113641-88-6Relevant academic research and scientific papers
A bodipy based hydroxylamine sensor
Sedgwick, Adam C.,Chapman, Robert S. L.,Gardiner, Jordan E.,Peacock, Lucy R.,Kim, Gyoungmi,Yoon, Juyoung,Bull, Steven D.,James, Tony D.
supporting information, p. 10441 - 10443 (2017/09/25)
With this research, we have developed a bodipy based system as the first "turn-on" fluorescence system for the detection hydroxylamine.
Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines
Kubota, Katsumi,Kurebayashi, Hirotaka,Miyachi, Hirotaka,Tobe, Masanori,Onishi, Masako,Isobe, Yoshiaki
experimental part, p. 3005 - 3021 (2011/06/19)
A series of tricyclic carboxylic acids having 6-amino-pyrimidine-2,4(1H,3H) -dione with piperazino or homopiperazino moiety linked by propylene, were synthesized and evaluated for their affinity toward human histamine H 1 receptor and Caco-2 cell permeability. Selected compounds were further evaluated for their oral anti-histaminic activity in mice, bioavailability in rats, and their anti-inflammatory activity in mice OVA-induced biphasic cutaneous reaction model. Among the compounds tested, dibenzoxazepine carboxylic acid 13b showed both histamine H1 receptor antagonistic activity and anti-inflammatory activity in vivo. In addition, 13b exhibited low affinity toward α1 receptor and low occupancy of H1 receptor in the brain. It is therefore, believed that 13b is a potential candidate for development as 3rd generation anti-histamine.
Design, synthesis and biological evaluation of novel substituted benzoylguanidine derivatives as potent Na+/H+ exchanger inhibitors
Xu, Wen-Ting,Jin, Ning,Xu, Jing,Xu, Yun-Gen,Wang, Qiu-Juan,You, Qi-Dong
scheme or table, p. 3283 - 3287 (2010/03/31)
A novel series of substituted benzoylguanidine derivatives were designed and synthesized as potent NHE1 inhibitors. Most compounds can significantly inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, among which compound 5f (ICs
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury
Zhang, Rui,Lei, Lin,Xu, Yun-Gen,Hua, Wei-Yi,Gong, Guo-Qing
, p. 2430 - 2433 (2008/04/18)
A novel series of benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines were designed and synthesized as Na+/H+exchanger inhibitors. Most of them were found to inhibit NHE1-mediated platelet swelling in a concentration-dependent manner, and to have significant cardioprotective effect against myocardial ischemic-reperfusion injury, among which compounds 10a and 34 were more potent than cariporide in both in vivo and in vitro tests.
Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors
Asaki, Tetsuo,Sugiyama, Yukiteru,Hamamoto, Taisuke,Higashioka, Masaya,Umehara, Masato,Naito, Haruna,Niwa, Tomoko
, p. 1421 - 1425 (2007/10/03)
A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bc
AMIDE DERIVATIVE
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Page/Page column 13, (2008/06/13)
The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.
AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues
Kasibhatla, Srinivas Rao,Bookser, Brett C.,Probst, Gary,Appleman, James R.,Erion, Mark D.
, p. 1508 - 1518 (2007/10/03)
N3-Substituted coformycin aglycon analogues with improved AMP deaminase (AMPDA) inhibitory potency are described. Replacement of the 5-carboxypentyl substituent in the lead AMPDA inhibitor 3-(5-carboxypentyl)-3,6,7,8- tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (2) described in the previous article with various carboxyarylalkyl groups resulted in compounds with 10- 100-fold improved AMPDA inhibitory potencies. The optimal N3 substituent had m-carboxyphenyl with a two-carbon alkyl tether. For example, 3-[2-(3-carboxy- 5-ethylphenyl)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (43g) inhibited human AMPDA with a K(i) = 0.06 μM. The compounds within the series also exhibited > 1000-fold specificity for AMPDA relative to adenosine deaminase.
Synthesis and properties of an optically active helical bis-cobaltocenium ion
Gilbert, Adam M.,Katz, Thomas J.,Geiger, William E.,Robben, Matthew P.,Rheingold, Arnold L.
, p. 3199 - 3211 (2007/10/02)
The optically active helical bis-cobaltocenium salt 6 is synthesized, as are two related monocobaltocenium salts, 29 and 30. The structure of 6 is analyzed by X-ray diffraction, which shows that the metals are separated by 8.49 ?. Reducing 6 either electrochemically or with K(Hg) produces species that absorb near 920 nm, but the absorption is not an intervalence transition. It originates instead from isolated Co(II) centers. This is demonstrated by the reduction product of 29, which has only one cobalt, also absorbing at a similar wavelength (λmax, = 957 nm). The optical and ESR spectra imply that the unpaired electron in monoreduced 6 is largely localized on cobalt and that direduced 6 is essentially a Co(II)Co(II) diradical. The difference between two Co(III)/Co(II) reduction potentials of 6, 130 mV, is shown to be appropriate for a conjugated dimetallocene with metals so distant. Crystal data for 6: M = 1275.02; orthorhombic, space group P212121; Z = 4; a = 11.560(4), b = 12.244(3), and c = 41.349(17) ?; V = 5852.5 ?3; R = 0.1137 for 4653 reflections having Fo ≥ nσ(Fo) (n = 7.5).
