2469-99-0Relevant articles and documents
Kinetic Evidence for the Intermediacy of 1-Azirines in the Gas-Phase Thermal Isomerization of 3H-Isoxazoles to α-Carbonylacetonitrile Derivatives
Perez, Jorge D.,Yranzo, Gloria I.,Wunderlin, Daniel A.
, p. 982 - 984 (1982)
Thermal isomerization of 5-methylisoxazole and 5-amino-4-methylisoxazole to acetylacetonitrile and 2-cyanopropionamide, respectively, was studied in a flow system.The activation parameters are reported.According to the experimental results, a concerted 1,3 sigmatropic shift to 1-azirines is proposed as the rate-limiting step in these reactions.A general reaction mechanism for the isomerization of isoxazoles into 1-azirines, oxazoles, and α-carbonylacetonitrile derivatives is discussed.
Design, synthesis, and in vitro anticancer screening of novel pyrazolinyl-pyrazole/1, 2, 3-triazole hybrids
Ismail, Magda M. F.,Abdulwahab, Hanan G.,Elnagdi, Mohamed H.
, p. 3584 - 3596 (2020)
Novel hybrids, pyrazolinylpyrazoles, and pyrazolinyltriazoles were designed, synthesized, and screened for their anticancer activity. Eleven compounds were selected by the National Cancer Institute (NCI)/USA for anticancer screening at single high dose (10?5 M) in full NCI 60 cell panels. Two compounds: 4-aminopyrazole-5-carbonitrile, 5c (NSC-747630/1) and ethyl 4-aminopyrazole-5- carboxylate, 7d (NSC-747634/1) were the most active candidates of the series and were selected for further evaluation at five dose screening as they displayed significant growth inhibition with full panel median growth inhibition (GI50) 5.47 and 2.24 μM, respectively. Both 5c and 7d hybrids exhibited broad spectrum antitumor activity; however 7d showed moderate selectivity (selectivity ratio 3.6) toward leukemia.
AMIDITE COMPOUND AND METHOD FOR PRODUCING POLYNUCLEOTIDE USING SAID COMPOUND
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Paragraph 0173-0174, (2021/08/06)
The present invention provides an amidite compound represented by formula (1) which enables a synthesis of RNA with high purity, and the method for preparing a polynucleotide by using the same compound. (In the formula (1), wherein R represents the following formula (wherein Ra and Rb are identical to or different from each other and each represents a methyl group, an ethyl group, or a hydrogen atom, with the proviso that Ra and Rb does not represent a hydrogen atom, n is an integer of 1 to 5), and Ba represents a group containing optionally protected nucleobase structure, and G1 and G2 are identical to or different from each other and each represents a protecting group for a hydroxy group, and G3 are identical to or different from each other and each represents an alkyl group.
Identification of diphenylalkylisoxazol-5-amine scaffold as novel activator of cardiac myosin
Boggu, Pulla Reddy,Venkateswararao, Eeda,Manickam, Manoj,Sharma, Niti,Kang, Jong Seong,Jung, Sang-Hun
, (2020/09/16)
To identify novel potent cardiac myosin activator, a series of diphenylalkylisoxazol-5-amine compounds 4–7 have been synthesized and evaluated for cardiac myosin ATPase activation. Among the 37 compounds, 4a (CMA at 10 μM = 81.6%), 4w (CMA at 10 μM = 71.2%) and 6b (CMA at 10 μM = 67.4%) showed potent cardiac myosin activation at a single concentration of 10 μM. These results suggested that the introduction of the amino-isoxazole ring as a bioisostere for urea group is acceptable for the cardiac myosin activation. Additional structure–activity relationship (SAR) studies were conducted. Para substitution (-Cl, –OCH3, -SO2N(CH3)2) to the phenyl rings or replacement of a phenyl ring with a heterocycle (pyridine, piperidine and tetrahydropyran) appeared to attenuate cardiac myosin activation at 10 μM. Additional hydrogen bonding acceptor next to the amino group of the isoxazoles did not enhance the activity. The potent isoxazole compounds showed selectivity for cardiac myosin activation over skeletal and smooth muscle myosin, and therefore these potent and selective isoxazole compounds could be considered as a new series of cardiac myosin ATPase activators for the treatment of systolic heart failure.