoles are a class of antimicrobial drugs that

47 xycycline, penicillin, moxifloxacin, and the nitroimidazoles are effective treatments for gonorrhea,

48 g either 2-aminoimidazolone or 5-guanidino-4-nitroimidazole at a specific site, were ligated into sin

49 Several 2-nitroimidazole-based molecules (NIs) are used as clinica

50 Some of the best nitroimidazole CA IX inhibitors showed significant activ

51 le and CGI-17341, PA-824 is a prodrug of the nitroimidazole class, requiring bioreductive activation

52 ,3,3,3-pentafluoropropyl)acetam ide (EF5), a nitroimidazole compound that binds selectively to hypoxi

53 vestigated the mechanism by which fungicidal nitroimidazole compounds modulate AC activity.

54 The 2-nitroimidazole containing lead compound 3b (TH-302) was

55 f association under hypoxic conditions for 2-nitroimidazole-containing BB2r-targeted radioconjugates

56 These preliminary results suggest that a nitroimidazole-containing bivalent-targeting agent, [(68

57 ecific 2-aminoimidazolone- and 5-guanidino-4-nitroimidazole-containing genomes, and analysis of the r

58 Pd- or Ni-catalyzed C-H arylation of 4-nitroimidazole derivatives directed by a manipulable nit

59 ites; the major one is the corresponding des-nitroimidazole (des-nitro).

60 s of six classes, including fluoroquinolone, nitroimidazole, diarylquinolines, and oxazolidinones), w

61 that this nitration product is 5-guanidino-4-nitroimidazole diphosphate (NIm-DP), a degradation produ

62 Localization and quantitation of 2-nitroimidazole drug binding in low pO2 tumors is a techn

63 d, and contemporary strategies to facilitate nitroimidazole drug development are highlighted.

64 urther evidence of the toxic mechanisms of 5-nitroimidazole drugs has been revealed, which may be of

65 However, it can be further sensitized with nitroimidazole drugs, implying that it is partially hypo

66 increased degree of hypoxia (measured by the nitroimidazole EF5).

67 We used immunohistochemical detection of the nitroimidazole EF5, administered by intravascular infusi

68 method measures intracellular binding of the nitroimidazole EF5, which covalently binds to cellular m

69 ohistochemical detection of binding of the 2-nitroimidazole EF5.

70 ng of EF5, a fluorinated derivative of the 2-nitroimidazole, Etanidazole, can predict radioresistance

71 The nitroimidazole fexinidazole is a potential treatment.

72 Giardiasis failing nitroimidazole first-line treatment is an emerging probl

73 10B12H11SH) with 1-(2-bromoethyl)-2-methyl-5-nitroimidazole followed by purification of the adduct.

74 5-Guanidino-4-nitroimidazole formation in peroxynitrite-treated DNA wa

75 The yield of 5-guanidino-4-nitroimidazole formed in single-stranded DNA was approxi

76 hypoxia was investigated in vivo using the 2-nitroimidazole hypoxia marker, pimonidazole.

77 vation in hypoxic cells similar to that of 2-nitroimidazole hypoxia PET tracers.

78 o-closo-dodecaborato)thio]ethyl]-2- methyl-5-nitroimidazole (imidocaptate), by coupling the Cs salt o

79 he G to A mutation elicited by 5-guanidino-4-nitroimidazole implicates this lesion as a novel source

80 st that 2-aminoimidazolone and 5-guanidino-4-nitroimidazole in DNA are substrates for one or more of

81 The retention of nitroimidazole in Group 1 rabbits (brief occlusion) was

82 In vitro antibiotic resistance to 5-nitroimidazole in T. vaginalis remains low (4.3%) but sh

83 f the guanine-derived product, 5-guanidino-4-nitroimidazole, in synthetic oligonucleotides and DNA tr

84 ey determinants of aerobic activity in the 4-nitroimidazoles include the bicyclic oxazine, the lipoph

85 Bicyclic nitroimidazoles, including PA-824, are exciting candidat

86 A series of nitroimidazoles incorporating sulfonamide/sulfamide/sulf

87 midazolone; however, bypass of 5-guanidino-4-nitroimidazole increased nearly 10-fold.

88 was determined using the nucleoside analogs nitroimidazole, inosine, 7-deazaguanosine and 2-pyrimidi

89 rporation of the hypoxia-selective prodrug 2-nitroimidazole into receptor-targeted peptides.

90 nstrated that incorporation of one or more 2-nitroimidazoles into the BB2r-targeted peptide significa

91 ake of [18F]FETA in liver suggests that this nitroimidazole is metabolized less than [18F]FMISO.

92 he Suzuki-Miyaura cross-coupling reaction of nitroimidazoles is slightly lower in comparison to the d

93 re, we report that one lesion, 5-guanidino-4-nitroimidazole, is a substrate for multiple SOS polymera

94 Metronidazole, a 5-nitroimidazole, is often used as empirical therapy for a

95 Nitroimidazoles labeled with positron-emitting radionucl

96 bic Mycobacterium tuberculosis (Mtb) while 5-nitroimidazoles like metronidazole are active against on

97 xperiments further showed that 5-guanidino-4-nitroimidazole may cause G-->T and G-->C transversions i

98 st that nuclear DNA containing 5-guanidino-4-nitroimidazole may not be quickly repaired by DNA repair

99 tramethylpiperidin-N-oxyl (4, TEMPO) and the nitroimidazole misonidazole (5).

100 oligonucleotide containing the 5-guanidino-4-nitroimidazole modification was only partially cleaved b

101 ligonucleotides containing the 5-guanidino-4-nitroimidazole modification were purified by reverse-pha

102 the BB2r-targeted agents that incorporated 2-nitroimidazole moieties demonstrated improved retention.

103 2, (111) IN-3, and (111) IN-4, composed of 2-nitroimidazole moieties of 0, 1, 2, and 3, respectively-

104 st other HAP, including the clinical stage 2-nitroimidazole mustard TH-302, dinitrobenzamide mustard

105 For the 5-nitroimidazoles, neither the corresponding bicyclic anal

106 developed by incorporating hypoxia-sensitive nitroimidazole (NI) into the FAP-targeting agent FAPI-04

107 ia is prevalent in solid tumors, and various nitroimidazole (NI) radioligands can be trapped inside h

108 ve hyaluronic acid (HS-HA) conjugated with 2-nitroimidazole (NI), a hydrophobic component that can be

109 5-Guanidino-4-nitroimidazole (NI), derived from guanine oxidation by r

110 ard dinucleotide template indicated that the nitroimidazole nucleoside analogs could be used to incre

111 This study evaluates a new 99mTc-labeled nitroimidazole of potential benefit in standard myocardi

112 olones and quinolones, one imidazole and one nitroimidazole, one triazole, one diaminopyridine and on

113 re synthesized in five steps starting from 4-nitroimidazole, others were derived from 1a through simp

114 The 4-nitroimidazole PA-824 is active against aerobic and anae

115 a in pancreatic cancer patients, using the 2-nitroimidazole PET tracer (18)F-fluoroazomycin arabinosi

116 clines, quinolones, macrolides, nitrofurans, nitroimidazoles, phenicols, lincosamides, pleuromutilins

117 While the 4-nitroimidazole portion was specifically required, severa

118 We postulated that nitroimidazoles, previously used for radiosensitizing so

119 The hetero-bifunctional nitroimidazole radiosensitizer CI-1010, R-alpha-[[(2-bro

120 Prodrugs activated by 2-nitroimidazole reduction demonstrated up to 400-fold enh

121 The majority of nitroimidazole-refractory Giardia infections (57%) were

122 Nitroimidazole-refractory giardiasis cases, defined as m

123 Nitroimidazole-refractory giardiasis was primarily seen

124 Quinacrine is an effective treatment for nitroimidazole-refractory giardiasis with good tolerabil

125 inacrine was a highly effective treatment in nitroimidazole-refractory giardiasis, but patients shoul

126 zole plus chloroquine had a low cure rate in nitroimidazole-refractory giardiasis.

127 efficacy and tolerability of quinacrine for nitroimidazole-refractory giardiasis.

128 daily plus 155 mg twice daily for 5 days) in nitroimidazole-refractory giardiasis.

129 determination of nitrofuran metabolites and nitroimidazole residues in honey.

130 s AHD, AOZ, AMOZ and SEM, respectively while nitroimidazole residues; ronidazole (RNZ) and dimetridaz

131 RNA gene for identification purposes and the nitroimidazole resistance (nim) gene for detection of re

132 nization as the mobilization region of the 5-nitroimidazole resistance plasmid pIP417 and the clindam

133 In contrast, nitroimidazole retention in Groups 2 and 3 increased wit

134 The pattern of nitroimidazole retention on autoradiographs was then com

135 inhibitors, the most potent being 5-amino-4-nitroimidazole ribonucleotide with a K(i) of 0.7 +/- 0.5

136 there is now a renewed interest in bicyclic nitroimidazole scaffolds as a source of therapeutics aga

137 The fluorinated nitroimidazoles showed similar tumor distributions when

138 in the presence and absence of 2-methyl-4(5)-nitroimidazole, showing impressive rate enhancements of

139 vitro and in vivo profiles of a new bicyclic nitroimidazole subclass, namely, nitroimidazopyrazinones

140 xycycline, penicillin, moxifloxacin, and the nitroimidazoles, such as metronidazole, are effective tr

141 2-Nitroimidazoles, such as pimonidazole, are reduced in ce

142 These compounds are bicyclic nitroimidazoles that act as pro-drugs, requiring activat

143 is review, we summarize different classes of nitroimidazoles that have been described in the literatu

144 tumor and skin from patients given EF5, a 2-nitroimidazole tissue hypoxia monitor.

145 a heme-dependent flavin enzyme that degrades nitroimidazoles to amines lacking antimicrobial activity

146 to use the hypoxia-trapping capability of 2-nitroimidazoles to increase the retention of the agent i

147 ties of 2-aminoimidazolone and 5-guanidino-4-nitroimidazole, two products of peroxynitrite oxidation

148 re on alcohol abstinence in the setting of 5-nitroimidazole use was reviewed.

149 Dimetridazole (DMT), a nitroimidazole used in veterinary medicine for treating

150 In contrast, 5-guanidino-4-nitroimidazole was a strong block to replication and 50%

151 Technetium-99m-labeled nitroimidazole was administered to rabbits during the ea

152 With calf thymus DNA, 5-guanidino-4-nitroimidazole was dose-dependently formed at low peroxy

153 temperature, the modified base 5-guanidino-4-nitroimidazole was generated along with several other pr

154 were characterized, and their modulation by nitroimidazoles was investigated.

155 Delamanid, a-first-in-class bicyclic nitroimidazole, was recently approved for multidrug-resi

156 or 14 days; 500 mg clarithromycin and 500 mg nitroimidazole were added, twice daily for the final 7 d

157 While nitroimidazoles were discovered in the 1950s, there has

158 Penicillins and Nitroimidazoles were reported to be the most used antibi

159 cattle S. aureus isolates were resistant to Nitroimidazoles while 92.9% were resistant to Penicillin

160 d 5-nitroimidazooxazine provided the first 5-nitroimidazole with aerobic activity.

161 Rationale: Pretomanid is a new nitroimidazole with proven treatment-shortening efficacy