ライフサイエンスコーパス: beta-carboline

1 phthol phosphoric acid to give an asymmetric beta-carboline.

2 N2 is the directing group than N9 in C1-aryl-beta-carbolines.

3 -e, which is known as the sulfur analogue of beta-carbolines.

4 llosteric regulatory site of benzodiazepines/beta-carbolines.

5 reaction of 1,2,3-trisubstituted tetrahydro-beta-carbolines.

6 o give 1-methyl-6-hydroxy-1,2,3,4-tetrahydro-beta-carboline (1), known to be formed at elevated level

7 , and tetrahydro-beta-carbolines (tetrahydro-beta-carboline, 1-methyltetrahydro-beta-carboline and pi

8 Treatment of tetrahydro-beta-carboline-1-thione with 2-bromooct-7-enoyl chloride

9 xin or with the BDZ inverse agonist n-methyl-beta-carboline-3-carboxamide (beta-CC), and a seizure ra

10 ne receptor partial inverse agonist N-methyl-beta-carboline-3-carboxamide (FG-7142).

11 challenge with the anxiogenic drug, N-methyl-beta-carboline-3-carboxamide (FG-7142; a partial inverse

12 oxylate ethyl ester (beta-CCE), and N-methyl-beta-carboline-3-carboxamide (FG7142), but not including

13 creasing GABA(A) tone with FG-7142 (N-methyl-beta-carboline-3-carboxamide) improved DMTP at low but n

14 ors by 1 muM diazepam, 30 mM EtOH, and 1 muM beta-carboline-3-carboxy ethyl ester (but not 1 muM Zn(2

15 ts treated with methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (1 microgram) and simply re

16 seizure threshold, a beta carboline [methyl-beta-carboline-3-carboxylate (beta-CCM)]-induced model o

17 rse BZ agonist, methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (DMCM; 1 or 10 microM), fai

18 pidem (EC50 = 75 nM), and dimethoxyl-4-ethyl-beta-carboline-3-carboxylate (IC50 = 60 nM).

19 inity, whereas methyl-6, 7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate inhibited GABAR currents.

20 flumazenil, and methyl-6,7-dimethoxy-4 ethyl-beta-carboline-3-carboxylate were inactive.

21 cation zinc and methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate, and differences in enhance

22 s, CGS-9895 and methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate, had qualitatively similar

23 ce against PTZ, methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate, picrotoxin, and amygdala-k

24 tors with the exception of dimethoxy-4-ethyl-beta-carboline-3-carboxylate, which behaved as a partial

25 beta-carboline methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate.

26 synthesis of 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC, 24,

27 Tetrahydro-beta-carboline-3-carboxylic acids were active against th

28 dimerization model studies on the tetrahydro beta-carboline (35).

29 ogical pH yields 1-methyl-1,2,3,4-tetrahydro-beta-carboline-5,6-dione (8) that reacts avidly with fre

30 8-S-glutathionyl-1-methyl-1,2,3,4-tetrahydro-beta-carboline-5,6-dione (9A and 9B).

31 lation approach has been developed utilizing beta-carboline alkaloids as the directing group.

32 A number of tremorogenic beta-carboline alkaloids have been found in common plant

33 Thus, comutagenicity of beta-carboline alkaloids with aromatic amines is shown t

34 d comutagen norharman along with two related beta-carboline alkaloids, carboline, and 5-carboline, wh

35 he synthesis of two biologically interesting beta-carboline alkaloids, ZK93423 and abecarnil (ZK11211

36 that structurally related 1,2,3,4-tetrahydro-beta-carbolines also bind at 5-HT(5A) receptors, and (d)

37 The versatility of beta-carboline amides as directing groups is evidenced b

38 We report here beta-carboline amides as intrinsic directing groups for

39 The highest content of the beta-carbolines among the traditional raw materials was

40 A reversal of the behavioural phenotype with beta-carboline, an anxiogenic inverse benzodiazepine rec

41 etrahydro-beta-carboline, 1-methyltetrahydro-beta-carboline and pinoline) were good OH radical scaven

42 The reaction between substituted 1-formyl-9H-beta-carbolines and terminal alkynes in the presence of

43 henanthridine, quinazoline, phthalazine, and beta-carboline, and electrophiles included acetyl chlori

44 These high-affinity tetrahydro-beta-carboline antagonists are able to discriminate amon

45 enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidat

46 Maillard reaction could be used to generate beta-carboline antioxidants.

47 , 2,8-quinolinediols, and 1-methyl-3-carboxy-beta-carboline are described.

48 ng ChemGPS-NP, we found that the more active beta-carbolines are all more lipophilic and larger than

49 beta-Carbolines are bioactive pyridoindole alkaloids occ

50 which contain a tetrahydro-beta-carboline or beta-carboline backbone, respectively.

51 ovel class of substituted 7,8-dichloro-1-oxo-beta-carbolines based on the distinct structural feature

52 d intramolecular cyclization of a tetrahydro-beta-carboline-based dipeptide has been developed to pre

53 A series of novel beta-carboline-based N-heterocyclic carbenes was prepare

54 The beta-carboline compounds norharman and harman exhibit ne

55 Chicory coffee has proved to be a source of beta-carboline compounds.

56 Harmaline, a beta-carboline derivative thought to induce tremor by fa

57 Harmaline, a beta-carboline derivative, is known to produce tremor th

58 Library of biologically relevant new beta-carboline derivatives and isolation of its cyclorut

59 be a versatile precursor to different fused beta-carboline derivatives via simple synthetic transfor

60 ethod to determine blood levels of two major beta-carboline derivatives, harmane and harmine.

61 Various 6-methoxytetrahydro-beta-carboline derivatives, namely BEN (6-methoxy-1-phen

62 pharmacologically investigated 37 tetrahydro-beta-carboline derivatives.

63 These novel beta-carbolines display similar growth inhibitory activi

64 gative [3-carbomethoxy-4-ethyl-6,7-dimethoxy-beta-carboline (DMCM)] BZD ligands.

65 zepine agonist, methyl-6,7-dimethoxy-4-ethyl-beta-carboline (DMCM, 10(-2)M).

66 delta receptors is blocked by flumazenil and beta-carboline-ethyl ester (beta-CCE).

67 The anxiogenic beta-carboline, FG 7142 (20 mg/kg) significantly increas

68 ctive tetrahydroisoquinolines and tetrahydro-beta-carbolines frequently with 99% ee's.

69 hydroxy-beta-carbolines, whereas tetrahydro-beta-carbolines gave oxidative and degradation products.

70 ne lung extract allowed the isolation of the beta-carbolines harmane and harmalan as confirmed by ESM

71 We therefore propose that the beta-carbolines harmane and harmalan represent active co

72 The naturally occurring beta-carboline, harmane, has been implicated in various

73 identified several alkaloids, including the beta-carboline harmine and the isoquinoline berberine, t

74 2-benzyl-3-ethoxycarbonyl-1,2,3,4-tetrahydro-beta-carbolines has been synthesized via the Pictet-Spen

75 To accomplish this, we developed 3-propoxy-beta-carboline hydrochloride (3-PBC), a mixed agonist-an

76 thyl moiety to a carbazole (e.g., 34, 36) or beta-carboline (i.e., 37), result in reduced affinity an

77 -tryptophan and 1-carboxy-1-methyltetrahydro-beta-carboline in the active CDS extract.

78 Previous literature indicates that certain beta-carbolines including harmane modulate central monoa

79 ation of cis-1,2,3-trisubstituted tetrahydro-beta-carbolines into the trans isomers via a potential c

80 In contrast, beta-carboline inverse-agonism was unaltered in chimeric

81 he two subunits differ in sensitivity to the beta-carboline methyl-6,7-dimethoxy-4-ethyl-beta-carboli

82 dividual differences in seizure threshold, a beta carboline [methyl-beta-carboline-3-carboxylate (bet

83 Further, intra-DRN administration of a beta-carboline mimicked the effects of IS, because rats

84 On the basis of IC50 and reaction rates (k), beta-carbolines (norharman and harman), and tetrahydro-b

85 The tetrahydro-beta-carboline of strictosidine aglycone is converted in

86 tet-Spengler reaction, which yields either a beta-carboline or a tetrahydroquinoline product from an

87 alkaloid harmine, which contain a tetrahydro-beta-carboline or beta-carboline backbone, respectively.

88 led mechanism for enzymatic catalysis of the beta-carboline product is proposed from these data.

89 atalyzing the stereoselective synthesis of a beta-carboline product.

90 N dimerization of substituted carbazoles and beta-carbolines, providing entry into seldom explored ch

91 beta-Carbolines reacted with hydroxyl radicals (OH) affo

92 r the construction of the bridged tetrahydro-beta-carboline ring system 5 has been developed that fea

93 igned and synthesized approximately 50 novel beta-carbolines structurally related to harmine.

94 by mild stress can be mimicked by anxiogenic beta-carbolines such as FG7142.

95 )9 and the two isomers of 1,2,3,4-tetrahydro-beta-carboline (Tca)9 Modifications in the cyclic templa

96 lines (norharman and harman), and tetrahydro-beta-carbolines (tetrahydro-beta-carboline, 1-methyltetr

97 ence for the synthesis of 1,2,3,4-tetrahydro-beta-carbolines (THBCs) relying on a ruthenium hydride/B

98 s the first report on the synthesis of spiro-beta-carbolines through a multicatalytic cascade process

99 agents were designed as hybrid molecules of beta-carboline (topoisomerase inhibition moiety) and bis

100 for both laboratory and clinical studies of beta-carboline toxicities.

101 subjected to the action of high temperature, beta-carboline was not detected.

102 Synthesis of substituted beta-carbolines was accomplished by utilizing the cataly

103 l group tolerance for C1-phenyl/thienyl/PAHs-beta-carbolines was demonstrated.

104 od to prepare 1-substituted N-Boc-tetrahydro-beta-carbolines was developed by lithiation followed by

105 s of 1-phenyl-substituted 1,2,3,4-tetrahydro-beta-carbolines was investigated via a Hammett study.

106 These and other related beta-carbolines were also examined in five recombinant G

107 totoxicity properties of 6-methoxytetrahydro-beta-carbolines were demonstrated for the first time.

108 on of the 3-amino ligands 40 and 41, all the beta-carbolines were found to exhibit high binding affin

109 beta-Carbolines were scavengers of OH in the three assay

110 ith hydroxyl radicals (OH) affording hydroxy-beta-carbolines, whereas tetrahydro-beta-carbolines gave

111 The latter undergoes rearrangement to a beta-carboline, which upon brominative oxidation undergo

112 n of 1,2,3-trisubstituted 1,2,3,4-tetrahydro-beta-carbolines, while the olefinic mechanism had been r

113 esis of various 1,4-disubstituted tetrahydro-beta-carbolines with excellent stereoselectivity (de, ee

114 rnish both cis- and trans-1,2,3,4-tetrahydro-beta-carbolines, with the trans isomer predominating.