61429-74-1Relevant academic research and scientific papers
Chroman-4-one derivatives targeting pteridine reductase 1 and showing anti-parasitic activity
Di Pisa, Flavio,Landi, Giacomo,Dello Iacono, Lucia,Pozzi, Cecilia,Borsari, Chiara,Ferrari, Stefania,Santucci, Matteo,Santarem, Nuno,Cordeiro-Da-Silva, Anabela,Moraes, Carolina B.,Alcantara, Laura M.,Fontana, Vanessa,Freitas-Junior, Lucio H.,Gul, Sheraz,Kuzikov, Maria,Behrens, Birte,P?hner, Ina,Wade, Rebecca C.,Costi, Maria Paola,Mangani, Stefano
, (2017)
Flavonoids have previously been identified as antiparasitic agents and pteridine reductase 1 (PTR1) inhibitors. Herein, we focus our attention on the chroman-4-one scaffold. Three chroman-4-one analogues (1-3) of previously published chromen-4-one derivat
Comparing Drug Images and Repurposing Drugs with BioGPS and FLAPdock: The Thymidylate Synthase Case
Siragusa, Lydia,Luciani, Rosaria,Borsari, Chiara,Ferrari, Stefania,Costi, Maria Paola,Cruciani, Gabriele,Spyrakis, Francesca
, p. 1653 - 1666 (2016/08/28)
Repurposing and repositioning drugs has become a frequently pursued and successful strategy in the current era, as new chemical entities are increasingly difficult to find and get approved. Herein we report an integrated BioGPS/FLAPdock pipeline for rapid
NEW COMPOUNDS, WHICH ARE POTENT INHIBITORS OF NA/CA EXCHANGE MECHANISM AND ARE USEFUL IN THE TREATMENT OF ARRHYTHMIAS
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Page/Page column 55-56, (2010/02/11)
Therapeutically active compounds of formula (I): wherein X is -O-, -CH2- or -C(O)-; Z is -CHR9- or valence bond; Y is -CH2-, -C(O)-, CH(OR10)-, -CH(NR11R12 )-, -O-, -S-, -S(O)- or -S(O2)-, provided that in case Z is a valence bond, Y is not C(O); the dashed line represents an optional double bond in which case Z is -CR9- and Y is -CH-, C(OR10)- or -C(NR11R12 )-; R1 is -(CH2)nNR4R7 or one of the following groups:n is 1 - 4; R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, -NHR8 or -COOH; R4 and R7 are independently H, lower alkyl or lower hydroxyalkyl; R5 is H, lower alkoxy, -CF3, -NH2 or -CN; R6 is -NO2 , -NR14R19, -CF3 or R8 and R16 are independently H or acyl; R9 is H or lower alkyl; R10 is H, alkylsulfonyl or acyl; R11 and R12 are independently H, lower alkyl or acyl; R13 and R18 are independently H or -OR20; R14 and R19 are independently H, acyl, alkylsulfonyl, C(S)NHR17 or C(O)NHR17; R15 is H or NH2; R17 is H or lower alkyl; R20 is H or acyl; and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds are potent inhibitors of Na/Ca exchange mechanism.
PYRIDINE DERIVATIVES USEFUL FOR INHIBITING SODIUM/CALCIUM EXCHANGE SYSTEM
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Page 53, (2008/06/13)
Therapeutically active compounds of formula (I) or (II) wherein X is -O-, -CH2- or -C(O)-; Z is -CHR12- or a valence bond; Y is -CH2-, -C(O)-, CH(OR13)-, -O-, -S-; provided that in case Z is a valence bond, Y is not C(O); the dashed line representing an optional double bond in which case Z is -CR12- -and Y is -CH2-, -C(O)- or -CH(OR10)- (in formula II) or -CH- (in formula I); R2 and R3 are independently H, lower alkyl, lower alkoxy, -NO2, halogen, -CF3, -OH, benzyloxy or a group of formula (IIIa). R1 is H, CN, halogen, -CONH2, -COOR15, CH2NR15R18, NHC(O)R5, NHCH2R5, NHR20, NR21R22, NHC(NH)NHCH3 or, in case the compound is of formula (II) wherein the optional double bond exists or in case R2 or R3 is benzyloxy or a group of formula (IIIa) or in case the pyridine ring of formula (I) or (II) is attached to the oxygen atom in 3-, 4- or 5-position, R1 can also be -NO2 or NR16R17; R4 is H, -NO2, CN, halogen, -CONH2, -COOR15, -CH2NR15R18, -NR16R17, NHC(O)R5 or -NHC(NH)NHCH3; R5 is alkyl substituted with 1-3 substituents selected from the group consisting of halogen, amino and hydroxy, or carboxyalkyl, in which the alkyl portion is optionally substituted with 1-3 substituents selected from the group consisting of halogen, amino and hydroxyl, -CHR6NR,R8 or one of the following groups: formula (IVa), (IVb), (IVc), (IVd), (IVe), and pharmaceutically acceptable salts and esters thereof. The compounds are potent inhibitors of Na+/Ca2+ exchange mechanism.
