ライフサイエンスコーパス: desmethyl

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

23 ective against tgDHFR than its corresponding desmethyl analogue.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

55 9008 was radiolabeled by N-alkylation of the desmethyl precursor using (11)C-methyl iodide.

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

57 The desmethyl precursors of active inhibitors lacked a perma

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

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

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

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

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

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

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

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

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

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

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

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

70 4-hydroxytamoxifen [4-OHT], and 4-hydroxy-N-desmethyl-tamoxifen [endoxifen]).

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

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

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

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

75 High-dose desmethyl tirilazad improves neurologic function after h

76 Desmethyl tirilazad is a lipid-soluble free radical quen

77 Neither desmethyl tirilazad nor deferoxamine improves pathologic

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

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

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

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

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

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

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