4665-58-1Relevant academic research and scientific papers
Nitroxide derivative of ROCK kinase inhibitor
-
Paragraph 0475-0481, (2020/06/17)
The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
Design, synthesis and biological activity evaluation of NO donor-containing ferrocene-pyrazole derivative
-
Paragraph 0031; 0039-0040, (2020/02/14)
The invention discloses an NO donor-containing ferrocene-pyrazole derivative and a preparation method thereof. A structure of the NO donor-containing ferrocene-pyrazole derivative is shown by the following formula, wherein R is selected from the following groups.
Design, synthesis and biological evaluation of novel ferrocene-pyrazole derivatives containing nitric oxide donors as COX-2 inhibitors for cancer therapy
Ren, Shen-Zhen,Wang, Zhong-Chang,Zhu, Dan,Zhu, Xiao-Hua,Shen, Fa-Qian,Wu, Song-Yu,Chen, Jin-Jin,Xu, Chen,Zhu, Hai-Liang
, p. 909 - 924 (2018/08/31)
A series of novel ferrocene-pyrazole derivatives containing nitric oxide donors as COX-2 inhibitors for cancer therapy were designed, synthesized and biologically evaluated. Among them, compound 7l displayed the most potent inhibitory against COX-2 (IC50 = 0.82 μM) and antiproliferative activities against Hela cells (IC50 = 0.34 μM) compared with Celecoxib (IC50 = 0.38 and 7.91 μM). The further mechanistic studies revealed that 7l could induce apoptosis of Hela cells by mitochondrial depolarization and the antiproliferative activities of 7l were positively correlated with the levels of intracellular NO release in Hela cells. Most notably, 7l could dramatically suppress tumor growth in Hela cells xenografted mouse model. In summary, compound 7l may be promising candidates for cancer therapy.
Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors
Biava, Mariangela,Battilocchio, Claudio,Poce, Giovanna,Alfonso, Salvatore,Consalvi, Sara,Di Capua, Angela,Calderone, Vincenzo,Martelli, Alma,Testai, Lara,Sautebin, Lidia,Rossi, Antonietta,Ghelardini, Carla,Di Cesare Mannelli, Lorenzo,Giordani, Antonio,Persiani, Stefano,Colovic, Milena,Dovizio, Melania,Patrignani, Paola,Anzini, Maurizio
, p. 772 - 786 (2014/01/23)
We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties.
1,5-Diaryl-2-alkylpyrrole-3-Substituted Nitro Esters, Selective COX-2 Inhibitors and Nitric Oxide Donors
-
Paragraph 0244, (2013/07/05)
1,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of Formula (I) are provided. Such compounds are potent and selective COX-2 inhibitors which are able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. Formula (I) includes compounds wherein the groups R′ and R″ are: —H, —F, —Cl, —Br, —CH3, —CF3, —OCH3, —SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position ?3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group —(CHR3)—, Y is an oxygen atom or the group —NR3— and Z is a carbonyl or a group —(CHR3)—, or a [—CH(COOH)—] group, or a group —(NR3)—, W is an aliphatic chain substituted with one or two (—O—NO2) groups, R2 is: —H, —OH, —OCH3, or —NHR3. R3 is: —H, —CH3, —CH2CH3, [—CH2(CH3)2]. R′″ is methylsulphonyl or sulphonamido. Pharmaceutical formulations and methods of making an using such formulations are also provided.
NITRATE AND DIAZENIUMDIOLATE DERIVATIVES OF PIOGLITAZONE
-
Paragraph 0065; 0066, (2013/03/28)
Nitrate ester and diazeniumdiolate derivatives of pioglitazone are described. They have valuable properties in the treatment of vascular and metabolic diseases, for example type 2 diabetes.
L,5-DIARYL-2-ALKVLPVRROLE-3-SUBSTITUTED NITRO ESTERS, SELECTIVE COX-2 INHIBITORS AND NITRIC OXIDE DONORS
-
Page/Page column 65; 66, (2012/03/27)
The present invention relates to l,5-diaryl-2-alkylpyrrole-3-substituted nitro esters, of formula (I), which are potent and selective COX-2 inhibitors able to release NO in concentrations that make it possible to counteract the side effects due to selective COX-2 inhibition, without giving rise to hypotensive effects. (I). Where the groups R' and R" are: -H, -F, -CI, -Br, -CH3, -CF3, -OCH3, -SCH3, R1 is methyl, ethyl, trifluoromethyl, hydroxymethyl, methoxymethyl and the substituent in position -3 of the pyrrole ring is a chain, where the groups X, Y, Z, W and R2 are: X is a carbonyl or a group -(CHR3)-, Y is an oxygen atom or the group -NR3- and Z is a carbonyl or a group - (CHR3)-, or a [-CH(COOH)-] group, or a group -(NR3)-, W is an aliphatic chain substituted with one or two (-O-NO2) groups, R2 is: -H, -OH, -OCH3, or -NHR3. R3 is: -H, -CH3, -CH2CH3, [-CH2(CH3)2]. R'" is methylsulphonyl or sulphonamido. The purpose of the invention includes: preparation of the compounds of formula (I), the respective pharmaceutical formulations and use thereof for treating acute and chronic pain, for treating inflammatory disorders and for drug treatment of some forms of tumours.
VALSARTAN DERIVATIVES CARRYING NITROGEN OXIDE DONORS FOR THE TREATMENT OF VASCULAR AND METABOLIC DISEASES
-
Page/Page column 15-16, (2011/11/06)
Nitrate esters and diazeniumdiolate derivatives of valsartanamide are described. They have valuable properties in the treatment of vascular and metabolic diseases.
A valsartanamide dinitrate derivative for the treatment of vascular and metabolic diseases
-
Page/Page column 9, (2011/11/01)
A dinitrate ester of a valsartanamide is described. It has superior properties in the treatment of vascular and metabolic diseases.
NITRATE AND DIAZENIUMDIOLATE DERIVATIVES OF PIOGLITAZONE
-
Page/Page column 14-15, (2011/12/14)
Nitrate ester and diazeniumdiolate derivatives of pioglitazone are described. They have valuable properties in the treatment of vascular and metabolic diseases, for example type 2 diabetes.
