ライフサイエンスコーパス: benzenesulfonamide

1 nd developed a series of molecules (thiazole benzenesulfonamides).

2 drogenative coupling of benzyl alcohols with benzenesulfonamide.

3 2,4,6-trimethyl-N-[3-(trifluoromethyl)phenyl]benzenesulfonamide.

4 stabilized by electronically modulating the benzenesulfonamide.

5 ising from 3-((9H-purin-6-yl)amino)-N-methyl-benzenesulfonamide (1) is disclosed along with fundament

6 When two molecules of a benzenesulfonamide (1) were bound simultaneously to one

7 hiazol-2-yl)thio)phenyl)-4-(trifluorome thyl)benzenesulfonamide (1, T2384) revealed two orthosteric p

8 1-aryl-3,4-dihydro-1H-isoquinolin-2-carbonyl)benzenesulfonamides (23-33) was designed.

9 th 4-(3,4-dihydro-1H-isoquinoline-2-carbonyl)benzenesulfonamide (3) (PDB code 4Z1J ), a novel series

10 4-(4-fluorophenyl)-5-hydroxy-2H-pyrazol-3-yl]benzenesulfonamide 31 template readily synthesized from

11 ber (4-[125I]iodo-N-[2-(1'-piperidinyl)ethyl]benzenesulfonamide, 4-[125I]IPBS) was accomplished in hi

12 -([1,1'-biphenyl]-3-yl)-9H-purin-2-yl)amino) benzenesulfonamide (73) that exhibited high potency towa

13 -II) analyte and immobilized 4-(2-aminoethyl)benzenesulfonamide (ABS) ligand display a 100-fold (20 d

14 rbonic anhydrase inhibitors, 4-(2-aminoethyl)benzenesulfonamide (AEBS) and 4-aminobenzensulfonamide (

15 CAII) binding to immobilized 4-(2-aminoethyl)benzenesulfonamide (AEBSA) to examine the efficiency and

16 single molecule, 4-methyl-N-9H-xanthen-9-yl-benzenesulfonamide (AH-7614), has been described as an F

17 -ray evidence) derived from N-oxiranylmethyl benzenesulfonamide and beta-chloro-cinnamaldehyde as an

18 metal-free reaction between N-oxiranylmethyl benzenesulfonamide and beta-chloro-cinnamaldehyde, depen

19 e) and its elaboration by introduction of C4-benzenesulfonamide and C7- and C8-7-deazapurine substitu

20 Benzenesulfonamide and carbonic anhydrase have been chos

21 Benzenesulfonamide and iminodiacetate (IDA)-conjugated C

22 hydrase-II (hCA-II) as the enzyme source and benzenesulfonamide and its derivatives as inhibitors.

23 onic anhydrase and vancomycin to immobilized benzenesulfonamide and N-alpha-Ac-Lys-D-Ala-D-Ala groups

24 4-(Trifluoromethyl)benzenesulfonamide and N-bromosuccinimide were used as t

25 ions of series of ligands containing coupled benzenesulfonamide and oligoethylene glycol moieties (H2

26 rafts reaction of 4-methyl-N-(pent-4-yn-1-yl)benzenesulfonamides and aldehydes in good yields.

27 oped a series of nearly 50 ortho-substituted benzenesulfonamides and experimentally measured their in

28 asses consisting of N-[2-(diethylamino)ethyl]benzenesulfonamides and N-[2-(diethylamino)ethyl]benzene

29 carbonic anhydrase fusion protein that binds benzenesulfonamides and that also includes the RGD pepti

30 d carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors.

31 l)-3-(1-methylpiperidin-4-ylamino)-4-methoxy benzenesulfonamide as potent and selective 5-HT(6) recep

32 ies of cyclohexylamine- and piperidine-based benzenesulfonamides as potent and selective Nav1.7 inhib

33 -methyl]-phen yl}-4-nitro-3-trifluoro-methyl-benzenesulfonamide) as the lead agent.

34 scribes novel N-sulfonyl-aminobiaryl (biaryl-benzenesulfonamides) as potent anticancer agents targeti

35 A series of small molecule benzenesulfonamide based CA-IX inhibitors containing nov

36 synthesis of asymmetrical ureido-containing benzenesulfonamides based on in situ generation of the c

37 ization of a previously identified series of benzenesulfonamide-based perforin inhibitors for their p

38 ion of a 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide-based scaffold.

39 Benzenesulfonamides bearing various substituted (hetero)

40 ibitor design, we generated four families of benzenesulfonamide (BSA) derivatives for SAR analysis.

41 zenesulfonamide-CAII than that for ortho-NO2-benzenesulfonamide-CAII complex.

42 phase stability for the complex of para-NO2-benzenesulfonamide-CAII than that for ortho-NO2-benzenes

43 s postulate is explored here by three-tailed benzenesulfonamide CAIs (TTI) to fully exploit such amin

44 Moreover, the precursor N-(benzenesulfonyl)benzenesulfonamide can be recovered and transformed to N

45 the structure-kinetic relationship in hCAII/benzenesulfonamide complexes, depicting a paradigmatic s

46 2-Nitro-N-alkyl-N-(2-oxo-2-phenylethyl)benzenesulfonamide compounds are known to undergo base-m

47 ein we report the synthesis of two series of benzenesulfonamide containing compounds that incorporate

48 The ionized NH(-) group of each benzenesulfonamide coordinates to the active site Zn(2+)

49 se results demonstrate that radiohalogenated benzenesulfonamides could be a potentially useful class

50 Evaluation of various para-substituted benzenesulfonamides defined a substituent effect on bind

51 We found that compound LF3, a 4-thioureido-benzenesulfonamide derivative, robustly inhibited this i

52 We report two series of novel benzenesulfonamide derivatives acting as effective carbo

53 the target CA active sites was planned with benzenesulfonamide derivatives and, for the first time,

54 diselenobisbenzoic scaffold, amino acid, and benzenesulfonamide derivatives were prepared and biologi

55 hip (SAR) study was carried out with 32 such benzenesulfonamides differing in tails combination that

56 the substituted aminobenzene, benzoate, and benzenesulfonamide disulfide subclasses.

57 -methyl-N-methyl-N-(2-phenyl-2H-pyrazol-3-yl)benzenesulfonamide (DMZ), was determined by X-ray crysta

58 potency of L2 is diminished (to the level of benzenesulfonamide) either in the presence of EDTA or up

59 (4'-cyano-3'-fluoro-biphenyl-2-yl)-4-methoxy-benzenesulfonamide] exhibits remarkable antiproliferativ

60 -dichloro-N-methyl-N-(2-methyl-4-nitrophenyl)benzenesulfonamide (FH535-M), was inactive as an uncoupl

61 Achmatowicz oxidation of a furyl-substituted benzenesulfonamide followed by a conjugate addition to t

62 L1 and L2, vis-a-vis their parent compound, benzenesulfonamide, for recombinant human carbonic anhyd

63 bitor of the coumarin and chromone type with benzenesulfonamide fragments as highly effective CAIs.

64 amino groups of the dendrimer with 4-carboxy-benzenesulfonamide functionalities.

65 gn of short molecular linkers connecting the benzenesulfonamide group and a para-substituted tail gro

66 In solution, the benzenesulfonamide group coordinates as an anion to a Zn

67 vulsant thiazolidine-2,4-diones with pendant benzenesulfonamide group that target epilepsy-associated

68 vity appears to reside in the inability of a benzenesulfonamide group to bind at the equivalent of th

69 rawing electrons and lowering the pKa of the benzenesulfonamide group.

70 ]indol-8-ylidene)methyl]amino}-N-(2- pyridyl)benzenesulfonamide (GW8510) or the inactive congener iso

71 -dimethyl-3-pyridinyl)oxy]-2-pyridinyl}amino)benzenesulfonamide] (IC(50) = 18 and 47 nM, respectively

72 compound, 4-dodecyl-N-(1,3,4-thiadiazol-2-yl)benzenesulfonamide, inhibited AKT and its downstream tar

73 isozymes I and II, the binding affinities of benzenesulfonamide inhibitors are invariably higher with

74 carbonic anhydrase II (CAII, EC 4.2.1.1) and benzenesulfonamide inhibitors in the gas phase.

75 non, we have designed and synthesized simple benzenesulfonamide inhibitors substituted at the para po

76 substituted N-methyl-3-(pyrimidin-4-ylamino)benzenesulfonamide inhibitors that display excellent pot

77 and in the case of binding of p-substituted benzenesulfonamide inhibitors to bovine carbonic anhydra

78 The N-oxiranylmethyl benzenesulfonamide itself upon heating gives readily sep

79 pling of the in situ generated aldehyde with benzenesulfonamide leads to the desired product.

80 ho position of N-(3,4-dimethyl-5-isoxazolyl) benzenesulfonamide led to the identification of the biph

81 in can bind to a monolayer that presents the benzenesulfonamide ligand, thereby positioning the RGD p

82 Monovalent carbonic anhydrase (CA) binds to benzenesulfonamide ligands presented on the surface of t

83 onic anhydrase II (BCA) and para-substituted benzenesulfonamide ligands with chains of 1-5 glycine su

84 against all 48 human nuclear receptors, the benzenesulfonamide liver X receptor (LXR) agonist N-(2,2

85 cture-activity relationships of xanthin-8-yl-benzenesulfonamides mainly by introducing a variety of l

86 h both the 3-(morpholinosulfonyl)anilino and benzenesulfonamide moieties in these compounds are criti

87 midoamine) (PAMAM) dendrimers decorated with benzenesulfonamide moieties were prepared by derivatizin

88 The 1,2,3-triazole with a benzenesulfonamide motif is present in the produced mole

89 Although a benzenesulfonamide (or related arylsulfonamide) group mi

90 carbonic anhydrase enriched macrocycles with benzenesulfonamide pharmacophore and nanomolar K(d).

91 analogues possessing a substituted thiazole benzenesulfonamide pharmacophore that are potent human b

92 The process affords alkylated benzenesulfonamides poised for medicinal chemistry appli

93 structure-affinity studies indicate that the benzenesulfonamide portion of the phenylethylamine and p

94 Each inhibitor contains a benzenesulfonamide prong and a cupric iminodiacetate (ID

95 The efficient one-pot conversion of the benzenesulfonamide-protected pyrrolidine 9 to the Cbz-pr

96 para-substituted n-alkyl and hydroxyethylene-benzenesulfonamides, providing a complete reconstruction

97 compound of this series, namely, 4-sulfamido-benzenesulfonamide, revealed the binding of two molecule

98 The in vitro binding affinity of the benzenesulfonamide rhenium complexes yielded IC(50) valu

99 lphenyl)-3-(trifluoromethyl)- H-pyrazol-1-yl]benzenesulfonamide, SC-58635, celecoxib), which is curre

100 , featured by an innovative N-(5-pyrimidinyl)benzenesulfonamide scaffold and promising low micromolar

101 augmenting the substituents attached to the benzenesulfonamide scaffold in three ways, namely, subst

102 (4-(((3,4,5-trimethoxyphenyl)tellanyl)methyl)benzenesulfonamide) showed an IC(50) of 0.02 muM being h

103 (2-(4-substitued piperazin-1-yl)ethyl)ureido)benzenesulfonamides, showed low nanomolar inhibitory act

104 (3-(2,4-difluorophenyl)-oxoimidazolidin-1-yl)benzenesulfonamide (SLC-149), is evaluated on CAIX and a

105 n of 4-(nitroso)-N-(5-methyl-1,2-oxazol-3-yl)benzenesulfonamide (SMX-NO), the reactive metabolite of

106 A benzenesulfonamide substituent at the N-terminus of the

107 1-hydroxy-1-(trifluoromethyl)-eth yl]phenyl]-benzenesulfonamide (T0901317) and 3-[3-[N-(2-chloro-3-tr

108 -1-hydroxy-1-(trifluoromethyl)ethyl ]phenyl]-benzenesulfonamide (T0901317) inhibited transactivation

109 2-(phenylcarbonyl)hydrazino]carbonyl] benzyl]benzenesulfonamide (TCN 201) produced smaller but not st

110 inity of L1 for hCA-I was similar to that of benzenesulfonamide, the binding affinity of L2 was appro

111 ty approached that of fragment sized primary benzenesulfonamides, the classical zinc binding group fo

112 tituted with linkers of varying lengths to p-benzenesulfonamide to yield nondiastereomeric biosensors

113 erted N-alkyl-2-nitro-N-(2-oxo-2-aryl-ethyl)-benzenesulfonamides to 2H-indazoles 1-oxides under mild

114 -1-hydroxy-1-trifluoromethyl-ethyl )-phenyl]-benzenesulfonamide (TO-901317), which is a potent stimul

115 Herein, novel 4-(pyrazolyl)benzenesulfonamide ureas (SH7a-t) were developed and eva

116 sible N-alkyl-2-nitro-N-(2-oxo-2-aryl-ethyl)-benzenesulfonamides using glycine, 2-nitrobenzenesulfony

117 By attaching IDA-bound Cu(2+) to benzenesulfonamide via different chain length spacers, w

118 attachment of iminodiacetate (IDA)-Cu(2+) to benzenesulfonamide (via a triethylene glycol spacer) enh

119 nal H-bond between the amine and neighboring benzenesulfonamide was stabilized by electronically modu

120 2,4-Disubsituted benzenesulfonamides were identified as potent inhibitors

121 naphthyl, and various heteroaryl substituted benzenesulfonamides which displayed subnanomolar hCA IX

122 Starting from the trifluorinated benzenesulfonamide with cyclooctylamino substituent at t

123 onic anhydrase II (BCA) and para-substituted benzenesulfonamides with chains of oligoglycine, oligosa

124 A series of fluorinated benzenesulfonamides with substituents on the benzene rin

125 synthesized di-meta-substituted fluorinated benzenesulfonamides with up to 10-fold affinity improvem