ライフサイエンスコーパス: aminomethyl

1 A series of bioisosteric 4-(aminomethyl)-1-hydroxypyrazole (4-AHP) analogues of musc

2 enylallyllithium 7, and 2-bis(2-methoxyethyl)aminomethyl-1,3-diphenylallyllithi um 8, are indeed full

3 itative N,N-dichlorination of (R)- and (S)-2-aminomethyl-1,4-benzodioxane and successive functional g

4 olscine (7.75), 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane hydrochloride (WB-4101; 6.8

5 synthesis of the gamma-amino acid (1R,2R)-2-aminomethyl-1-cyclopentane carboxylic acid (AMCP) and an

6 NMR studies shows that 2-bis(2-methoxyethyl)aminomethyl-1-phenylallyllithium 7, and 2-bis(2-methoxye

7 After selective attachment of 2-aminomethyl-18-crown-6 (18c6), individual AP lesions are

8 -(Aminomethyl)-2,6-difluorophenol (6) and 4-(aminomethyl)-2, 6-difluorophenol (7) were synthesized in

9 3-(Aminomethyl)-2,6-difluorophenol (6) and 4-(aminomethyl)-

10 system ThiXYZ transports N-formyl-4-amino-5-(aminomethyl)-2-methylpyrimidine (FAMP), a thiamin salvag

11 detected by the fluorogenic traps 3-amino,4-aminomethyl-2',7'-difluorofluorescein diacetate and diam

12 In all genotypes, much 3-amino,4-aminomethyl-2',7'-difluorofluorescein diacetate fluoresc

13 Herein, we report the synthesis of 4'-C-aminomethyl-2'-deoxy-2'-fluorouridine, a therapeutically

14 dynamics simulations revealed that the 4'-C-aminomethyl-2'-O-methyl modified nucleotides adopt South

15 is work has implications for the use of 4'-C-aminomethyl-2'-O-methyl modified nucleotides to overcome

16 The linear syntheses of 4'-C-aminomethyl-2'-O-methyl uridine and cytidine nucleoside

17 modified, 2'-fluoro-, 2'-O-methyl-, and 4'-C-aminomethyl-2'-O-methyluridine showed the chemical natur

18 4,5-diaminofluorescein (DAF-2) and 3-amino,4-aminomethyl-2'7'-difluorescein (DAF-FM).

19 ctivity as a 5-HT(2C) agonist, a series of 1-aminomethyl-2-phenylcyclopropanes was investigated as 5-

20 Inhibitor 19b with a (R)-aminomethyl-2-pyrrolidinone and a Cp-THF was shown to be

21 se (PR) inhibitor containing a novel P1' (R)-aminomethyl-2-pyrrolidinone group.

22 edications for cocaine abuse, a series of 2-(aminomethyl)-3-phenylbicyclo[2.2.2]- and -[2.2.1]alkane

23 29)]; isochromans [(1R,3S)-3-(1'adamantyl)-1-aminomethyl-3,4-dihydo-5,6-dihydroxy-1H-2-benzo pyran (A

24 -benzo pyran (A77636) and (1R,3S)-3-phenyl-1-aminomethyl-3,4-dihydo-5,6-dihydroxy-1H-2-benzopyran (A6

25 c acid (7) and tert-butyl (+/-)-(2S,3R,4R)-2-aminomethyl-3-bis(tert-butyloxycarbonyl)amino-1-(N'-eth

26 uoronium ions react with alkenes 5 to give 4-aminomethyl-3-hydroxycyclobutene 11, derived by ring cle

27 n-propylamino)tetralin (8-OH-DPAT), 25 ng (5-aminomethyl-3-hydroxyisoxazole)hydrobromide (muscimol),

28 methyl-, 2-aminomethyl-, and N-substituted 2-aminomethyl-3-hydroxymorphinans.

29 By using 5-aminomethyl-3-hydroxysoxazole to temporarily inactivate

30 ree psoralens, 8-methoxypsoralen (8-MOP), 4'-aminomethyl 4,5', 8-trimethylpsoralen (AMT), and the nov

31 beta-(Aminomethyl)-4-chlorobenzenepropanoic acid (baclofen) wa

32 Potencies of the full agonists R-(+)-beta-(aminomethyl)-4-chlorobenzenepropanoic acid hydrochloride

33 e-guided design, we developed substituted 2-(aminomethyl)-4-ethynyl-6-iodophenols as p53-Y220C stabil

34 quent lead molecule from this series, (+)-6-(aminomethyl)-5-(2,4-dichlorophenyl)-N-(1-ethyl-1H-pyrazo

35 Two series with 2-(aminomethyl)-5-chlorobenzylamide and 4-amidinobenzylamid

36 Pregabalin [S-[+]-3-isobutylGABA or (S)-3-(aminomethyl)-5-methylhexanoic acid, Lyrica] is an antico

37 lin (PGB) [(S)-(+)-3-isobutyl-GABA or (S)-3-(aminomethyl)-5-methylhexanoic acid] can produce concentr

38 synthetic routes to enantiomerically pure 3'-aminomethyl-5'-carboxy-3',5'-dideoxy nucleosides, monome

39 -9-hydroxyfluoren-9(R)-ylcarbonyl-l-prolyl-2-aminomethyl-5-chlorobenz ylamide (19b), with high potenc

40 re, 9-hydroxy-9-fluorenylcarbonyl-l-prolyl-2-aminomethyl-5-chlorobenzylamide (2), with improved poten

41 ), PKC (administration of Ro 31-82425; 2-[8-(aminomethyl)-6,7,8,9-tetrahydropyrido[1,2-a]indol-3-yl]-

42 g in identification of racemic-trans-(3-((4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)

43 nolic group for the aminosulfonyl moiety [1-(aminomethyl)-6-hydroxynaphthalene (23) and 8-hydroxy-1,2

44 ylmethyl-7,8-dihydronormorphinone and 7alpha-aminomethyl-6,14-endoethanonororipavine have pronounced

45 uX(CNN)(dppb)] (1, X = Cl; 2, X = H; CNN = 2-aminomethyl-6-tolylpyridine, dppb = 1,4-bis(diphenylphos

46 racterization of DNA oligomers containing 7-(aminomethyl)-7-deazaguanine (1) residues using a variety

47 A set of nine 4-aminomethyl-7-alkoxycoumarin derivatives was synthesized

48 leasing hormone (GnRH) antagonists such as 6-aminomethyl-7-aryl-pyrrolo[1,2-a]pyrimid-4-ones (5) and

49 SAR from bicyclic GnRH antagonists such as 6-aminomethyl-7-arylpyrrolo[1,2-a]pyrimid-4-ones (1) and 2

50 oup of 7-cyano-7-deazaguanine (preQ(0)) to 7-aminomethyl-7-deazaguanine (preQ(1)), the only nitrile r

51 nverts 7-cyano-7-deazaguanine (preQ0) into 7-aminomethyl-7-deazaguanine (preQ1) for the biosynthesis

52 ction of 7-cyano-7-deazaguanine (preQ0) to 7-aminomethyl-7-deazaguanine (preQ1), a late step in the q

53 of the SD sequence of an mRNA hosting the 7-aminomethyl-7-deazaguanine (preQ1)-sensing riboswitch.

54 The preQ1 (7-aminomethyl-7-deazaguanine) riboswitch family comprises

55 trol bacterial genes in response to preQ1 (7-aminomethyl-7-deazaguanine), a precursor to the essentia

56 ndent reduction of 7-cyano-7-deazaguanineto7-aminomethyl-7-deazaguanine, a late step in the biosynthe

57 ynthesized and modified with the precursor 7-aminomethyl-7-deazaguanine, and this served as an effici

58 o aromatic rings and basic nitrogen atom, 9-(aminomethyl)-9,10-dihydroanthracene (AMDA; 1) is remarka

59 The effects of 3-position substitution of 9-aminomethyl-9,10-dihydroanthracene (AMDA) on 5-HT 2A rec

60 NMe2)(mu-O)3 (5) containing novel chelating (aminomethyl)amide-N(Me)CH2NMe2 ligands.

61 le of the amine, (b) a 1:1 complex with tris(aminomethyl)amine in which each calixarene unit contains

62 Derivatives with various aminomethyl and aminoethyl substituents on the para posi

63 phore to control the relative disposition of aminomethyl and carboxyl substituents.

64 oxymorphinans, including 2-hydroxymethyl-, 2-aminomethyl-, and N-substituted 2-aminomethyl-3-hydroxym

65 l analogs and found that the substitution of aminomethyl at the meta-position greatly enhances inacti

66 difications examined included, at 3': amino, aminomethyl, azido, guanidino, ureido; and at 5': uronam

67 ophenyl)-4-[N-(pyridine-3-ylmethoxy-carbonyl)aminomethyl]benzamide (MS-275)] infusion also reverses t

68 nophenyl)-4-[N-(pyridin-3-yl-methoxycarbonyl)aminomethyl]benzamide derivative (MS-275), which is a po

69 ophenyl)-4-[N-(pyridine-3-ylmethoxy-carbonyl)aminomethyl]benzamide].

70 phenyl)-4-[N-(pyridine-3-yl-methoxycarbonyl)-aminomethyl]-benzamide (MS-275), and vorinostat led to d

71 esis, and evaluation of a series of related (aminomethyl)benzamides in assays predictive of antipsych

72 chelator, N,N,N',N'-tetrapropionato-1,3-bis(aminomethyl)benzene (TPDBA), for complete extraction of

73 chelator, N,N,N',N'-tetrapropionate-1,3-bis(aminomethyl)benzene (TPDBA), has been used that permits

74 pling fluorinated carboxylic acids onto poly(aminomethyl)benzene scaffolds.

75 itatively this reversal is compatible with 4-aminomethyl benzoic acid competitively binding to the ex

76 mmetrically from a central scaffold (bis-3,5-aminomethyl benzoic acid, AMAB) to connect two ethacryni

77 Recently, we described N-(3-(aminomethyl)benzyl)acetamidine (13) as a slow, tight-bin

78 N-(3-(Aminomethyl)benzyl)acetamidine (1400W) was a slow, tight

79 N-(3-(Aminomethyl)benzyl)acetamidine (1400W) was reported to b

80 We have investigated the effect of N-(3-(aminomethyl)benzyl)acetamidine (1400W), a novel and high

81 ucible nitric oxide synthase inhibitor N-(3-(aminomethyl)benzyl)acetamidine dihydrochloride (1400W) a

82 s, N(5)-(1-iminoethyl)-L-ornithine and N-(3-(aminomethyl)benzyl)acetamidine, provide clues on how thi

83 e were treated with the iNOS inhibitor N -(3-aminomethyl)benzyl-acetamindine (1400W).

84 tor chlormethiazole and iNOS inhibitor N-(3-(aminomethyl)-benzyl) acetamidine abrogated the toxicity

85 effects of selective NOS II antagonists N-(3-aminomethyl) benzylacetamidine dihydrochloride (1400W) a

86 ation was suppressed by aminoguanidine, N-(3-aminomethyl)benzylacetamidine (1400W), or allopurinol, s

87 hyl)ornithine (L-NIO) or iNOS inhibitor N-(3-aminomethyl)benzylacetamidine, 2HCl (1400W) had no effec

88 paring polycyclic N,O-acetals from simple 1-(aminomethyl)-beta-naphthols and 2-(aminomethyl)-phenols.

89 The 7-hydroxy-2-(aminomethyl)chroman moiety was observed to be the primar

90 luation of a D(2/3)R agonist ligand from the aminomethyl chromane (AMC) class-(R)-2-[(4-(18)F-fluorob

91 A series of 2-(aminomethyl)chromans (2-AMCs) was synthesized and evalua

92 ia a carbene complex (1d) that isomerizes to aminomethyl complex 7d.

93 ifferences in their rates of hydrolysis of 5-aminomethyl coumarin (AMC) from C-terminally labeled pep

94 s-Menten kinetic analyses of 21 oligopeptide aminomethyl-coumarin substrates.

95 igomers (di-, tri-, and tetramers) of cis-2-(aminomethyl)cyclobutane carboxylic acid, a gamma-amino a

96 trast, the ionophore with the cis-1,3,5-tris(aminomethyl)cyclohexane scaffold exhibits a more Hofmeis

97 Tris(2-aminoethylamine) and cis-1,3,5-tris(aminomethyl)cyclohexane were employed as the scaffolds.

98 psilon-aminocaproic acid (EACA) and trans-4-(aminomethyl)cyclohexane-1-carboxylic acid (AMCHA), which

99 that the alpha2delta ligands gabapentin [1-(aminomethyl)cyclohexaneacetic acid] and pregabalin (PGB)

100 usly, it was determined that OA and trans-4-(aminomethyl)cyclohexanecarboxylic acid (AMCHA) (K(a) app

101 , zwitterions of similar size such as trans-(aminomethyl)cyclohexanecarboxylic acid (AMCHA) and p-ben

102 , 7-aminoheptanoic acid (7-AHpA), and trans-(aminomethyl)cyclohexanecarboxylic acid (AMCHA) to each o

103 of r(K57D)K3 for the lysine analogue trans-(aminomethyl)cyclohexanecarboxylic acid (AMCHA) was inves

104 These were trans-4-(aminomethyl)cyclohexanecarboxylic acid (t-AMCHA), prolin

105 agonist L-054,264 (N-[(1R)-2-[[[(1S*,3R*)-3-(aminomethyl)cyclohexyl]methyl]amino]-1-(1H-indol-3-ylm e

106 The 4-tert-butyl and 4-aminomethyl derivatives of phenylalanine (tBuPhe and AMP

107 omomethyl porphyrins were converted to their aminomethyl derivatives, H2(alpha,alpha-AP) and H2(alpha

108 was subjected to reductive amination to give aminomethyl derivatives.

109 The introduction of an aminomethyl group on the phenyl group led to monomer X,

110 Addition of the aminomethyl group to Phe substantially improved the sele

111 elded tetra-substituted sulfamidates with an aminomethyl group.

112 ic intermediates bearing carbamoylmethyl and aminomethyl groups at C-8.

113 ed and connected with secondary and tertiary aminomethyl groups, amide bonds, and hydroxymethylene gr

114 ety in DXP was replaced by hydroxymethyl and aminomethyl groups.

115 yrrolo[1,2-a]pyrimid-4-ones (5) and 2-aryl-3-aminomethyl-imidazolo[1,2-a]pyrimid-5-ones (6a,b), a ser

116 ndensed with indoles affording an array of 3-aminomethyl indoles.

117 A novel palladium-catalyzed approach to 2-(aminomethyl)indoles from 3-(o-trifluoroacetamidoaryl)-1-

118 Potent and much more selective N-aminomethyl-isatin-beta-thiosemicarbazones were discover

119 the inducible nitric oxide synthase (iNOS) N-aminomethyl-L-lysine.

120 We report herein an alternative aminomethyl linker that delivers similar potency and imp

121 To introduce the aminomethyl moiety of 2 via a palladium-catalyzed cyanat

122 inhibitors identified acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide as potent leads with une

123 xyphenyl)-2-chloro-5-[2-(bis(2-pyridylmethyl)aminomethyl)-N-meth ylaniline]-6-hydroxy-3-xanthanone) i

124 exes, where BPAMP is [2-(bis(2-pyridylmethyl)aminomethyl)-N-methylaniline]-phenol and M = Mn(2+), Zn(

125 plasma amine oxidase (BPAO), namely, (2-(6-(aminomethyl)naphthalen-2-yloxy)ethyl)trimethylammonium (

126 ts such as fluoro, bromo, nitro, acetyl, and aminomethyl on the isoquinoline ring resulted in a signi

127 e report the design of chiral mono-protected aminomethyl oxazoline ligands that enable desymmetrizati

128 the first time using chiral acetyl-protected aminomethyl oxazoline ligands.

129 n two complementary polymer coatings, poly(4-aminomethyl-p-xylylene-co-p-xylylene) and poly(4-formyl-

130 RT variants containing meta-Tyr, nor-Tyr, aminomethyl-Phe, and 1- and 2-naphthyl-Tyr were produced

131 l permeability, yielding azido-Phe-Leu-Leu-4-aminomethyl-Phe-methyl vinyl sulfone (4a, LU-102), and a

132 Aminomethyl-Phe115 RT incorporated dCTP more efficiently

133 ontaining these side chains suggest that the aminomethyl-Phe115 substitution provides new hydrogen bo

134 all inhibited by ethacrynic acid and certain aminomethyl phenols.

135 simple 1-(aminomethyl)-beta-naphthols and 2-(aminomethyl)-phenols.

136 yl-polyoxazole moiety is linked by a 1,3-bis(aminomethyl)phenyl group with a 5-(2-aminoethyl)- (18) o

137 S inhibition potency was achieved with N-(3-(aminomethyl)phenyl)-2-furanylamidine (77) (Ki-nNOS = 0.0

138 idine nitrogen and phenyl ring to give N-(3-(aminomethyl)phenyl)acetamidine (14) dramatically altered

139 Finally, alpha-fluoro-N-(3-(aminomethyl)phenyl)acetamidine (74) (Ki-nNOS = 0.011 mic

140 ity to N-terminal phenylalanine (Phe) and 4-(aminomethyl)phenylalanine (AMPhe) and prevents their rem

141 the preclinical development of DPC602, a 2-(aminomethyl)phenylpyrazole analogue, as a highly potent,

142 terized a new tagging reagent, (3R,4S)-1-(4-(aminomethyl)phenylsulfonyl)pyrrolidine-3,4-diol (APPD),

143 This includes aminomethyl phosphonate [AMP](2-), 1-aminoethyl phosphon

144 itively inhibited by alternative substrates (aminomethyl phosphonate [AMPA] and N-methyl glyphosate [

145 ng the concentration of glyphosate and AMPA (aminomethyl phosphonic acid, one of its major degradatio

146 tion by synthesis of an N-methyl-3-fluoro-4-(aminomethyl)piperidine urea led to compound 30 that has

147 Aminomethyl polystyrene resin was reacted with 4-(5'-for

148 Two classes of aminomethyl polystyrene resin-bound linkers of p-acetoxy

149 ating reagent was subjected to reaction with aminomethyl polystyrene resin-bound p-acetoxybenzyl alco

150 litated using a solid phase, N-(2-aminoethyl)aminomethyl polystyrene.

151 (EDA), piperazine (PPZ), and methyl 2,2-bis(aminomethyl)propionate (COOMe) cores.

152 the positively charged 4-amino-TEMPO and 3-(aminomethyl)-proxyl radical and polar 4-hydroxy-TEMPO ra

153 ariety of substitution patterns as well as 3-aminomethyl-pyrazolo[3,4-b]pyridines.

154 se novel RTILs were readily prepared from 2-(aminomethyl)pyridine and amino acid ester derived isocya

155 More than 25 new cobalt-(aminomethyl)pyridine complexes were developed as catalys

156 4-AP, 4-(aminomethyl)pyridine, 4-(methylamino)pyridine, and 4-di(

157 -morpholinylmethyl)-5-aminopyridine-, and 5-(aminomethyl)pyridine-2-carboxaldehyde thiosemicarbazones

158 Of these diamines, (R)-2-(aminomethyl)pyrrolidine is a particularly potent and sel

159 ubstituted alkenyl sulfones through an alpha-aminomethyl radical addition-elimination pathway.

160 withC bond attacks by its Calpha atom on the aminomethyl radical functionality N(Me)-CH2.

161 withC bond attacks by its Calpha atom on the aminomethyl radical functionality N(Me)-CH2. presumably

162 This was attached to aminomethyl resin and elongated using standard Fmoc prot

163 Standard manipulations produced the aminomethyl side chain.

164 he benzylic position was used to install the aminomethyl side-chain in the C(1)-aromatic substituent.

165 ferase inhibitors, we have synthesized three aminomethyl-substituted O(6)-benzylguanines and the thre

166 ituted analogs structurally derived from the aminomethyl-substituted pyrazolo[1,5- a]pyridine lead co

167 h interfering with binding, whereas the meta-aminomethyl substitution allows an interaction of the am

168 feature of this new class of ligands is a 2-aminomethyl-trans-cyclopropyl side chain attached to a s