ライフサイエンスコーパス: aminopyrimidine

1 2-aminopyridine) and (R) in (26IO)3 (from 2-aminopyrimidine).

2 he substitution of the indazole in 1 for a 2-aminopyrimidine.

3 of the commercially available 4,6-dichloro-5-aminopyrimidine 1 with isothiocyanates.

4 -6-aminopyrimidines 4 via glycosylation of 4-aminopyrimidines 2 or 5 is described.

5 Silylated 4-aminopyrimidines 2 or 5 upon ribosylation with 1 provide

6 A family of sequence-related 2'-aminopyrimidine, 2'-hydroxylpurine aptamers, developed b

7 yrimidin-4-amines 3 or 4-(N-ribofuranosyl)-6-aminopyrimidines 4 via glycosylation of 4-aminopyrimidin

8 h the aid of X-ray structure-based analysis, aminopyrimidine amides 2 and 3 were designed from aminoq

9 -activity relationships of a series of novel aminopyrimidine amides 3 possessing improved cellular po

10 ns to design and synthesize a new library of aminopyrimidine analogues targeting site-2 of the plecks

11 s led to hybrid molecules which incorporated aminopyrimidine and aminopyridine moieties with ATP mime

12 The ability to detect both the aminopyrimidine and iminopyrimidine tautomeric forms of

13 of anti-Cdk inhibitors, we synthesized aryl aminopyrimidines and examined the effect of these compou

14 olism, is comprised of the thiazolium and 4'-aminopyrimidine aromatic rings, but only recently has pa

15 n electrophilic covalent catalyst and the 4'-aminopyrimidine as acid-base catalyst involving its 1',4

16 both rings of ThDP in YPDC catalysis (the 4'-aminopyrimidine as acid-base, and thiazolium as electrop

17 , we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved sol

18 In a designed series of aminopyrimidine-based inhibitors, we unexpectedly encoun

19 based core differs structurally from that of aminopyrimidine-based third-generation EGFR inhibitors a

20 s, and pharmacological characterization of 2-aminopyrimidine carbamates, a new class of compounds wit

21 a focus on the functional profiling of the 2-aminopyrimidine chemotype that has advanced to the clini

22 The aminopyrimidine compounds were reported to disrupt dynam

23 to D2/D3 and 5-HT1A receptor binding of the aminopyrimidine, cycloalkyl, and phenylpiperazine portio

24 We have identified an aminopyrimidine derivative (CYT387), which inhibits JAK1

25 of the carbamate led to the highly potent 2-aminopyrimidine derivative 20j with a significantly impr

26 investigation, we describe novel substituted aminopyrimidine derivatives that inhibit human GSK-3 pot

27 e discovery and SAR of a series of 6-alkyl-2-aminopyrimidine derived histamine H4 antagonists that le

28 tennimide crystal structure (26IO)4 (from 2-aminopyrimidine) exhibits three discrete conformational

29 ocycle (d2APy) while the second contains a 2-aminopyrimidine heterocycle (d2APm).

30 of an arylaldehyde, nitromethane, and the 6-aminopyrimidine in acetic acid containing ammonium aceta

31 et out to investigate whether mildly basic 2-aminopyrimidines in combination with the appropriate lin

32 alyzed by the KOBu(t)/DMSO system leads to 2-aminopyrimidines in up to 80% yield.

33 the optimization of highly ligand efficient aminopyrimidine lead compounds.

34 ut only recently has participation of the 4'-aminopyrimidine moiety in catalysis gained wider accepta

35 midines, the introduction of an additional 2-aminopyrimidine moiety in combination with the appropria

36 s that a chain of residues connecting the 4'-aminopyrimidine N1' atoms of thiamin diphosphates (ThDPs

37 des and an alkyne hydroamination employing 2-aminopyrimidine nucleophiles.

38 l also prefer this tautomer, and that the 4'-aminopyrimidine of ThDP participates in multiple steps o

39 ctive pan-ErbB kinase inhibitor from a novel aminopyrimidine oxime structural class that blocks the p

40 An aminopyrimidine, PNU 112455A, was identified in a screen

41 thaloyl dichloride with 2-aminopyridine or 2-aminopyrimidine provides a facile entry into a new class

42 hese results suggest that biaryl substituted aminopyrimidines represented by compound 9l may serve as

43 ture-activity relationships of substituted 2-aminopyrimidines, representing a new class of reversible

44 by reaction of 2-aminopyridines or 2-(or 4-)aminopyrimidines, respectively, with 1,2-bis(benzotriazo

45 the 1',4'-iminopyrimidine tautomer of the 4'-aminopyrimidine ring in thiamin diphosphate.

46 binds a water molecule and points toward the aminopyrimidine ring of ThDP.

47 crystallographic studies suggest that the 4'-aminopyrimidine ring of the thiamin diphosphate coenzyme

48 odels for the 1',4'-imino tautomer of the 4'-aminopyrimidine ring of thiamin diphosphate recently fou

49 ntify the various tautomeric forms of the 4'-aminopyrimidine ring on four thiamin diphosphate enzymes

50 and three conserved hydrogen bonds to the 4'-aminopyrimidine ring to enforce the V conformation, even

51 f covalent bond formation and response in 4'-aminopyrimidine ring's tautomeric state to intermediate

52 is hydrogen bonded to the N1' atom of the 4'-aminopyrimidine ring), as well as its position are consi

53 t the identification of such a molecule - an AminoPYrimidine-Sulfonamide (APYS1) that has potent, bac

54 a charge-transfer transition between the 4'-aminopyrimidine tautomer (presumed electron donor) and t

55 oism band characteristic of the canonical 4'-aminopyrimidine tautomer of bound thiamin diphosphate (A

56 y, both the 1',4'-iminopyrimidine and the 4'-aminopyrimidine tautomers coexist on the E1 component of

57 ed with the discovery of a compound with a 2-aminopyrimidine template that targeted the Wnt beta-cate

58 emissive adenosine analogue thieno[3,4-d]-6-aminopyrimidine ((th)A).

59 sly identified a series of 4,6-substituted 2-aminopyrimidines that associate with this soluble surrog

60 ts and from the previously analyzed set of 2-aminopyrimidines that displayed distinct cooperative int

61 In the series of 2-aminopyrimidines, the introduction of an additional 2-am

62 behavior of a number of 4,6-disubstituted 2-aminopyrimidines to Lymnaea AChBP, with different molecu

63 binding to the enzymes activates both the 4'-aminopyrimidine (via pK(a) elevation) and the thiazolium

64 A series of 2-aminopyrimidines was synthesized as ligands of the hista

65 DC-0941) as templates, (thienopyrimidin-2-yl)aminopyrimidines were discovered as potent inhibitors of

66 ivity relationships (SAR) around a series of aminopyrimidines were evaluated utilizing biochemical an

67 modular sequences from 2-aminopyridine and 2-aminopyrimidine wherein aminations of intermediate pyri(

68 The screening identified an aminopyrimidine with affinity in the high micromolar ran

69 of a series of over 50 newly characterized 2-aminopyrimidines with affinity for AChBP showed only two

70 rporated into design of a second subset of 2-aminopyrimidines yielding several congeners that elicite