160658-69-5Relevant academic research and scientific papers
2-ARYL- AND 2-HETEROARYLTHIAZOLYL COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE THEREOF
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Page/Page column 50; 51, (2009/10/22)
The present invention discloses fused bicyclic 2-aryl- or 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumo
1,2-Diarylimidazoles as potent, cyclooxygenase-2 selective, and orally active antiinflammatory agents
Khanna, Ish K.,Weier, Richard M.,Yu, Yi,Xu, Xiang D.,Koszyk, Francis J.,Collins, Paul W.,Koboldt, Carol M.,Veenhuizen, Amy W.,Perkins, William E.,Casier, Jacquelen J.,Masferrer, Jaime L.,Zhang, Yan Y.,Gregory, Susan A.,Seibert, Karen,Isakson, Peter C.
, p. 1634 - 1647 (2007/10/03)
Series of 1,2-diarylimidazoles has been synthesized and found to contain highly potent and selective inhibitors of the human COX-2 enzyme. The paper describes a short synthesis of the target 1,2-diarylimidazoles starting with aryl nitriles. Different portions of the diarylimidazole (I) were modified to establish SAR. Systematic variations of the substituents in the aryl ring B have yielded very potent (IC50 = 10-100 nm) and selective (1000-12500) inhibitors of the COX-2 enzyme. The study on the influence of substituents in the imidazole ring established that a CF3 group at position 4 gives the optimum oral activity. A number of the diarylimidazoles showed excellent inhibition in the adjuvant induced arthritis model (e.g., ED50 = 0.02 mpk for 22 and 34). The diarylimidazoles are also potent inhibitors of carrageenan-induced edema (ED50 = 9-30 mpk) and hyperalgesia (ED50 = 11- 40 mpk). Several orally active diarylimidazoles show no GI toxicity in the rat and mouse up to 200 mpk.
N-(3-Fluorobenzyl)heterocyclic derivatives and their use as pesticides
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, (2008/06/13)
Compound of general formula: in which n is 1, 2 or 3; R1, R2, R3 and R4 independently represent a hydrogen atom or an alkyl group; X represents and oxygen atom or a group >CR5R6, >NR7, >NCOR8 or >S(O)p, where R5, R6, R7 and R8 independently represent a hydrogen atom or an alkyl group and p is 0, 1 or 2; A represents an optionally substituted 3-fluorobenzyl group; and Y represents a group =CH or =N- are disclosed. The compounds are pesticidal.
