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3 protocols using 2 aminobenzothiazole

1

Evaluation of Novel Benzimidazole and Benzothiazole Compounds

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All tested compounds were at the highest purity commercially available. 2-aminobenzimidazole (ABI), 2GBI, 2-aminobenzothiazole (ABTA), and 2-guanidino-benzothiazole (GBTA) were from Sigma-Aldrich. 6-fluoro-1H-1,3-benzodiazol-2-amine (ABIFβ); 5,6-difluoro-1H-1,3-benzodiazol-2-amine (ABIF2), and 4,5,6-trifluoro-1H-1, 3-benzodiazol-2-amine (ABIF3) were from Enamine. 4-fluoro-1H-1, 3-benzodiazol-2-amine (ABIFα) was from Combi-Blocks. 3-(2-amino-5-methyl-1H-imidazol-4-yl)-1-(3,5-difluorophenyl)propan-1-one hydrochloride (HIF); 3-(2-amino-5-methyl-1H-imidazol-4-yl)-1-phenylpropan-1-one hydrochloride (HIFNF); N-[(2-amino-5-methyl-1H-imidazol-4-yl)methyl]-3,5-difluorobenzamide (HIFNH); 3-(2-amino-5-methyl-1H-imidazol-4-yl)-1-(3,5-difluorophenyl)propan-1-ol hydrochloride (HIFOH); and (2E)-3-(2-amino-5-methyl-1H-imidazol-4-yl)-1-(3,5-difluorophenyl)prop-2-en-1-one hydrochloride (HIFEN) were custom synthesized by Enamine at a minimum purity of 95% (liquid chromatography–mass spectrometry). See text at the bottom of the PDF for characterization.
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2

Synthesis and Characterization of Benzothiazole Derivatives

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All reagents, catalysts,
and chemicals utilized in the study were of analytical quality and
supplied by commercial providers. The chemicals used in this study
were sourced from various suppliers. 2-Aminobenzothiazole (Sigma-Aldrich,
99%), sulfapyridine (NENTECH, U.K., 99%), sulfaguanidine (Tokyo Chemical
Industry, Japan, 98%), piperazine (Central Dreug House, India, 99%),
benzylamine (Loba Chemi, India, 99%), cyclohexylamine (Sigma-Aldrich,
99%), 3,4 dimethylaniline (GCC, U.K., 98%), 4-chloroaniline (Sigma-Aldrich,
98%), 4-bromoaniline (Sigma-Aldrich, 90%), 4-fluoroaniline (Sigma-Aldrich,
99%), 4-nitroaniline (Janssen, Belgium, 98%), diethylamine (GCC, U.K.,
98%), m-toluidine (Sigma-Aldrich, 99%), morpholine
(Tokyo Chemical Industry, Japan, 99%), dimethylformamide (DMF) (Carlo
Erba, France, 99.9%), acetone (Carlo Erba, France, 99%), triethylamine
(TEA) (TEDIA, 99%), ethanol (Carlo Erba, France, 98%), n-hexane (Carlo Erba, France, 95%), sodium bicarbonate (NaHCO3) (GCC, U.K., 99.5%), sodium hydroxide (NaOH) (GCC, U.K.,
99.5%), chloroform (Carlo Erba, France, 99.9%), and dimethyl sulfoxide
(DMSO) (Carlo Erba, France, 99%) and monochloroacetyl chloride (α
Chemika, India) were used.
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3

Amyloid Aggregation Inhibitor Screening

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Rhodamine-B, 2-aminobenzothiazole,
and phosphorus(V) oxychloride were purchased from Sigma-Aldrich. Triethyl
amine, ThT, dry DCM, hexane, chloroform, ethyl acetate, and nitrocellulose
membrane were purchased from Merck (Germany). Silica gel was taken
from SRL. 1,1,1,3,3,3-Hexafluoroisopropanol (HFIP) was procured from
Spectrochem. 2-[4-(2-Hydroxyethyl)piperazin-1-yl]ethanesulfonic acid
and nickel chloride hexahydrate were purchased from Himedia. Copper(II)
chloride, MTT, zinc nitrate hexahydrate, cobalt chloride, 4-piperazinediethanesulfonic
acid, Dulbecco’s modified Eagle’s medium (DMEM), ethylenediaminetetraacetic
acid, and cell culture-grade dimethylsulfoxide (DMSO) were purchased
from Sigma-Aldrich. Various culture media and serum were procured
from Invitrogen. β-Amyloid (1–42) was procured from Alxotec
(Sweden). Primary antibody 6E10 was taken from Bio Legend, A11 was
taken from Thermo Scientific, and OC were taken from Millipore. All
these chemicals were used in various experiments without further purification.
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