17839-51-9Relevant academic research and scientific papers
HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 -HYDROXYSTEROID DEHYDROGENASE
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Page/Page column 47, (2010/08/07)
Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
Substituent effects on the reactivity of benzo-1,2-dithiolan-3-one 1-oxides and their possible application to the synthesis of DNA-targeting drugs
Sawwan, Nahed,Brzostowska, Edyta M.,Greer, Alexander
, p. 6968 - 6971 (2007/10/03)
The efficiency of polysulfane product generation has been investigated for n-propyl thiol reactions with ortho- and para-substituted benzo-1,2-dithiolan-3- one 1-oxides in acetonitrile-water (7:3) mixtures. The reaction is facilitated by reducing the electron density at the para position or by placing substituents bearing lone pair electrons ortho to the dithiolanone-oxide (S1) reaction center. Through-space and through-bond effects both contribute to the conversion of polysulfane products.
Novel inhibitors of the prenylated protein methyltransferase reveal distinctive structural requirements
Marciano, Daniele,Aharonson, Ziporet,Varsano, Tal,Haklai, Roni,Kloog, Yoel
, p. 1709 - 1714 (2007/10/03)
Inhibitors of a prenylated protein methyltransferase were synthesized and evaluated. S-farnesyl-5-fluorothiosalicylic acid and the 5-chloro analog (but not the 4-fluoro, 4-chloro or 3-chloro analogs) were potent inhibitors, as was the parent compound S-farnesyl thiosalicylic acid (FTS), whose methyl ester was far less active. S-geranyl and S-geranylgeranyl thiosalicylic acids were more than ten times less potent than FTS.
7-Substituted Benzothiophenes and 1,2-Benzisothiazoles. Part 2. Chloro and Nitro Derivatives
Rahman, Loay K. A.,Scrowston, Richard M.
, p. 385 - 390 (2007/10/02)
The 7-chloro and 7-nitro derivatives of benzothiophene and 1,2-benzisothiazole have been prepared from readily available precursors, which for each substituent are common to both ring systems. 7-Chlorobenzothiophene has been obtained from 3-chloro-2-mercaptobenzoic acid via 7-chlorobenzothiophen-3(2H)-one, or from 2,3-dichlorobenzaldehyde, either via β-(2,3-dichlorophenyl)-α-mercaptoacrylic acid (16) or, preferably, via 7-chlorobenzothiophene-2-carboxylic acid.Hexamethylphosphoric triamide is a particularly useful solvent in which to effect the selective nucleophilic replacement of the 2-chloro substituent in 2,3-dichlorobenzaldehyde. 7-Chloro-1,2-benzisothiazole is available by treatment of 3-chloro-2-mercaptobenzaldehyde with chloramine (57percent), or by heating 2,3-dichlorobenzaldehyde with sulphur and aqueous ammonia (46percent). 7-Nitrobenzothiophene has been obtained by treatment of 2-bromo-3-nitrobenzaldehyde with mercaptoacetic acid under alkaline conditions, followed by decarboxylation of the resulting 2-carboxylic acid.Cyclisation of 2-(n- or t-butylthio)-3-nitrobenzaldoxime with polyphosphoric acid gives 7-nitro-1,2-benzisothiazole in high yield. 3-Nitro-2-t-bytylthiobenzaldehyde behaves unexpectedly with chloramine, to give what is believed to be 7-nitro-2-t-butyl-1,2-benzothiazolium chloride (24) (73percent).
Aroyl-aminoacids, amides and esters thereof
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, (2008/06/13)
Compounds of the structure STR1 wherein: Q is oxygen, sulfur or imino.X and Y are hydrogen, halogen, hydroxy, alkoxy, trifluoromethyl, nitro, carboxy, cyano, sulfonamido, sulfhydryl, alkyl, alkenyl, alkynyl, alkanoyl, alkylmercapto, amino, alkylamino, dialkylamino, alkysulfinyl, and alkylsulfonyl and may be the same or different;R 1 is hydrogen, alkanoyl, substituted alkanoyl wherein the substituent is hydroxy, amino or cycloalkyl, aroyl, arylalkanoyl, or cycloalkylcarbonyl,n is an integer from 1 to 4 inclusive,R 2 and R 3 are hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, aryl, aralkyl, and substituted derivatives thereof wherein the substituents are hydroxy, amino, alkylamino, dialkylamino, alkoxy, halogen, hydroxy, mercapto, alkylmercapto and nitro, and may be the same or different;M is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, and hetero; andZ is hydroxy, amino, alkylamino, dialkylamino, or alkoxy,have angiotensin converting enzyme inhibitory activity.
Aroylaminoacid disulfides
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, (2008/06/13)
Compounds of the structure STR1 wherein: P and Q are independently hydrogen, halo, CF 3, OR 1, SR 1, sulfamoyl, alkyl and NR 1 R 2 ;R 1, and R 2 are independently hydrogen, alkyl, aminoalky, aryl, aralkyl, heteroaryl or cycloalkyl;Y is OH, OR 1, NH 2, or, N(R 1 R 2); andM is alkyl, cycloalkyl, aryl, aminoalkyl, aralkyl, heteroaryl or heterocyclicwherein:the alkyl groups and the alkyl moieties of aminoalkyl, alkoxy and thioalkyl contain from 1 to 6 carbon atoms; the cycloalkyl group contains from 3 to 8 carbon atoms; the aryl group contains from 6 to 10 carbon atoms; the aralkyl group contains from 7 to 16 carbon atoms; and the hetero group is selected from pyrrolidyl, piperidinyl, morpholinyl, pyridyl, quinolinyl, furyl, furfuryl and thienyl; and where Y is a hydroxy, their pharmaceutically acceptable, non-toxic alkali, alkaline earth and amine salts, have angiotensin converting enzyme inhibitory activity.
