- The in vivo antinociceptive and μ-opioid receptor activating effects of the combination of N-phenyl-2′,4′-dimethyl-4,5′-bi-1,3-thiazol-2-amines and naloxone
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Morphine is widely used for the treatment of severe pain. This analgesic effect is mediated principally by the activation of μ-opioid receptors (MOR). However, prolonged activation of MOR also results in tolerance, dependence, addiction, constipation, nau
- Lin, Shu-Yu,Kuo, Yu-Hsien,Tien, Ya-Wen,Ke, Yi-Yu,Chang, Wan-Ting,Chang, Hsiao-Fu,Ou, Li-Chin,Law, Ping-Yee,Xi, Jing-Hua,Tao, Pao-Luh,Loh, Horace H.,Chao, Yu-Sheng,Shih, Chuan,Chen, Chiung-Tong,Yeh, Shiu-Hwa,Ueng, Shau-Hua
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p. 312 - 323
(2019/02/20)
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- OPIOID RECEPTOR MODULATORS AND USE THEREOF
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Disclosed is an in vitro screening method for identifying an antagonist-to-agonist allosteric modifier of a mu-opioid receptor and an in vivo method for confirming that a test compound is such a modifier of a mu-opioid receptor. Also disclosed is a method
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Paragraph 0048; 0253; 0254; 0255
(2017/03/21)
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- Structural requirement(s) of N-phenylthioureas and benzaldehyde thiosemicarbazones as inhibitors of melanogenesis in melanoma B 16 cells
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In order to define the structural requirements of phenylthiourea (PTU), a series of thiourea and thiosemicarbazone analogs were prepared and evaluated as inhibitors of melanogenesis in melanoma B16 cells. The most potent analog was 2-(4-tert-butylbenzylidene)hydrazinecarbothioamide (1u) with an IC50 value of 2.7 μM in inhibition of melanogenesis. The structure for potent inhibitory activity of these derivatives are required with the direct connection of π-planar structure to thiourea without steric hinderance in PTU derivatives and the hydrophobic substituent at para position in case of semicarbazones.
- Thanigaimalai,Le Hoang, Tuan Anh,Lee, Ki-Cheul,Bang, Seong-Cheol,Sharma, Vinay K.,Yun, Cheong-Yong,Roh, Eunmiri,Hwang, Bang-Yeon,Kim, Youngsoo,Jung, Sang-Hun
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supporting information; experimental part
p. 2991 - 2993
(2010/08/06)
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- Novel synthetic approach to N-aryl-4-(3-pyridyl)thiazol-2-amine and analogues using HMCM-41 as catalyst, and their biological evaluation as human platelet aggregation inhibitors
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A novel synthetic approach to N-aryl-4-(3-pyridyl)thiazol-2-amine and analogues using HMCM-41, a mesoporous aluminosilicate catalyst and their in vitro ADP-induced platelet aggregation inhibitory activity on human blood platelets is described. Among the test compounds N-(2′-flourophenyl)-4-(3-pyridyl)thiazol-2-amine (9e) was found to be the most potent, IC50 = 4.84 × 10-7 M.
- Bhoga, Umadevi
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p. 1144 - 1150
(2008/03/12)
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- Synthesis and biological activities of new 1,4-benzothiazine derivatives
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New 2H-1,4-benzothiazin-3(4H)-one derivatives possessing (4-phenyl-1-piperazinyl)alkyl moieties at the 2-position were synthesized and tested for calcium antagonistic and calmodulin antagonistic activities. Antihypertensive effects in spontaneously hypertensive rats were also evaluated. In general, these compounds were rather weak calcium channel blockers, although, in contrast, many of them had moderate to potent calmodulin antagonistic activity, and 2-[3-(4-(4-fluorophenyl)-1-piperazinyl]propyl]-2H-1,4-benzothiazin-3(4H )-one derivatives 45, 74 and 75 showed potent antihypertensive effects.
- Kajino,Mizuno,Tawada,Shibouta,Nishikawa,Meguro
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p. 2888 - 2895
(2007/10/02)
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- Improved Procedures for the Preparation of Cycloalkyl-, Arylalkyl-, and Arylthioureas
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An improved procedure for the preparation of arylthioureas consists of the reaction of benzoyl isothiocyanate with anilines in acetone and debenzoylation of the resultant N-aryl-N'-benzoylthioureas with 5percent aqueous sodium hydroxide.Bicycloalkylthioureas and N-(arylalkyl)thioureas (e.g. 9H-9-fluorenylthiourea) are directly prepared from the corresponding isothiocyanates and ammonia.
- Rasmussen, C. R.,Villani, F. J.,Weaner, L. E.,Reynolds, B. E.,Hood, A. R.,et al.
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p. 456 - 459
(2007/10/02)
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- Heterocyclic derivatives of guanidine
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5-Membered, 6-membered and 7-membered heterocyclic derivatives of guanidine having hypoglycemic activity.
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