ライフサイエンスコーパス: desmethyl

1 imazalil, 1.11-1.56 ng/mL for acetamiprid-N-desmethyl, 1.28-1.46 ng/mL for clothianidin, 0.94-1.49 n

2 laced, and 10-desmethylerythromycin A and 10-desmethyl-12-deoxyerythromycin A, both of which lack the

3 Specifically, 12-desmethyl-12-deoxyerythromycin A, which lacks the methyl

4 acetamiprid and its degradate, acetamiprid-N-desmethyl (18 +/- 4%, p = 0.01, CI = 95%).

5 red strain produced the predicted product, 2-desmethyl-2-methoxy-DEB, instead of 6-DEB and 2-desmethy

6 ered C-1027 analogues: 7''-desmethyl-C-1027 (desmethyl), 20'-deschloro-C-1027 (deschloro), and 22'-de

7 termediate of phytosterol biosynthesis and 4-desmethyl-24,25-dihydrolanosterol, a postulated downstre

8 In contrast, the targeted 16-desmethyl-25,26-dihydrodictyostatin analogues retained a

9 nthetic and medicinal chemistry analyses, 16-desmethyl-25,26-dihydrodictyostatin and its C6 epimer we

10 A (10) and (9R), (8S)-9-deoxo-4"-deoxy-3'-N-desmethyl-3'-N-ethanol-6, 9-epoxyerythromycin A (15) had

11 ssay: e.g., (9R), (8S)-9-deoxo-4"-deoxy-3'-N-desmethyl-3'-N-ethyl-6, 9-epoxyerythromycin A (10) and (

12 n, 6,9-hemiacetal 8,9-anhydro-4''-deoxy-3'-N-desmethyl-3'-N-ethylerythromycin B (ABT-229), or N-[(1S)

13 h 2-epi-5-epi-valiolone synthases (EEVS) and desmethyl-4-deoxygadusol synthases (DDGS) provided furth

14 n the formation of the rearranged metabolite desmethyl-5-deoxyenterocin and the shunt products wailup

15 methyl-2-methoxy-DEB, instead of 6-DEB and 2-desmethyl-6-DEB, which were formed in the absence of the

16 hase was engineered to exclusively produce 2-desmethyl-6-deoxyerythronolide B.

17 onolide B, and the desired novel analogue, 6-desmethyl-6-deoxyerythronolide B.

18 A previously unknown chemical structure, 6-desmethyl-6-ethylerythromycin A (6-ethylErA), was produc

19 ro Cystatin-C group (< LOQ, n = 7), higher N-desmethyl-acetamiprid (p = 0.013), dinotefuran (p = 0.04

20 fied seven neonicotinoids and a metabolite N-desmethyl-acetamiprid by LC-MS/MS; and we investigated t

21 N-Desmethyl-acetamiprid was detected in 92.4% of the urine

22 s positions on the naphthalene moiety of the desmethyl analog 10 gave compounds that displaced [3H]CP

23 anato substitution on the indole ring of the desmethyl analog provided isothiocyanate 12 that displac

24 The enantiomers of PTX 251D and their desmethyl analogs were synthesized from N-Boc-protected

25 d FaDu EC(50) = 17.5 nM) compared with the 9-desmethyl analogue 1.

26 e macrobicyclic homologues of BT-33 and a C7 desmethyl analogue and find that the C7 methyl group of

27 The O-desmethyl analogue of 10 was converted into [ (11)C] 10

28 oduced only small quantities of the expected desmethyl analogue of 6-deoxyerythronolide B.

29 (i) for sigma(2) = 0.59 +/- 0.02 nM) and its desmethyl analogue, (+/-)-8 (K(i) for sigma(1) = 108 +/-

30 ective against tgDHFR than its corresponding desmethyl analogue.

31 While the N(6)-desmethyl analogues 3a and 4 were inactive at the A(3)-A

32 Examination of the NMR of the desmethyl analogues revealed that the compound existed a

33 Biological assays reveal that both the desmethyl and C1-epimeric monomeric nuphar analogous are

34 New routes to the beta-methyl-, desmethyl-, and alpha-methyl-pyrrolidine-5,5-trans-lacta

35 of a readily accessible common precursor, N-desmethyl-B-obscurine.

36 In this study, N-desmethyl brigatinib was successfully synthesized as a p

37 dKAI2 exhibits a clear ligand preference for desmethyl butenolides and weak responses to methyl-subst

38 The preference of KAI2 for desmethyl butenolides is conserved in Selaginella moelle

39 from multiple species are most sensitive to desmethyl butenolides that lack a methyl group.

40 recently bioengineered C-1027 analogues: 7''-desmethyl-C-1027 (desmethyl), 20'-deschloro-C-1027 (desc

41 hydroxyl carvedilol), and - 10.1 kcal/mol (O-desmethyl carvedilol), respectively.

42 ral data of two closely related analogues, 6-desmethyl-chelocardin and its semisynthetic derivative 1

43 Fluoxetine and N-desmethyl citalopram were the most rapidly attenuated co

44 ied between 2.0 (imidacloprid) and 25.8 h (N-desmethyl-clothianidin), whereas mean urinary eliminatio

45 Desmethyl-GR24 and desmethyl-CN-debranone are active by KAI2 but not D14.

46 ecies Minyobates bombetes, and its racemic 3-desmethyl derivative (2) are reported.

47 Here we report the structure of dMyx--a desmethyl derivative of myxopyronin B--complexed with a

48 Here, we show that desmethyl desamino pateamine A (DMDA-PatA) represses tra

49 s by preparing a simplified PatA derivative (desmethyl, desamino PatA, DMDAPatA, 3).

50 all reporter mRNAs was equally sensitive to desmethyl-desamino-pateamine A (0.2-200 nM), an initiati

51 C]iodomethane, which is then used to treat N-desmethyl-ER176 in the presence of base ((t)BuOK) at roo

52 Desmethyl-GR24 and desmethyl-CN-debranone are active by

53 The indomethacin metabolite 5'-O-desmethyl indomethacin (5'-DMI) possessed binding affini

54 erestingly, of the three analogues, only the desmethyl-induced DNA damage response was similar to C-1

55 on, although the amount of breaks induced by desmethyl is greatly reduced compared with the other ana

56 activity from 2-fold (deschloro) to 55-fold (desmethyl) less than C-1027.

57 s brain entry of the PET radiotracer (11)C-N-desmethyl-loperamide ((11)C-dLop).

58 -gp), but it is rapidly metabolized to 11C-N-desmethyl-loperamide (11C-dLop), which is also a substra

59 T), but its metabolism to [N-methyl-(11)C] N-desmethyl-loperamide ([(11)C]dLop; [(11)C]3) precludes q

60 The radiotracer [(11)C]N-desmethyl-loperamide (dLop) images the in vivo function

61 he avid and selective P-gp substrate (11)C-N-desmethyl-loperamide (dLop) while avoiding side effects

62 try of both loperamide and its metabolite, N-desmethyl-loperamide (N-dLop), and thereby prevents cent

63 Here, we describe the synthesis of the desmethyl macrocycles, conformational studies on the atr

64 The synthesis of desmethyl macrolides has emerged as a novel strategy for

65 Metabolically, we show that the N-desmethyl metabolite is responsible for PK11195-mediated

66 tissue types, whereas the presence of the N-desmethyl metabolite was detected only in the lung secti

67 mutant, in total 11 new chartreusin analogs (desmethyl, methyl, ethyl, vinyl, ethynyl, bromo, hydroxy

68 The aziridinomitosene derivative (1S,2S)-6-desmethyl(methylaziridino)mitosene (4) was shown to alky

69 A series of 9-dihydro-9-acetamido-N-desmethyl-N-isopropyl erythromycin A analogues and relat

70 exposed to NAP, its oxidative metabolite 6-O-desmethyl NAP (DM-NAP), its AG or synthesized NAP-AG hum

71 Dehydro- and desmethyl-ofloxacin are further oxidized through several

72 via H atom abstraction to form dehydro- and desmethyl-ofloxacin, respectively; desaturation is a nov

73 synthetic LtnA2 analogues containing either desmethyl- or oxa-lanthionine rings confirm that the pre

74 e) was synthesized by (11)C-methylation of O-desmethyl-ORM-13070 with (11)C-methyl triflate, which wa

75 Desmethyl precursor 2 was reacted with (11)C-methyl iodi

76 or the corresponding unlabeled inhibitor (or desmethyl precursor to AR-R 17443 of similar potency) we

77 9008 was radiolabeled by N-alkylation of the desmethyl precursor using (11)C-methyl iodide.

78 synthesized by reaction of the corresponding desmethyl precursor with (11)C-CO(2) and reduction.

79 ined by (11)C methylation of a synthesized O-desmethyl precursor.

80 The desmethyl precursors of active inhibitors lacked a perma

81 roduced by N-alkylation of the corresponding desmethyl precursors using [11C]iodomethane.

82 ed in high yields and quality from their 6-O-desmethyl-precursors.

83 Bis-18,18'-desmethyl ritterazine N has been prepared in enantiomeri

84 ted method for the synthesis of simplified 2-desmethyl sanctolide A analogs is reported.

85 AChBP and nAChR bound to 13-desmethyl spirolide C efficiently; however, the cross-re

86 detection method allowed the detection of 13-desmethyl spirolide C in the range of 10-6000 mug/kg of

87 Significantly, the relative level of 4-desmethyl sterols (end-product sterols) was higher in se

88 ecificity of karlotoxins is shown to require desmethyl sterols.

89 As such, our work recognizes desmethyl SuFEx-IT as a valuable alternative to common F

90 In addition, we demonstrate the utility of desmethyl SuFEx-IT by successful preparation of a series

91 hectogram-scale preparation of the analogous desmethyl SuFEx-IT from inexpensive starting materials.

92 met for the major tacrolimus metabolite 13-O-desmethyl tacrolimus for AUC, but it failed the EMA crit

93 nding metabolites, 4-hydroxy TAM (OHT) and N-desmethyl TAM (DMT) have been well characterized.

94 xyguanosin-N(2)-yl)-N-desmethyltamoxifen (dG-desmethyl-TAM) and electrospray ionization tandem mass s

95 g levels of tamoxifen and its metabolites (N-desmethyl tamoxifen [N-DMT], 4-hydroxytamoxifen [4-OHT],

96 y enzyme responsible for the conversion of N-desmethyl tamoxifen to endoxifen.

97 of tamoxifen and its metabolites, 4HT and N-desmethyl-tamoxifen (NDT).

98 4-hydroxytamoxifen [4-OHT], and 4-hydroxy-N-desmethyl-tamoxifen [endoxifen]).

99 eration even in the presence of tamoxifen, N-desmethyl-tamoxifen, and 4-hydroxytamoxifen.

100 Desmethyl tirilazad (20 mg/kg) and 100 mg/kg deferoxamin

101 Desmethyl tirilazad (20 mg/kg) improves neurologic exam,

102 randomly assigned to receive either 20 mg/kg desmethyl tirilazad at -15 mins followed by 8 mg/kg/hr f

103 High-dose desmethyl tirilazad improves neurologic function after h

104 Desmethyl tirilazad is a lipid-soluble free radical quen

105 Neither desmethyl tirilazad nor deferoxamine improves pathologic

106 mg/kg) improves neurologic exam, but 3 mg/kg Desmethyl tirilazad or 100 mg/kg deferoxamine does not.

107 randomly assigned to receive either 3 mg/kg desmethyl tirilazad or vehicle at -15 and 90 mins.

108 eases on moving from the alpha-methyl to the desmethyl to the beta-methyl series.

109 avored for Fe(VI) leading predominantly to N-desmethyl-TRA (ca. 40%), whereas the proposed oxygen tra

110 Synthesis of a C(15)-desmethyl tricycle core of lycopodine has been accomplis

111 ced nearly normal quantities of the expected desmethyl triketide lactone.

112 the antidepressant venlafaxine metabolite, O-desmethyl venlafaxine, as top priority.

113 everal compounds (citalopram, venlafaxine, O-desmethyl-venlafaxine) were not attenuated.