ライフサイエンスコーパス: hydantoin

1 the ongoing optimization of antischistosomal hydantoins.

2 followed by a base-catalyzed cyclization to hydantoins.

3 ructural context affects OG oxidation to the hydantoins.

4 erted to regiosiomeric mixtures of tricyclic hydantoins.

5 The aryl hydantoin 1 (Ro 13-3978) was identified in the early 198

6 dium channel binding activity (log IC50) for hydantoins 1-12 and diphenylhydantoin (DPH) (r2 = 0.638)

7 Hydantoin 13 had excellent selectivity over other zinc m

8 through structure-based drug design to give hydantoin 13.

9 ict literature sodium channel activities for hydantoins 14-20, which were not included in the trainin

10 -1,3,4-oxadiazole (24) and a phenylmethylene hydantoin (28), both exhibited nanomolar affinity and se

11 esence of amines, G or OG oxidation produces hydantoin amine adducts.

12 n of 5-(3,4-dichlorophenyl) methylhydantoin (hydantoin), an antiviral drug that inhibits the replicat

13 aldol reaction between a suitably protected hydantoin and an optically enriched alpha-chloroaldehyde

14 bypass lesions found in ancient DNA, such as hydantoins and abasic sites.

15 from two chemical classes, spirosuccinamide/hydantoins and carboxylic acids.

16 rolyzed and oxidatively deprotected to yield hydantoins and unsaturated alpha-quaternary amino acids.

17 neration series of highly potent spirocyclic hydantoin antagonists of LFA-1.

18 scovered through structural modifications of hydantoin antiandrogens.

19 milar extent as sorbinil, a poorly selective hydantoin ARI previously shown to prevent retinopathy in

20 HQD)(2)PHAL, employing various N-chlorinated hydantoins as the terminal chlorenium source.

21 n-associated antigen-1 (LFA-1) of a class of hydantoin-based antagonists of leukocyte cell adhesion h

22 BIRT377 (1, Figure 1), a previously reported hydantoin-based LFA-1 inhibitor, these compounds are cha

23 12 years and includes the description of the hydantoin-based marketed drugs and clinical candidates.

24 opment of applications of N,N'-disubstituted hydantoin bearing alpha-amino acids by improving yields,

25 otein by the hydantoins, indicating that the hydantoin-binding site resides on the I-domain.

26 Furthermore, these quaternary hydantoins can be chemically manipulated to yield the co

27 A variety of hydantoins can be formed effectively under mild reaction

28 Hydantoins can be synthesized from the corresponding ami

29 Finally the hydantoin CoMFA model was used to design the structurall

30 Hydantoins containing trienes and tetraenes undergo sele

31 inct from the previously described series of hydantoin-containing indole derivatives (Nec-1), the Nec

32 A short synthesis of the hydantoin-containing marine sponge metabolites axinohyda

33 The principal SAR insight was that the hydantoin core of 1 is required for high antischistosoma

34 no acid-based core structure, derived from a hydantoin core, with unique heterocycles on the side cha

35 own hydantoinases for D-5-(2-methylthioethyl)hydantoin (D-MTEH) over the L-enantiomer leads to the ac

36 r rearrangement pathway to the corresponding hydantoin derivative competes with HNO formation, partic

37 Dantrolene sodium is a medically important hydantoin derivative that interferes with release of Ca2

38 metathesis to produce a functionalized fused hydantoin derivative.

39 elop an informative mathematical model using hydantoin derivatives as a training set of substrates by

40 A series of hydantoin derivatives have been prepared as single isome

41 e resulting urea to give bicyclic alpha-aryl hydantoin derivatives of substituted prolines.

42 5-Substituted-3-(alkoxycarbonyl)alkyl-hydantoin derivatives were prepared by mechanochemistry

43 s resulted in the first reported examples of hydantoin derivatives with good PK in preclinical specie

44 ation of this strategy to the development of hydantoin-derived aggrecanase inhibitors (eg, 3) for the

45 d with a hydantoin triene to give a bicyclic hydantoin dimer in high yield.

46 nificant barriers (10 kcal/mol), while fused hydantoins (five-membered fusion) have barriers that are

47 rds quaternary 5,5-(aryl, allyl)-substituted hydantoins found in many biologically significant compou

48 brane protein for sodium-linked transport of hydantoins from Microbacterium liquefaciens.

49 for the preparation of enantiomerically pure hydantoins from optically pure alpha-amino amides utiliz

50 However, NEIL1, NEIL2 and NEIL3 remove hydantoins from telomeric quadruplexes formed by five TT

51 ndly preparation of 5- and 5,5-disubstituted hydantoins from various amino ester hydrochlorides and p

52 The tolerance of the hydantoin group to the selenoxide elimination reaction c

53 inoalkyl group could be added to the central hydantoin group without significantly affecting binding.

54 OG), and its further oxidation products, the hydantoins guanidinohydantoin (Gh) and spiroiminodihydan

55 The biologically relevant hydantoin (imidazolidinedione) heterocycle functions as

56 Secondary amides afford the hydantoins in good to excellent yields, which decrease a

57 ino esters, in smooth conditions, leading to hydantoins in good yields and with no need of purificati

58 ey can be converted to unsymmetric ureas and hydantoins in high yields.

59 from binding to the purified protein by the hydantoins, indicating that the hydantoin-binding site r

60 e, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of

61 A series of hydantoin inhibitors of ADAMTS-4 and ADAMTS-5 were ident

62 nd highly selective non-carboxylic acid, non-hydantoin inhibitors of AR yet described (IC50, 1 nM; ED

63 is involved in virus encapsidation and that hydantoin inhibits this stage of replication.

64 on of imidazolones to alpha,beta-unsaturated hydantoins is outlined and represents a new approach to

65 ther sodium ions or the substrate 5-benzyl-l-hydantoin (L-BH) does not shift this conformational equi

66 Interestingly, a hydantoin lesion at the site most prone to oxidation in

67 te specificity with hNEIL1 revealed that the hydantoin lesions are excised much more efficiently (>10

68 These results indicate that the hydantoin lesions are the best substrates identified thu

69 NEIL1 and NEIL3 DNA glycosylases can remove hydantoin lesions but none of the glycosylases, includin

70 pathways mediate repair of a diverse set of hydantoin lesions in cells.

71 However, removal of hydantoin lesions in the absence of an opposite base may

72 Hydantoin lesions produced from further oxidation of 8-o

73 , the excision efficiency by hNEIL1 of these hydantoin lesions relative to other known substrates was

74 y and efficient activity of EcFpg toward the hydantoin lesions suggest that EcFpg mediates repair of

75 nce of the helix-destabilizing nature of the hydantoin lesions that facilitates their recognition wit

76 ) with a wide variety of oxidants yields the hydantoin lesions, guanidinohydantoin (Gh) and spiroimin

77 Of these, the hydantoin lesions, guanidinohydantoin (Gh) and the two d

78 quire a base opposite to identify and remove hydantoin lesions.

79 was successful in designing an effective non-hydantoin ligand.

80 are recognised through hydrogen bonds to the hydantoin moiety and the complementarity of the 5-substi

81 f the hydrazine allowed the preparation of a hydantoin motif bearing an aminopropyl side chain, which

82 tures of the dimetal TnDhp in complexes with hydantoin, N-carbamyl-beta-alanine, and N-carbamyl-beta-

83 that led to a structurally unprecedented non-hydantoin, non-carboxylic acid aldose reductase inhibito

84 not sufficient to account for the effects of hydantoins on the NVSC.

85 guanine (5-HO-OG) partitioning along the two hydantoin pathways, allowing us to propose a mechanism f

86 l member of the NCS1 family, the Mhp1 benzyl-hydantoin permease from Microbacterium liquefaciens, all

87 However, this series of aryl hydantoins produced antiandrogenic side effects in the h

88 The hydrolysis of the hydantoin products provides derivatives of quaternary am

89 to further oxidation to the highly mutagenic hydantoin products spiroiminodihydantoin (Sp) and 5-guan

90 Derivatives of 4-hydantoin-proline have been synthesized via a direct two

91 d L-hydantoinase, an L-N-carbamoylase, and a hydantoin racemase produced 91 mM L-met from 100 mM D,L-

92 Replacement of the phenol ring with a hydantoin resulted in weak antagonists.

93 In order to understand the importance of the hydantoin ring for good sodium channel binding, related

94 Two major conclusions were drawn: (1) The hydantoin ring is not critical for compounds with long a

95 Next, we noted the hydantoin ring of dGh mimics thymine, while the iminohyd

96 the four possible points of diversity in the hydantoin ring.

97 and serves to control the orientation of the hydantoin ring.

98 n performed on a 4-methyl-4-(4-hydroxyphenyl)hydantoin series is described which resulted in the deve

99 ed volume as key contributing factors in the hydantoin series while correctly predicting the experime

100 ntional five-step solid-phase synthesis of a hydantoin, similar results were obtained for both the H-

101 xidation of 8-oxoG leads to the formation of hydantoins, specifically guanidinohydantoin (Gh) and spi

102 nctional groups (67-84% yields from a common hydantoin starting material) as well as a spiroligomer t

103 Novel synthetic routes to various hydantoin structures, the advances brought to the classi

104 We show precisely where 5-substituted hydantoin substrates bind in an extended configuration a

105 for good sodium channel binding, related non-hydantoins such as hydroxy amides, oxazolidinediones, hy

106 he conformational cycle of the Na(+)-coupled hydantoin symporter Mhp1 from Microbacterium liquefacien

107 latter specifically in the setting of foetal hydantoin syndrome.

108 The review highlights the hydantoin syntheses presented from the point of view of

109 An amount of 163 rhodanines, hydantoins, thiohydantoins, and thiazolidinediones were

110 iminary 3-D QSAR model for the binding of 14 hydantoins to the neuronal voltage-gated sodium channel;

111 The hydantoin transporter Mhp1 is a sodium-coupled secondary

112 trom resolution structure of the NCS1 benzyl-hydantoin transporter, Mhp1, from Microbacterium liquefa

113 els of full-length plus-strand virion RNA in hydantoin-treated cultures.

114 oss metathesis (RC-RO-RC-CM) occurred with a hydantoin triene to give a bicyclic hydantoin dimer in h

115 The hydrolysis of the bicyclic hydantoins under basic conditions gave a range of enanti

116 open by an inhibitor, 5-(2-naphthylmethyl)-L-hydantoin, which becomes a substrate when leucine 363 is

117 roteins that together catabolize substituted hydantoins, whose chemical structure resembles that of a

118 he amino acid, followed by ring closure to a hydantoin with concomitant explulsion of the recyclable

119 Comparisons among different hydantoins with the same log P but different low-energy