ライフサイエンスコーパス: aminoquinoline

1 ative for the formation of the C-N bond in 4-aminoquinolines.

2 to increase the permeability of parasites to aminoquinolines.

3 bled us to integrate the C-3 side chain on 2-aminoquinoline 1 extending deep into the P2' binding poc

4 d screening of a focused fragment library, 2-aminoquinoline 1 was identified as an initial hit for BA

5 type A light chain (BoNT/A LC) inhibitor bis-aminoquinoline (1) were prepared.

6 -(L)-leucylaminoquinoline (9) to leucine and aminoquinoline (10).

7 ive conversion to the fluorescent product, 6-aminoquinoline (2).

8 5h, prepared from the auxiliaries such as, 8-aminoquinoline, 2-(methylthio)aniline, and N',N'-dimethy

9 An unprecedented reactivity of 3-aminoquinoline-2,4-diones is reported.

10 Initial 4-anilino-6-aminoquinoline-3-carbonitrile leads showed poor selectiv

11 ution at the C-8 position of our 4-anilino-6-aminoquinoline-3-carbonitrile leads.

12 The 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles were prepared from the ap

13 of (+/-)-streptonigrin, a potent tetracyclic aminoquinoline-5,8-dione antitumor antibiotic that reach

14 es yielded similar MS/MS results; however, 6-aminoquinoline (6-AQ), 2-amino-9(10 H)-acridone (AMAC) a

15 e was either maintained or replaced with a 4-aminoquinoline-7-carbonitrile were synthesized in an eff

16 development of hemolytic anemia when given 8-aminoquinolines (8-AQs), an important class of antimalar

17 adding further evidence that antimalarial 4-aminoquinolines act by this mechanism.

18 a carboxylic acid 2-methylthioaniline- or 8-aminoquinoline amide substrate, aryl or alkyl iodide cou

19 istic understanding of the toxicity of the 4-aminoquinoline amodiaquine (1b), three series of amodiaq

20 nyl chlorides and bidentate ligands (e.g., 8-aminoquinoline and 2-(methylthio)aniline), has been inve

21 structure-activity relationship of seventy 4-aminoquinoline and 9-aminoacridine analogues reveals tha

22 For 13 aminoquinoline and aminoacridine compounds, relative dru

23 -induced electron transfer (PET) between the aminoquinoline and naphthalimide moieties by glucosamine

24 In this investigation, new hybrids of 4-aminoquinoline and pyrimidine moieties that show antipla

25 his study, 5-substituted phenyl ether-linked aminoquinolines and derivatives were synthesized and ass

26 We have previously described a system of 2-aminoquinoline- and 2-aminoquinazoline-based C-deoxynucl

27 A method for cobalt-catalyzed, aminoquinoline- and picolinamide-directed C(sp(2))-H bon

28 macology has also been established for the 4-aminoquinoline antimalarial class.

29 Amodiaquine (AQ) (2) is a 4-aminoquinoline antimalarial that can cause adverse side

30 Amodiaquine (AQ) and tebuquine are 4-aminoquinoline antimalarials with Mannich base side chai

31 linary approach for the development of new 4-aminoquinoline antimalarials, with efficacy superior to

32 Aminoquinolines (AQs) with diaminoalkane side chains (-H

33 n Ni-catalyzed C(sp(3))-H activation using 8-aminoquinoline as a directing group motivated us to exam

34 fluoroalkylated gamma-lactams derived from 4-aminoquinoline as potent chemotherapeutic agents for mal

35 atic amides is achieved in the presence of 8-aminoquinoline, as a removable directing group, using Mn

36 antimalarials, including endoperoxides and 4-aminoquinolines, as well as compounds active against ase

37 ple and general method for copper-catalyzed, aminoquinoline-assisted amination of beta-C(sp(2))-H bon

38 r alkylation of sp(3) and sp(2) C-H bonds, 8-aminoquinoline auxiliary affords the best results.

39 rs were synthesized with aminonaphthalene or aminoquinoline auxiliary groups tethered to N-4 of cytos

40 for amine gamma-functionalization, and the 8-aminoquinoline auxiliary is used for carboxylic acid bet

41 n of secondary sp(3) C-H bonds is desired, 8-aminoquinoline auxiliary may be used.

42 Using 8-aminoquinoline-based aryl carboxamides, the direct ortho

43 and, among the non-nucleoside inhibitors, 4-aminoquinoline-based inhibitors, such as SGI-1027 and it

44 2-Aminoquinoline-based scaffolds were designed with the ho

45 Removable picolinamide and 8-aminoquinoline bidentate directing groups are used to co

46 ers previously associated with resistance to aminoquinolines, but increased sensitivity to lumefantri

47 Tethering a fluorine atom to the aminoquinoline C(3) position afforded fluoroaminoquinoli

48 Unlike diprotic chloroquine (CQ), its two 4-aminoquinoline carbon isosteres (1, 2) are monoprotic at

49 omising members of our previously reported 2-aminoquinoline class of nNOS inhibitors, although orally

50 4-aminoquinolines, classically prepared via SNAr chemistry

51 Several compounds built on a 7-substituted 2-aminoquinoline core are potent and isoform-selective; X-

52 plasmodial activities of various substituted aminoquinolines coupled to an adamantane carrier are des

53 We synthesized both truncated and polar 2-aminoquinoline derivatives and assayed them against reco

54 loroquine yielded a series of new 7-chloro-4-aminoquinoline derivatives exhibiting high in vitro acti

55 Aminoquinoline derivatives were evaluated against a pane

56 earranged phenyl ether- and aniline-linked 2-aminoquinoline derivatives were therefore designed to (a

57 llic aryl-Co(III) intermediate proposed in 8-aminoquinoline-directed Co-catalyzed C-H activation proc

58 lent regiocontrol is achieved utilizing an 8-aminoquinoline directing group that can be readily cleav

59 N-tert-Butyl isoquine (4) (GSK369796) is a 4-aminoquinoline drug candidate selected and developed as

60 Resistance to 4-aminoquinoline drugs is associated with reduced drug per

61 ective; X-ray crystallography indicates that aminoquinolines exert inhibitory effects by mimicking su

62 fluorescein modified with a functionalized 8-aminoquinoline group as a copper-binding moiety, were sy

63 Their haemolytic risk when treated with 8-aminoquinolines has not been well characterized.

64 malarial drugs, chloroquine (CQ) and other 4-aminoquinolines have shown high potency and good bioavai

65 wo fluorescein-based dyes derivatized with 8-aminoquinoline, have been prepared and their photophysic

66 ly developed a class of membrane-permeable 2-aminoquinoline inhibitors and later rearranged the scaff

67 opment in the vector; and NPC-1161B, a new 8-aminoquinoline, inhibits sporogony.

68 obic substituent next to the cyano group and aminoquinoline methylation considerably improved isoform

69 n indol-3-yl linked to the 2-position of a 4-aminoquinoline moiety, shows promising activity against

70 and 78 are the first examples of either an 4-aminoquinoline or a tetraoxane liver stage inhibitors.

71 novel antimalarial drug that combines the 4-aminoquinoline pharmacophore of chloroquine with that of

72 8-aminoquinolines (primaquine and tafenoquine) are used fo

73 ical cure of Plasmodium vivax malaria with 8-aminoquinolines (primaquine or tafenoquine) is complicat

74 noxy)-methyl]-6-methoxy-8-bis [carboxymethyl]aminoquinoline (Quin-2).

75 Amodiaquine (AQ), a 4-aminoquinoline related to CQ, is recommended and often u

76 For 4-aminoquinolines related to CQ, our data suggest that ele

77 A new model of 4-aminoquinoline resistance is proposed to take account of

78 Considering aminoquinoline resistance, DP was associated with increa

79 in Tanzania; and (iii) the persistence of 4-aminoquinoline-resistant parasites in South America, whe

80 he addition of an additional subcomponent, 8-aminoquinoline, resulted in the formation of a third, mo

81 Nonquaternerized 4-aminoquinolines retain significant potency but are relat

82 compared with CQ include the presence of two aminoquinoline rings and a triamine linker and C-7 chlor

83 2-Aminoquinolines showed promise as bioavailable nNOS inhi

84 uestion mark-6-methoxy-8-bis-(carboxymethyl)-aminoquinoline tetra-(acetoxymethyl)ester (Quin/AM), a c

85 nds of secondary amides included 5-methoxy-8-aminoquinoline, which can be removed under mild conditio

86 sis, 1,8-dihydroxyanthrone (dithranol) and 3-aminoquinoline with potassium trifluoroacetate used as t

87 Because 4-aminoquinolines with modified side chains, such as AQ-13