128540-23-8Relevant articles and documents
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 77, (2012/06/30)
The invention provides compounds of Formula (I) : wherein R1 is hydrogen, OH, halo, -CN, -NO2, -N=0, -NHOQ2, -OQ2, -SOQ2, -SO2Q2, -SON(Q2)2, - SO2N(Q2)2, -N(Q2)2, -C(O)OQ2, -C(O)Q2, -C(O)N(Q2)2, -C(=NQ2)NQ2, -NQ2C(=NQ2)NQ2, - C(O)N(Q2)(OQ2), -N(Q2)C(O)-Q2, -N(Q2)C(O)N(Q2)2, -N(Q2)C(O)O-Q2, -N(Q2)SO2Q2, -N(Q2)SOQ2, aliphatic, alkoxy, cycloaliphatic, aryl, arylalkyl, heterocyclic, or heteroaryl ring, each aliphatic, alkoxy, cycloaliphatic, aryl, arylalkyl, heterocyclic, and heteroaryl ring optionally including 1-3 substituents independently selected Q3; R2 and R3 are each independently hydrogen, OH, oxo, aliphatic, cycloaliphatic, heterocycloaliphatic, aryl, or heteroaryl, optionally substituted with 1-3 of Q1 or Q2; X is a branched or straight C1-12 aliphatic chain wherein up to two carbon units are optionally and independently replaced by -C(Q1)2-, -C(Q2)2-, CHQ1, CHQ2-, -CO-, -CS-, -CONQ2, -CO2-, -OCO-, -NQ2-, -NQ2CO2-, - O-, -NQ2CONQ2-, -OCONQ2-, -NQ2CO-, -S-, -SO-, -SO2-, -SO2NQ2-, -NQ2SO2-, or -NQ2SO2NQ2-; G and G1 are each independently a branched or straight C1-2 aliphatic chain, or heterocycloalkyl, wherein up to two carbon units are optionally and independently replaced by -C(Q1)2-, -C(Q2)2-, CHQ1, CHQ2-, -CO-, - CS-, -CONQ2, -CO2-, -OCO-, -NQ2-, -NQ2CO2-, -O-, -NQ2CONQ2-, -OCONQ2-, -NQ2CO-, -S-, -SO-, - SO2-, -SO2NQ2-, -NQ2SO2-, or -NQ2SO2NQ2-, and pharmaceutically acceptable salts, solvates or prodaigs thereof, as well as methods of treating estrogen receptor mediated diseases and disorders using the compounds of Formula (I).
Synthesis and optimization of antitubercular activities in a series of 4-(aryloxy)phenyl cyclopropyl methanols
Bisht, Surendra S.,Dwivedi, Namrata,Chaturvedi, Vinita,Anand, Namrata,Misra, Mridul,Sharma, Rahul,Kumar, Brijesh,Dwivedi, Richa,Singh, Shyam,Sinha, Sudhir Kumar,Gupta, Versha,Mishra,Dwivedi, Anil K.,Tripathi, Rama P.
experimental part, p. 5965 - 5978 (2011/01/13)
A series of [4-(aryloxy)phenyl]cyclopropyl methanones were synthesized by reaction of different benzyl alcohols with 4-chloro-4′-fluorobutyrophenone in DMF in the presence of NaH/TBAB. The methanones were further reduced to respective methanols. The antitubercular activity of these compounds was evaluated in vitro against Mycobacterium tuberculosis H37Rv. Compounds 19, 21, 35, 36 and 37 have shown minimum inhibitory concentration (MIC) of 3.12 μg/mL, while compounds 14, 25 and 18 have shown MIC of 1.56 μg/mL and 0.78 μg/mL respectively. One of the compounds, cyclopropyl-4-[4-(2-piperidin-1- yl-ethoxy)benzyloxy]phenyl}methanol (36) showed 98% killing of intracellular bacilli in mouse bone marrow derived macrophages and was active against MDR, XDR and rifampicin clinical isolates resistant strains with MIC 12.5 μg/mL. Compound 36 was orally active in vivo in mice against M. tuberculosis H37Rv with an increase in MST by 6 days with 1 log reduction in the bacillary density in lungs as compared to control on 30th day after infection.
5-[4-(ω-Dialkylaminoalkoxy)phenylmethylene]-1,3,3-trimethyl-2- oxabicyclo[2.2.2]octan-6-ones with platelet antiaggregating and other activities
Mariani,Bargagna,Longobardi,Schenone,Vitagliano,Cenicola,Losasso,Russo,Marmo
, p. 657 - 668 (2007/10/02)
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