169503-34-8Relevant academic research and scientific papers
4-Benzyl-1H-imidazoles with oxazoline termini as histamine H3 receptor agonists
Wijtmans, Maikel,Celanire, Sylvain,Snip, Erwin,Gillard, Michel R.,Gelens, Edith,Collart, Philippe P.,Venhuis, Bastiaan J.,Christophe, Bernard,Hulscher, Saskia,Van Der Goot, Henk,Lebon, Florence,Timmerman, Henk,Bakker, Remko A.,Lallemand, Bénédicte I. L. F.,Leurs, Rob,Talaga, Patrice E.,De Esch, Iwan J. P.
supporting information; experimental part, p. 2944 - 2953 (2009/04/11)
Research on the therapeutic applications of the histamine H3 receptor (H3R) has traditionally focused on antagonists/inverse agonists. In contrast, H3R agonists have received less attention despite their potential use in s
CONDENSED IMIDAZOLE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 21, (2008/06/13)
The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail
CONDENSED IMIDAZOLE DERIVATIVES AS AROMATASE INHIBITORS
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Page/Page column 18, (2008/06/13)
The application relates to novel heterocyclic compounds of the general formula (I) and salts, preferably pharmaceutically acceptable salts, thereof, in which R, R1, R2, R3, Q, m and n have the meanings explained in detail
Prenyl transferase inhibitors
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Page 46, (2008/06/13)
A family of imidazole compounds useful for inhibiting the activity of prenyl transferases. The compounds are covered by the following formula: wherein X is (CHR11)n3(CH2)n4Z(CH2)n5 where Z is O, N(R12), S, or a bond; Y is CO, CH2, CS, or a bond; R1 is or N(R24R23); and the remaining substituents are as defined in the disclosure.
Pyridone-containing farnesyltransferase inhibitors: Synthesis and biological evaluation
Hasvold, Lisa A.,Wang, Weibo,Gwaltney II, Stephen L.,Rockway, Todd W.,Nelson, Lissa T. J.,Mantei, Robert A.,Fakhoury, Stephen A.,Sullivan, Gerard M.,Li, Qun,Lin, Nan-Horng,Wang, Le,Zhang, Haiying,Cohen, Jerome,Gu, Wen-Zhen,Marsh, Kennan,Bauch, Joy,Rosenberg, Saul,Sham, Hing L.
, p. 4001 - 4005 (2007/10/03)
Farnesyltransferase inhibitors (FTIs) have been developed as potential anti-cancer agents due to their efficacy in blocking malignant growth in a variety of murine models of human tumors. To that end, we have developed a series of pyridone farnesyltransferase inhibitors with potent in vitro and cellular activity. The synthesis, SAR and biological properties of these compounds will be discussed.
Substituted imidazole derivatives and their use as histamine H3 receptor ligands
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, (2008/06/13)
Compounds of formula (I) and their pharmaceutically acceptable salts are useful as histamine H3receptor ligands. R1and R3are optional substituents such as C1to C6alkyl. R2represents a bond
INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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, (2008/06/13)
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
4-[(1H-imidazol-4-yl) methyl] benzamidines and benzylamidines: Novel antagonists of the histamine H3 receptor
Aslanian, Robert,Brown, Joan E.,Shih,Wa Mutahi, Mwangi,Green, Michael J.,She, Susan,Del Prado, Maurice,West, Robert,Hey, John
, p. 2263 - 2268 (2007/10/03)
A series of amidine substituted phenyl-, benzyl-, and phenethylimidazoles based on the known H3 against SKandF 91606 (4) has been synthesized and tested as ligands for the histamine H3 receptor. Insertion of a phenyl ring between the imidazole ring and the amidine moiety produces antagonists. The benzyl series was found to be the most potent and was further investigated. Compounds 9c and 18 (entries 5 and 12, Table 1) are potent ligands for the H3 receptor with K(i) values of 16 nM and 7.2 nM respectively. In vivo, both compounds were shown to be equipotent to thioperamide (2), the standard H3 antagonist.
