158941-08-3Relevant academic research and scientific papers
Discovery of rimonabant and its potential analogues as anti-TB drug candidates
Gajbhiye,More,Patil, Manoj D.,Ummanni,Kotapalli,Yogeeswari,Sriram,Masand
, p. 2960 - 2971 (2015/03/14)
Rimonabant and its analogues have been synthesized in moderate to good yields using a simple synthetic route. All the newly synthesized compounds were subjected to in vitro screening against M. tuberculosis and M. smegmatis. The most potent analogue JMG-14 exhibits MIC value of 3.13 compared to 3.25 and 50 μ/ml for ethambutol and pyrazinamide, respectively. The molecular docking reveals that pyrazole ring, number and position of halogen atoms play a crucial role in deciding interactions with MTCYP-121. These findings open up a new avenue in the search of potent anti-TB drugs with rimonabant and its novel analogue JMG-14 as lead molecules.
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H- pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobes
Wu, Chien-Huang,Hung, Ming-Shiu,Song, Jen-Shin,Yeh, Teng-Kuang,Chou, Ming-Chen,Chu, Cheng-Ming,Jan, Jiing-Jyh,Hsieh, Min-Tsang,Tseng, Shi-Liang,Chang, Chun-Ping,Hsieh, Wan-Ping,Lin, Yinchiu,Yeh, Yen-Nan,Chung, Wan-Ling,Kuo, Chun-Wei,Lin, Chin-Yu,Shy, Horng-Shing,Chao, Yu-Sheng,Shia, Kak-Shan
experimental part, p. 4496 - 4510 (2010/03/01)
By using the active metabolite 5 as an initial template, further structural modifications led to the identification of the titled compound 24 (BPR-890) as a highly potent CB1 inverse agonist possessing an excellent CB2/1 selectivity and remarkable in vivo
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: Development of central cannabinoid receptor ligands with lower lipophilicity
Katoch-Rouse, Reeti,Pavlova, Olga A.,Caulder, Tara,Hoffman, Alexander F.,Mukhin, Alexey G.,Horti, Andrew G.
, p. 642 - 645 (2007/10/03)
Exploration of the central CB1 cannabinoid receptors using positron emission tomography (PET) will allow for an understanding of the pharmacological and physiological role played by these receptors in the CNS. Current tracers are highly lipophi
Pyrazole-3-carboxamide derivatives, process for their preparation and pharmaceutical compositions in which they are present
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, (2008/06/13)
The present invention relates to novel pyrazole-3-carboxamide derivatives of the formula STR1 in which the substituents are as defined in the specification. The present invention further relates to a process for the preparation of these novel derivatives and to the pharmaceutical compositions in which they are present.
