18903-18-9Relevant articles and documents
REACTION OF ACYLAMINOCYANOESTERS WITH 2,4-BIS(4-METHOXYPHENYL)-1,3,2,4-DITHIADIPHOSPHETANE 2,4-DISULFIDE LEADING TO SUBSTITUTED AMINOTHIAZOLES. CRYSTAL STRUCTURE OF 5-AMINOTHIAZOLE-4-CARBOXYLIC ACID ETHYL ESTER.
Golankiewicz, Bozenna,Januszczyk, Piotr,Gdaniec, Maria,Kosturkiewicz, Zofia
, p. 5989 - 5994 (1985)
2-Acylamino-2-cyanoacetic acid ethyl esters 2a-c react with 2.4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulfide 1 in refluxing benzene with formation of 2-alkyl(aryl)-5-aminothiazole-4-carboxylic acid ethyl esters 3a-c.Structure 3 was estab
Design, synthesis, in vitro evaluation of a new pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives as cholinesterase inhibitors against Alzheimer's disease
Aisa, Haji Akber,Bozorov, Khurshed,Li, Yi,Liu, Liu,Nie, Lifei,Niu, Chao,Shen, Jingshan,Zeng, Yan,Zhao, Jiangyu
, (2022/02/16)
A novel of 40 pyrrolo[1,2-a]thiazolo[5,4-d]pyrimidinone derivatives were designed and synthesized as cholinesterase inhibitor agents. The in vitro enzyme assays proved that most of the compounds effectively inhibited cholinesterases in the micromolar rang
Synthesis and biological evaluation of thiabendazole derivatives as anti-angiogenesis and vascular disrupting agents
Zhang, Chao,Zhong, Bo,Yang, Simin,Pan, Liangkun,Yu, Siwang,Li, Zhongjun,Li, Shuchun,Su, Bin,Meng, Xiangbao
, p. 3774 - 3780 (2015/08/03)
Abstract Thiabendazole, already approved by FDA for oral use as an anti-fungal and anti-helminthic drug since 1967, has recently been repurposed as a vascular disrupting agent. By optimization of the structure of the lead compound, we successfully identified compound TBZ-19 and the new derivative is over 100-fold more potent than the lead compound against the growth of four different cell lines (A549, HCT-116, HepG2 and HUVECs). The most potent two candidates TBZ-07 and TBZ-19, exhibiting moderate inhibitory cell proliferation activity, were also verified as anti-angiogenesis and vascular disrupting agents. Therefore, TBZ-07 and TBZ-19 would be promising candidates with vasculature targeting activity and merit further development.
NOVEL AMINOTHIAZOLE CARBOXAMIDES AS KINASE INHIBITORS
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, (2014/03/25)
The present invention provides a compound of formula (I), as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kina
SUBSTITUTED ARYL PYRIMIDINONE DERIVATIVES
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, (2009/10/22)
Substituted aryl pyrimidinone derivatives are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
2-AMINO PYRIDINE COMPOUNDS
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Page/Page column 66-68, (2008/12/05)
The present invention is directed to 2-aminopyrimidine compounds and pharmaceutically acceptable salts thereof, their synthesis and their use as HSP-90 inhibitors.
2-PHENOXY PYRIMIDINONE ANALOGUES
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Page/Page column 23; 45-46, (2008/06/13)
2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment
PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
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Page/Page column 20, (2008/06/13)
The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.
HALOALKYL-SUBSTITUTED PYRIMIDINONE DERIVATIVES
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Page/Page column 48, (2008/06/13)
Haloalkyl-substituted pyrimidinone derivatives are provided, of the Formula (I): wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful
CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES
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Page/Page column 46-47, (2008/12/06)
Cis-cyclohexyl substituted pyrimidinone derivatives are provided, of Formula (I) wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful