72752-80-8Relevant academic research and scientific papers
SUBSTITUTED HYDROXYSTILBENE COMPOUNDS AND DERIVATIVES SYNTHESIS AND USES THEREOF
-
Page/Page column 197, (2021/07/02)
The present disclosure relates to substituted hydroxystilbene compounds and derivatives, specifically 2-substituted hydroxystilbene compounds and derivatives, the synthesis of such compounds and their use in therapy.
General and efficient synthesis of benzoxazol-2(3H)-ones: Evolution of their anti-cancer and anti-mycobacterial activities
Indrasena Reddy,Aruna,Sudhakar Babu,Vijayakumar,Manisha,Padma Sridevi,Yogeeswari,Sriram
, p. 59594 - 59602 (2015/02/19)
A novel class of benzo[d]oxazol-2(3H)-one derivatives has been synthesized and their in vitro cytotoxicity against human pancreatic adenocarcinoma and human non-small cell lung carcinoma cancer cell lines was evaluated. Many of these compounds were found to display excellent to moderate activity. Among them, 6b, 6l, 6n and 6x were identified as lead molecules. In particular, 6l and 6n were found to be potent against the pancreatic adenocarcinoma cell line whereas the 6x was found to be effective against the human non-small cell lung carcinoma cell line. Conversely, the compounds 6l-x were found to be ineffective against Mycobacterium tuberculosis. Of the various molecules, 6h showed promising anti-mycobacterial activity, with an IC50 value equal to that of ciprofloxacin.
NEW CYCLOHEXYLAMINE DERIVATIVES HAVING β2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
-
, (2013/05/23)
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
NEW CYCLOHEXYLAMINE DERIVATIVES HAVING BETA 2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
-
, (2013/05/23)
The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies.
2-OXO-3-BENZYLBENZOXAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS MET KINASE INHIBITORS FOR THE TREATMENT OF TUMOURS
-
Page/Page column 25, (2010/12/29)
Compounds of the formula (I), in which R1, R2, R3, R3′, R4, R4′, E, E′, E″ and E′″ have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES
-
Page/Page column 89, (2008/06/13)
The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.
BENZAMIDE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE
-
Page/Page column 106-107, (2008/06/13)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds which are derivatives of benzamide and suitable in methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions .
Piperidine derivatives as subtype selective N-methyl-D-aspartate antagonists
-
, (2008/06/13)
Described are piperidines of Formula I and pharmaceutically acceptable salts thereof. The compounds of Formula I are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, central nervous system disorders, depression, trauma, hypoglycemia, neurodegenerative disorders, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, pain, especially chronic pain, neuropathic pain, or surgical pain, or urinary incontinence.
Analogues of the Cyclic Hydroxamic Acid 2,4-Dihydroxy-7-methoxy-2H-1,4-benzoxazin-3-one: Decomposition to Benzoxazolinones and Reaction with β-Mercaptoethanol
Atkinson, Jeffrey,Morand, Peter,Arnason, John T.,Niemeyer, Hermann M.,Bravo, Hector R.
, p. 1788 - 1800 (2007/10/02)
Analogues of the aglucones of naturally occurring cyclic hydroxamic acids (2,4-dihydroxy-1,4-benzoxazin-3-ones) from Gramineae (Poaceae) have been synthesized by the reductive cyclization of the ring-substituted methyl α-(o-nitrophenoxy)-α-methoxyacetates, followed by demethylation of the C-2 methoxy group with BBr3 or BCl3 to reveal the 2-hydroxy group.A structure-activity series was produced by varying the substituent at C-7 on the aromatic ring .The pKa values for the hydroxamic acid and the phenol moieties were determined for each member of the C-7 series.They correlated well with ? in a linear free energy relationship (LFER) yielding values of ρ = 0.71 (with ?p) for pKa1 (the hydroxamic acid) and ρ = 1.6 (with ρm) for pKa2 (the phenol).A LFER also existed between the rate constants for the unimolecular decomposition of these hydroxamic acids to benzoxazolinones and ?+ (ρ = -1.1).The rates of hydroxamic acid reduction to lactams by β-mercaptoethanol were also investigated.It was found that only compounds with electron-rich aromatic rings and specifically an oxa functionality para to the hydroxamic acid nitrogen atom (compounds 1 and 3 - 5) had measurable rates of reduction. 1H NMR spectra recorded during this reaction in D2O buffers (pD 9), however, showed that compounds 1, 2, 6 - 9 (the only ones investigated) formed a hemithioacetal at C-2 even though only 1 has a measurable rate of reduction by the same thiol.The remarkable rate enhancement provided by an oxa functionality suggests that reduction occurs by direct attack of thiolate on the hydroxamic nitrogen of a resonance-stabilized ion pair.
