- A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2′,4′-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-Tetrahydrobenzo[6,7]cyclohepta[1,2-c ]pyrazole-3-carboxamide and analogue derivatives
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8-Chloro-1-(2′,4′-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-Tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide 9a was discovered as potent and selective CB1 antagonist by part of our group few years ago. In particular it was reported to
- Lazzari, Paolo,Distinto, Rita,Manca, Ilaria,Baillie, Gemma,Murineddu, Gabriele,Pira, Marilena,Falzoi, Matteo,Sani, Monica,Morales, Paula,Ross, Ruth,Zanda, Matteo,Jagerovic, Nadine,Pinna, Gérard Aimè
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p. 194 - 208
(2016/06/09)
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- PHARMACEUTICAL COMPOUNDS
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Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A′ are as defined in the description.B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3?, SO3H, COO?, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.
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- Pharmaceutical compounds wiht angiogenesis inbhibitory activity
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Compounds of formula (I): wherein: A, R, T, Q, L, Z, G, X and A' are as defined in the description. B and D, equal to or different from each other, are selected between heteroaryl and aryl, wherein at least one of the hydrogen atoms of said heteroaryl and aryl are substituted with groups selected from SO3-, SO3H, COO-, COOH, and one or more of the other hydrogen atoms of said heteroaryl and aryl are optionally substituted as reported in the description.
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- Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists
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The synthesis and biological evaluation of novel pyrazole and imidazole carboxamides as CB1 antagonists are described. As a part of eastern amide SAR, various chemically diverse motifs were introduced on rimonabant template. The central pyrazole core was
- Sasmal, Pradip K.,Talwar, Rashmi,Swetha,Balasubrahmanyam,Venkatesham,Rawoof, Khaji Abdul,Neelima Devi,Jadhav, Vikram P.,Khan, Sanjoy K.,Mohan, Priya,Srinivasa Reddy,Nyavanandi, Vijay Kumar,Nanduri, Srinivas,Shiva Kumar,Kannan,Srinivas,Nadipalli, Prabhakar,Chaudhury, Hira,Sebastian
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scheme or table
p. 4913 - 4918
(2011/09/16)
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- Tricyclic pyrazoles. 3. Synthesis, biological evaluation, and molecular modeling of analogues of the cannabinoid antagonist 8-chloro-1-(2′, 4′-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7] cyclohepta[1,2-c]pyrazole-3-carboxamide
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A series of analogues of 8-chloro-1-(2′,4′-dichlorophenyl)-AT- piperidin-1-yl-1,4,5,6-tetrahydrobenzo-[6,7]cyclohepta[1,2-c] pyrazole-3-carboxamide 4a (NESS 0327) (Ruiu, S.; Pinna, G. A.; Marchese, G.; Mussinu, J. M.; Saba, P.; Tambaro, S.; Casti, P.; Var
- Murineddu, Gabriele,Ruiu, Stefania,Loriga, Giovanni,Manca, Ilaria,Lazzari, Paolo,Reali, Roberta,Pani, Luca,Toma, Lucio,Pinna, Gérard A.
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p. 7351 - 7362
(2007/10/03)
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- Synthesis and characterization of NESS 0327: A novel putative antagonist of the CB1 cannabinoid receptor
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The compound N-piperidinyl-[8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydrobenzo [6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide] (NESS 0327) was synthesized and evaluated for binding affinity toward cannabinoid CB1 and CB2 receptor.
- Ruiu, Stefania,Pinna, Gerard A.,Marchese, Giorgio,Mussinu, Jean-Mario,Saba, Pierluigi,Tambaro, Simone,Casti, Paola,Vargiu, Romina,Pani, Luca
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p. 363 - 370
(2007/10/03)
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