cas 36765-84-1, 3-NITROPHENACYLAMINE HYDROCHLORIDE | Articles data ｜lookchem

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36765-84-1

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Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates
The present work reports on the synthesis, biological assaying and docking studies of a series of 12 aryl thiosemicarbazones, which were planned to act over two main enzymes, cruzain and trypanothione reductase. These enzymes are used as targets of trypanocidal activity in Chagas disease control with a minimal mutagenic profile. Three p-nitroaromatic thiosemicarbazones showed high activity against Trypanosoma cruzi in in vitro assays (IC50 57 μM), and no mutagenic profile was observed in micronucleous tests. Although the in vitro inhibition test showed that 10-μM doses of eight compounds inhibited cruzain activity, no correlation was found between cruzain inhibition and trypanocidal activity.
Blau, Lorena,Menegon, Renato Farina,Trossini, Gustavo H. G.,Molino, Jo?o Vitor Dutra,Vital, Drielli Gomes,Cicarelli, Regina Maria Barretto,Passerini, Gabriela Duó,Bosquesi, Priscila Longhin,Chin, Chung Man
p. 142 - 151
(2013/10/01)

Separation and Stereochemical Assignment of Erythro and Threo Isomers of the m-Nitro Analogue of (+/-)-Chloramphenicol
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Hill, Richard K.,Nugara, Peter N.,Holt, Elizabeth M.,Holland, Kathleen P.
p. 1045 - 1047
(2007/10/02)

Thiadizines
Novel heterocyclic compounds of the formula: STR1 wherein either X is --CR1 R2 -- and Y is oxygen, sulphur or --NR3, wherein R1, R2 and R3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or --NH-- and Y is --CH2 --; wherein R4 and R5, which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in claim 1, provided that R4 and R5 are not both hydrogen; or wherein R4 and R5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate. These compounds possess cardiotonic properties, and some of them possess peripheral vasodilator properties, and they are useful for the treatment of acute or chronic heart failure. Representative of the compounds is N,N-dimethyl-p-(5,6-dihydro-5-oxo-4H-1,3,4-thiadiazin-2-yl)benzamide. Also disclosed are processes for the manufacture of the compounds and pharmaceutical compositions containing them.
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(2008/06/13)

Not available
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REICHERT,BAEGE
p. 451 - 453
(2007/10/04)

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Chemical Properties

Melting Point: 210-212°C (dec.)
Boiling Point: 299.1°Cat760mmHg
Flash Point:134.7°C
Density: g/cm³
Vapor Pressure: 0.00122mmHg at 25°C
PSA: 88.91000
LogP: 2.76170

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