53137-27-2Relevant articles and documents
Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties
Ghonim, Aya E.,Ligresti, Alessia,Rabbito, Alessandro,Mahmoud, Ali Mokhtar,Di Marzo, Vincenzo,Osman, Noha A.,Abadi, Ashraf H.
, p. 154 - 170 (2019/07/12)
The strong therapeutic potential of CB2 receptor agonists for use as anti-inflammatory agents that lack psychiatric side effects has attracted substantial interest. We herein describe the rational design and synthesis of novel thiazole and benzothiazole derivatives and the evaluation of their binding affinity and functional activity on CB1 and CB2 receptors. The series with the general formula N-(3-pentylbenzo [d]thiazol-2(3H)-ylidene) carboxamide (compounds 6a-6d) exhibited the highest affinity and selectivity towards CB2 receptors with Kis in the picomolar or low nanomolar range, and selectivity indices (Ki hCB1/Ki hCB2) reaching up to 429 fold. Notably, these compounds also demonstrated an agonistic functional activity in cellular assays with EC50s in the low nanomolar range. More interestingly, compound 6d, the 3-(trifluoromethyl)benzamide derivative, exhibited remarkable protection against DSS-induced acute colitis in mice model.
HETEROCYCLIC COMPOUND AND p27Kip1 DEGRADATION INHIBITOR
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Paragraph 0333; 0334; 0335; 0336; 0338; 0339; 0340; 0341, (2013/04/10)
A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.
α2 Adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles
Boyd, Robert E.,Press, Jeffery B.,Rasmussen, C. Royce,Raffa, Robert B.,Codd, Ellen E.,Connelly, Charlene D.,Bennett, Debra J.,Kirifides, Alex L.,Gardocki, Joseph F.,Reynolds, Brian,Hortenstein, John T.,Reitz, Allen B.
, p. 5064 - 5071 (2007/10/03)
A series of (imidazolylmethyl)oxazoles and -thiazoles were prepared and evaluated as α2 adrenoceptor agonists. These compounds were also tested in in vivo paradigms that are predictive of analgesic activity. Variations in both the imidazole and thiazole portions of the molecule were investigated. Some of the more potent compounds such as 22, 26, 45, and 53 displayed α2 receptor binding in the 10-20 nM range and also had significant antinociceptive activity in the mouse abdominal irritant test (MAIT).
Pyrazolecarboxylic acid derivatives and plant disease control agent
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, (2008/06/13)
The present invention provides a plant disease control agent containing as active ingredient one or more compounds of the formula [1]A--COOR 1 [1]whereinR 1 represents a hydrogen atom or a C 1 -C 4 alkyl group, andA represents a group of the formula (A-1) or (A-2) STR1 R 2 represents a C 1 -C 4 alkyl group, R 3 represents a C 1 -C 4 alkyl group,R 4 represents a halogen atom or a C 1 -C 4 alkyl group, andR 5 represents a C 1 -C 4 alkyl group.Further, the compound of A-1 in the formula [1] in which R 3 is a halogen atom is also included in the present invention.
