Tag: M.W=150-200

Fancelli, Daniele published the artcileCinnamic Anilides as New Mitochondrial Permeability Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury Protective Effect in Vivo, Safety of (E)-3-(3-Nitrophenyl)acrylic acid, the publication is Journal of Medicinal Chemistry (2014), 57(12), 5333-5347, database is CAplus and MEDLINE.

In this account, we report the development of a series of substituted cinnamic anilides that represents a novel class of mitochondrial permeability transition pore (mPTP) inhibitors. Initial class expansion led to the establishment of the basic structural requirements for activity and to the identification of derivatives with inhibitory potency higher than that of the standard inhibitor cyclosporine-A (CsA). These compounds can inhibit mPTP opening in response to several stimuli including calcium overload, oxidative stress, and thiol cross-linkers. The activity of the cinnamic anilide mPTP inhibitors turned out to be additive with that of CsA, suggesting for these inhibitors a mol. target different from cyclophylin-D. In vitro and in vivo data are presented for (E)-3-(4-fluoro-3-hydroxy-phenyl)-N-naphthalen-1-yl-acrylamide 22, one of the most interesting compounds in this series, able to attenuate opening of the mPTP and limit reperfusion injury in a rabbit model of acute myocardial infarction.

Journal of Medicinal Chemistry published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C9H7NO4, Safety of (E)-3-(3-Nitrophenyl)acrylic acid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Abdelbaset, Mahmoud S. published the artcileDesign, synthesis, and biological evaluation of new series of pyrrol-2(3H)-one and pyridazin-3(2H)-one derivatives as tubulin polymerization inhibitors, Related Products of catalysis-chemistry, the publication is Bioorganic Chemistry (2021), 104522, database is CAplus and MEDLINE.

A potential microtubule destabilizing series of new thirty-five Pyrrol-2-one, Pyridazin-3(2H)-one and Pyridazin-3(2H)-one/oxime derivatives has been synthesized and tested for their antiproliferative activity against a panel of 60 human cancer cell lines. Compounds IVc, IVg and IVf showed a broad spectrum of growth inhibitory activity against cancer cell lines representing renal, cancer of lung, colon, central nervous system, ovary, and kidney. Among them, compound IVg was found to have broad spectrum anti-tumor activity against the tested nine tumor subpanels with selectivity ratios ranging between 0.21 and 3.77 at the GI50 level. In vitro assaying revealed tubulin polymerization inhibition by all active compounds IVc, IVg and IVf. The results of the docking study revealed nice fitting of compounds IVc, IVf, and IVg into CA-4 binding site in tubulin. The three compounds exhibited high binding affinities (ΔGb = -12.49 to -12.99 kcal/mol) toward tubulin compared to CA-4 (-8.87 kcal/mol). Investigation of the binding modes of the three compounds IVc, IVf, and IVg revealed that they interacted mainly hydrophobically with tubulin and similar binding orientations to that of CA-4. These observations suggest that tubulin is a possible target for these compounds

Bioorganic Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Gad, Nourhan M. published the artcileReactivity of 5-phenyl-3-[(2-chloroquinolin-3-yl)methylene]furan-2(3H)-one towards hydrazine and benzylamine: A comparative study, Application In Synthesis of 2051-95-8, the publication is Synthetic Communications (2021), 51(9), 1384-1397, database is CAplus.

The reactivity of a 2-chloroquinolinylfuranone derivative was investigated against two nitrogen nucleophilic reagents namely, hydrazine and benzylamine. It was found that the regioselectivity of the reaction products was mainly dependent on the nature of nucleophiles, reaction conditions and solvent used. Therefore, hydrazinolysis of afforded the corresponding acid hydrazide and pyridazinone derivatives depending on the reaction conditions. Otherwise, benzylamine reacted with at different reaction aspects to provide N-benzylamide, N-benzylpyrrolone, and 2-benzylaminoquinolinyl-N-benzylpyrrolone derivatives The chem. structures of all synthesized compounds were substantiated from their anal. as well as spectroscopic data. Based on the charge d. calculations and computational chem. study which excluded the aza-Michael addition reaction and confirm the higher electron-deficiency of lactone carbonyl group than C2-quinoline position, it could be concluded that the C2-furanone becomes more susceptible to attack by the nucleophilic reagent, hydrazine and benzylamine.

Synthetic Communications published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, Application In Synthesis of 2051-95-8.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Abbott, F. S. published the artcileQuantitative structure-anticonvulsant activity relationships of valproic acid, related carboxylic acids, and tetrazoles, Application of 2-Butylhexanoic acid, the publication is Neuropharmacology (1988), 27(3), 287-94, database is CAplus and MEDLINE.

Valproic acid and several structurally related carboxylic acids and tetrazole analogs antagonized seizures induced by pentylenetetrazole in mice. To investigate the influence of the alkyl substituents on the anticonvulsant activity, the octanol-water partition coefficients and relative pK_a values were determined Within the series of active carboxylic acids, there was a good correlation between the anticonvulsant activity and the partition coefficient The influence of pK_a on the anticonvulsant activity was small but of statistical significance. When the most active compound, 5-heptyltetrazole, was added to the carboxylic acid series, a low correlation between the anticonvulsant activity and a linear combination of lipophilicity and pK_a resulted. The effect of the polar moieties in alkyl-substituted anticonvulsant compounds was assessed by comparison of the regression equations with either an added pK_a or dipole moment term to the term of lipophilicity. It appears that other factors, such as the nature of the alkyl substituent, influence the anticonvulsant activity. The inactivity of the cyclohexylmethyl-substituted compounds, cyclohexylacetic acid, and 5-cyclohexylmethyltetrazole may be due to subtle steric effects at a critical step, either involving oxidative metabolism or an interaction at an active site.

Neuropharmacology published new progress about 3115-28-4. 3115-28-4 belongs to catalysis-chemistry, auxiliary class Aliphatic Chain, name is 2-Butylhexanoic acid, and the molecular formula is C10H20O2, Application of 2-Butylhexanoic acid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Shkulev, V. A. published the artcileOn the connection between reactivity and charge distribution of the azaadamantane ring, Safety of 1,3,5-Triazaadamantan-7-amine, the publication is Armyanskii Khimicheskii Zhurnal (1989), 42(6), 405-7, database is CAplus.

Charge distributions were calculated for di-, tri-, and tetraazaadamantanes; di- and triazahomoadamantane; and a 3,7-diacetyl-1,3,7-triazabicyclononane. Correlations between charge distribution and reactivity were obtained.

Armyanskii Khimicheskii Zhurnal published new progress about 14707-75-6. 14707-75-6 belongs to catalysis-chemistry, auxiliary class Triazinanes, name is 1,3,5-Triazaadamantan-7-amine, and the molecular formula is C18H34N4O5S, Safety of 1,3,5-Triazaadamantan-7-amine.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia