20982-28-9Relevant academic research and scientific papers
On the metabolites produced by Colletotrichum gloeosporioides a fungus proposed for the Ambrosia artemisiifolia biocontrol; spectroscopic data and absolute configuration assignment of colletochlorin A
Masi, Marco,Zonno, Maria Chiara,Cimmino, Alessio,Reveglia, Pierluigi,Berestetskiy, Alexander,Boari, Angela,Vurro, Maurizio,Evidente, Antonio
, p. 1537 - 1547 (2018)
Ambrosia artemisiifolia L. is responsible for serious allergies induced on humans. Different approaches for its control were proposed during the COST Action FA1203 “Sustainable management of Ambrosia artemisiifolia in Europe” (SMARTER). Fungal secondary metabolites often show potential herbicidal activity. Three phytotoxins were purified from the fungal culture filtrates of Colletotrichum gloeosporioides, isolated from infected leaves of A. artemisiifolia. They were identified by spectroscopic and chemical methods as colletochlorin A, orcinol and tyrosol (1, 2 and 3). The absolute configuration 6’R to colletochlorin A was assigned for the first time applying the advanced Mosher’s method. When assayed by leaf-puncture on A. artemisiifolia only 1 caused the appearance of large necrosis. The same symptoms were also induced by 1 on ambrosia plantlets associated with plant wilting. On Lemna minor, colletochlorin A caused a clear fronds browning, with a total reduction in chlorophyll content.
Verification of the necessity of the tolyl group of PF-543 for sphingosine kinase 1 inhibitory activity
Baek, Dong Jae,Ki, Sung Hwan,Kim, Sang-Bum,Kim, Sanghee,Kim, Su Bin,Kwon, Yongseok,Lee, Joo-Youn,Lee, Taeho,Moon, Hong Seop,Oh, Yoon Sin,Park, Eun-Young,Park, Jeong-Eun
, (2020/06/17)
PF-543, the most potent sphingosine kinase (SK) inhibitor, does not demonstrate effective anticancer activity in some cancer cells, unlike other known SK1 inhibitors. PF-543 has a non-lipid structure with a unique toluene backbone; however, the importance
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
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Paragraph 0522-0524, (2013/10/22)
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Novel Compounds
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Page/Page column 72, (2012/04/18)
The present invention relates to the new compounds of general formula I wherein A, U, V, X, Y, R1, R2 and R3 are defined as stated hereinafter, the tautomers, the isomers thereof, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
HYDANTOIN DERIVATIVES USEFUL AS KV3 INHIBITORS
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Page/Page column 67, (2012/06/30)
The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
Piperazine derivatives
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Page/Page column 47, (2010/02/10)
This invention relates to a compound of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, wherein R1 to R5 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation, compositions containing them and the uses of such derivatives. The compounds of the present invention inhibit the interaction of gp120 with CD4 and are therefore of use in the treatment of HIV, a retroviral infection genetically related to HIV, or AIDS.
FUSED HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF
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Page/Page column 64, (2008/06/13)
The present invention provides fused heterocyclic derivatives represented by the general formula: wherein R1 represents H, halogen, OH, etc.; R2 represents H, halogen or an alkyl group; R3 and R4 represent H, OH, halogen, etc.; Q represents alkylene, etc.; ring A represents aryl or heteroaryl; and G represents or ???or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an excellent inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.
Rapid and efficient acetylation of alcohols and phenols with acetic anhydride using tin(IV) porphyrin as catalyst
Tangestaninejad, Shahram,Habibi, Mohammad Hossein,Mirkhani, Valiollah,Moghadam, Majid
, p. 1337 - 1343 (2007/10/03)
The efficient and rapid esterification of alcohols and phenols in acetic anhydride was achieved by tin(IV) tetraphenylporphyrin perchlorate [SnIV (tpp) (ClO4)2] as catalyst in high yields. SnIV (tpp) (ClO4)2 showed highly catalytic activity on the acetylation reaction.
Propiophenone derivatives and process for preparing the same
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, (2008/06/13)
A propiophenone derivative of the formula (I): wherein OX is a hydroxy group which may optionally be protected, Y is a lower alkyl group, and Z is a beta -D-glucopyranosyl group wherein one or more hydroxy groups may optionally be protected, or a pharmace
Na+-glucose cotransporter (SGLT) inhibitors as antidiabetic agents. 4. Synthesis and pharmacological properties of 4'- dehydroxyphlorizin derivatives substituted on the B ring
Tsujihara, Kenji,Hongu, Mitsuya,Saito, Kunio,Kawanishi, Hiroyuki,Kuriyama, Kayoko,Matsumoto, Mamoru,Akira, Oku,Ueta, Kiichiro,Tsuda, Minoru,Saito, Akira
, p. 5311 - 5324 (2007/10/03)
In our studies of Na+-glucose cotransporter (SGLT) inhibitors as antidiabetic agents, a series of novel 4'- dehydroxyphlorizin derivatives substituted on the B ring was prepared and their effects on urinary glucose excretion were evaluated in rats. Introduction of only a small alkyl group at the 4'-position increased the activity, and 3-(benzo[b]furan-5- yl)-2',6'-dihydroxy-4'-methylpropiophenone 2'-O-β-D- glucopyranoside (4) showed the most potent effect. To overcome hydrolysis of compound 4 by β-glucosidase in the digestive tract, the OH groups on the glucose moiety of compound 4 were modified. Three prodrugs (5, 42, and 55) were more potent than the parent compound 4 by oral administration, and finally 3- (benzo[b]furan-5-yl)-2',6'-dihydroxy-4'-methylpropiophenone 2'-O- (6-O-methoxycarbonyl-β-D-glucopyranoside) (5) was selected as a new promising candidate. Compound 5 was metabolized mainly by liver esterase to the active form (4), which was about 10 times more potent than 5 in inhibiting SGLT. In oral glucose tolerance test in db/db mice, compound 5 dose-dependently suppressed the elevation of glucose levels. Single administration of 5 reduced hyperglycemia concurrently with increase of glucose excretion into urine in diabetic KK-A(y) mice. Furthermore, compound 5 suppressed the elevation of blood glucose levels but did not lower it below the normal level even in fasted conditions in KK- A(y) mice. Additionally, long-term treatment with 5 dose- dependently reduced hyperglycemia and HbA1c in KK-A(y) mice. These pharmacological data strongly suggest that compound 5 has a therapeutic potential in the treatment of NIDDM.
