- 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.
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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
- Golankiewicz, Bozenna,Januszczyk, Piotr,Gdaniec, Maria,Kosturkiewicz, Zofia
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- 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
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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
- Aisa, Haji Akber,Bozorov, Khurshed,Li, Yi,Liu, Liu,Nie, Lifei,Niu, Chao,Shen, Jingshan,Zeng, Yan,Zhao, Jiangyu
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- Synthesis and biological evaluation of thiabendazole derivatives as anti-angiogenesis and vascular disrupting agents
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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.
- Zhang, Chao,Zhong, Bo,Yang, Simin,Pan, Liangkun,Yu, Siwang,Li, Zhongjun,Li, Shuchun,Su, Bin,Meng, Xiangbao
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p. 3774 - 3780
(2015/08/03)
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- NOVEL AMINOTHIAZOLE CARBOXAMIDES AS KINASE INHIBITORS
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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
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Page/Page column 50
(2014/03/25)
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- SUBSTITUTED ARYL PYRIMIDINONE DERIVATIVES
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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.
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Page/Page column 45
(2009/10/22)
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- 2-AMINO PYRIDINE COMPOUNDS
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The present invention is directed to 2-aminopyrimidine compounds and pharmaceutically acceptable salts thereof, their synthesis and their use as HSP-90 inhibitors.
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Page/Page column 66-68
(2008/12/05)
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- 2-PHENOXY PYRIMIDINONE ANALOGUES
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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
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Page/Page column 23; 45-46
(2008/06/13)
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- PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
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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.
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Page/Page column 20
(2008/06/13)
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- HALOALKYL-SUBSTITUTED PYRIMIDINONE DERIVATIVES
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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
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Page/Page column 48
(2008/06/13)
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- CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES
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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
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Page/Page column 46-47
(2008/12/06)
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- BICYCLIC PYRIMIDIN-4-(3H)-ONES AND ANALOGUES AND DERIVATIVES THEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
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Compounds of formula (I); which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
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Page/Page column 42
(2010/02/12)
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- A one-pot synthesis of alkyl 5-amino-2-mercaptothiazole-4-carboxylates and sulphur-Claisen type rearrangement reactions of the corresponding S-allyl/propargyl compounds
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Alkyl 5-amino-2-mercaptothiazole-4-carboxylates (5) have been prepared in a one-pot synthesis by the action of hydrogen sulfide on a mixture of alkyl 2-oximino-2-cyanoacetate and trialkyl orthoformate in pyridine; reduction of the oximino group to imino f
- Ray, Sibdas,Ghosh, Sukla
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p. 1037 - 1043
(2007/10/03)
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- Novel analogues of tiazofurin by Lawesson reagent effected cyclization
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2-Benzylthiazole-4-carboxamide 4 and 5-(β-D-ribofuranosylamino) thiazole-4-carboxamide 10 were synthesized from phenylacetylamino- and formylamino cyanoacetic acid esters 1a and 1b, respectively. The ribosylation reaction leading to 10 gave rise also to i
- Golankiewicz,Januszczyk
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p. 313 - 316
(2007/10/02)
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- Synthesis of Compounds Related to 4(5)-Aminoimidazole-5(4)-carboxamides: Part IV - Synthesis of 2-Substituted 5-Aminothiazoles and Reaction of Related Thiazolium and Imidazolium Salts with Bases
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N-Cyanomethylimidates (Ia-e) have been reacted with H2S in pyridine.While ethyl N-(ethoxycarbonylcyanomethyl)acetimidate (Ia), ethyl N-(carbamoylcyanomethyl)acetimidate (Ib) and ethyl N-(carbamoylcyanomethyl)benzimidate (Ic) furnish varying amounts of a mixture of ethyl 5-amino-2-methylthiazole-4-carboxylate (IIIa) and ethyl 2-methyl-4(5)-mercaptoimidazole-5(4)-carboxylate (IVa) (in 2:1 ratio), 5-amino-2-methylthiazole-4-carboxamide (IIIb) and 2-methyl-4(5)-mercaptoimidazole-5(4)-carboxamide (IVb) (in 1:1 ratio) and 5-amino-2-phenylthiazole-4-carboxamide (IIIc) and4(5)-mercapto-2-phenylimidazole-5(4)-carboxamide (IVc) (in 1:5 ratio) respectively, the corresponding formimidates (Id,e) furnish the corresponding thiazole derivatives, ethyl 5-aminothiazole-4-carboxylate (IIId) and 5-aminothiazole-4-carboxamide (IIIe) as the sole products.Reaction of ethyl oximinocyanoacetate (VI) with H2S in pyridine in the presence of ethyl orthoformate, however, produces only the imidazole derivative, ethyl 4(5)-mercaptoimidazole-5(4)-carboxylate (IVd).The changing pattern of the products is interpreted in terms of the formation of thiol and thioamide intermediates.Treatment of 5-amino-1-benzyl-4-carboxamido-2,3-dimethylimidazolium toluene-p-sulphonate and 5-amino-4-carboxamido-1,2,3-trimethylimidazolium toluene-p-sulphonate with aq.NaOH or NaOEt in EtOH effects dequaternization to regenerate 5-amino-1-benzyl-2-methylimidazole-4-carboxamide and 1,2-dimethyl analogue respectively, while the 5-amino-4-ethoxycarbonyl-2,3-dimethylthiazolium toluene-p-sulphonate decomposes on warming with NaOEt in EtOH.
- Sen, A. K.,Mukhopadhyay, Ajoy Kumar
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p. 275 - 278
(2007/10/02)
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