537702-33-3Relevant academic research and scientific papers
Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a] benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi
Oh, Sangmi,Kim, Sungbum,Kong, Sunju,Yang, Gyongseon,Lee, Nakyung,Han, Dawoon,Goo, Junghyun,Siqueira-Neto, Jair L.,Freitas-Junior, Lucio H.,Song, Rita
, p. 395 - 403 (2014/08/05)
A high-throughput (HTS) and high-content screening (HCS) campaign of a commercial library identified 2,3-dihydroimidazo[1,2-a]benzimidazole analogues as a novel class of anti-parasitic agents. A series of synthetic derivatives were evaluated for their in vitro anti-leishmanial and anti-trypanosomal activities against Leishmania donovani and Trypanosoma cruzi, which have been known as the causative parasites for visceral leishmaniasis and Chagas disease, respectively. In the case of Leishmania, the compounds were tested in both intracellular amastigote and extracellular promastigote assays. Compounds 4 and 24 showed promising anti-leishmanial activity against intracellular L. donovani (3.05 and 5.29 μM, respectively) and anti-trypanosomal activity against T. cruzi (1.10 and 2.10 μM, respectively) without serious cytotoxicity toward THP-1 and U2OS cell lines.
Synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-a] benzimidazole derivatives against Leishmania donovani and Trypanosoma cruzi
Oh, Sangmi,Kim, Sungbum,Kong, Sunju,Yang, Gyongseon,Lee, Nakyung,Han, Dawoon,Goo, Junghyun,Siqueira-Neto, Jair L.,Freitas-Junior, Lucio H.,Song, Rita
, p. 395 - 403 (2015/03/13)
A high-throughput (HTS) and high-content screening (HCS) campaign of a commercial library identified 2,3-dihydroimidazo[1,2-a]benzimidazole analogues as a novel class of anti-parasitic agents. A series of synthetic derivatives were evaluated for their in vitro anti-leishmanial and anti-trypanosomal activities against Leishmania donovani and Trypanosoma cruzi, which have been known as the causative parasites for visceral leishmaniasis and Chagas disease, respectively. In the case of Leishmania, the compounds were tested in both intracellular amastigote and extracellular promastigote assays. Compounds 4 and 24 showed promising anti-leishmanial activity against intracellular L. donovani (3.05 and 5.29 μM, respectively) and anti-trypanosomal activity against T. cruzi (1.10 and 2.10 mM, respectively) without serious cytotoxicity toward THP-1 and U2OS cell lines.
Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists
Sasmal, Pradip K.,Sasmal, Sanjita,Rao, P. Tirumala,Venkatesham,Roshaiah,Abbineni, Chandrasekhar,Khanna, Ish,Jadhav, Vikram P.,Suresh,Talwar, Rashmi,Muzeeb, Syed,Receveur, Jean-Marie,Frimurer, Thomas M.,Rist, ?ystein,Elster, Lisbeth,H?gberg, Thomas
scheme or table, p. 5443 - 5448 (2011/01/03)
Melanin concentrating hormone (MCH) is an important mediator of energy homeostasis and plays role in several disorders such as obesity, stress, depression and anxiety. The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss with a lead compound from this series is exemplified.
SUBSTITUTED CYCLIC UREA DERIVATIVES AND THE USE THEREOF AS VANILLOID RECEPTOR 1 MODULATORS
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Page/Page column 80-81, (2010/11/24)
The invention relates to substituted cyclic urea derivatives, wherein X represents O, S or N-C=N; m is 1 or 2; n is 1 or 2; p1 and p2 represent independently 0, 1, 2 or 3, and the sum of p1 and p2 is 0, 1, 2 or 3. The invention also relates to methods for producing said derivatives, to drugs containing these compounds and to the use of these compounds for producing drugs. The inventive drugs are especially useful for vanilloid receptor 1 (VR1/TRPV1) regulation, preferably for vanilloid receptor 1 (VR1/TRPV1) inhibition and/or vanilloid receptor 1 (VR1/TRPV1) stimulation.
