Tag: M.W=100-150

Melancon, Bruce J. published the artcileOptimization of M₄ pos. allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacol., Related Products of pyrazines, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(11), 2296-2301, database is CAplus and MEDLINE.

Optimization of M₄ pos. allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacol. This letter describes the further chem. optimization of the 5-amino-thieno[2,3-c]pyridazine series (VU0467154/VU0467485) of M₄ pos. allosteric modulators (PAMs), developed via iterative parallel synthesis, culminating in the discovery of the non-human primate (NHP) in vivo tool compound, VU0476406 (8p). VU0476406 is an important in vivo tool compound to enable translation of pharmacodynamics from rodent to NHP, and while data related to a Parkinson’s disease model has been reported with 8p, this is the first disclosure of the optimization and discovery of VU0476406, as well as detailed pharmacol. and DMPK properties.

Bioorganic & Medicinal Chemistry Letters published new progress about 762263-64-9. 762263-64-9 belongs to pyrazines, auxiliary class Pyrazine,Boronic acid and ester,Boronic Acids, name is Pyrazin-2-ylboronic acid, and the molecular formula is C4H5BN2O2, Related Products of pyrazines.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Guernon, Jason M. published the artcile3-Bromocyclohexane-1,2-dione as a useful reagent for Hantzsch synthesis of thiazoles and the synthesis of related heterocycles, Safety of Pyrazine-2-carbothioamide, the publication is Tetrahedron Letters (2011), 52(28), 3633-3635, database is CAplus.

The authors describe the use of 3-bromocyclohexane-1,2-dione, an air stable, versatile reagent for the Hantzsch thiazole synthesis and the synthesis of other closely related heterocycles. For example, cyclocondensation of 3-bromocyclohexane-1,2-dione with RC(S)NH₂ (R = Ph, 4-pyridyl, t-Bu, etc.) gave I.

Tetrahedron Letters published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Safety of Pyrazine-2-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Zhai, Xin published the artcileSynthesis and antibacterial activities of 3-fluoro-4-(2-arylthiazol-4-yl)phenyloxazolidinone derivatives, Recommanded Product: Pyrazine-2-carbothioamide, the publication is Shenyang Yaoke Daxue Xuebao (2007), 24(5), 275-279, database is CAplus.

Fourteen new 3-fluoro-4-(2-arylthiazol-4-yl)phenyloxazolidinone derivatives was prepared from 2-chloromethyloxrane and 3-fluorophenyl isocyanate in seven steps to provide the target products and their structures are confirmed by ¹H NMR and MS. Primary in vitro antibacterial activity test indicated that ten of them show antibacterial activities.

Shenyang Yaoke Daxue Xuebao published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C3H12Cl2N2, Recommanded Product: Pyrazine-2-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Seko, Norihiko published the artcileSynthesis and platelet aggregation inhibitory activity of diphenylazole derivatives. I. Thiazole and imidazole derivatives, COA of Formula: C5H5N3S, the publication is Chemical & Pharmaceutical Bulletin (1991), 39(3), 651-7, database is CAplus and MEDLINE.

Diphenylimidazoles I (X = NH, R = OMe, R¹ = 2-, 3-, 4-pyridyl, 6-methyl-2-pyridyl, 2-, 3-thienyl, 5-methyl-2-thienyl, 3-methyl-2-thienyl, 2-pyrrolyl, 1,5-dimethyl-2-pyrrolyl) were prepared by the cyclocondensation of p-anisil with R¹CHO in the presence of NH₄OAc. Diphenylthiazoles I (X = S; R = OMe, H, F, SMe; R¹ = as above) were prepared by the cyclocondensation of p-RC₆H₄COCHBrC₆H₄R-p with R¹C(:S)NH₂. I (X = NH, S) were tested as inhibitors of platelet aggregation in in vitro experiments Diphenylthiazoles I (X = S) were more potent than diphenylimidazoles I (X = NH) in inhibiting arachidonic acid-induced platelet aggregation of rabbit platelet-rich plasma. Two diphenylimidazole and eight diphenylthiazole derivatives were evaluated for ex vivo arachidonic acid and collagen-induced platelet aggregation inhibitory activity using guinea pigs. I (R = OMe, R¹ = 1,5-dimethylpyrrol-2-yl, X = S) (II) showed strong activity in vitro and ex vivo. The ex vivo activity of II was 200 times stronger than that of aspirin.

Chemical & Pharmaceutical Bulletin published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C20H28B2O4S2, COA of Formula: C5H5N3S.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Dar’in, Dmitry published the artcileNon-chelating p-phenylidene-linked bis-imidazoline analogs of known influenza virus endonuclease inhibitors: Synthesis and anti-influenza activity, Computed Properties of 762263-64-9, the publication is European Journal of Medicinal Chemistry (2019), 526-532, database is CAplus and MEDLINE.

A novel chemotype topol. similar to known influenza virus PA endonuclease inhibitors was designed. It was aimed to reproduce the extended topol. of the known metal-chelating ligands with a p-phenylidene-linked bis-imidazoline scaffold. It was envisioned that aromatic groups introduced to this scaffolds via metal-catalyzed N-arylation (Buchwald-Hartwig or Chan-Evans-Lam) would contribute to lipophilic binding to the target and one of the imidazoline nitrogen atoms would ensure non-chelating coordination to the prosthetic divalent metal ion. The compounds displayed appreciable anti-influenza activity in vitro and substantial concentration window from the general cytotoxicity range. Docking anal. of low-energy poses of the most active compound (as well as their comparison to the binding of an inactive compound) revealed that these compounds reproduced similar binding components to a known PA endonuclease inhibitor and displayed similar binding pose and desired monodentate metal coordination, as was initially envisioned. These findings warrant further study of the mechanism of action of the newly discovered series.

European Journal of Medicinal Chemistry published new progress about 762263-64-9. 762263-64-9 belongs to pyrazines, auxiliary class Pyrazine,Boronic acid and ester,Boronic Acids, name is Pyrazin-2-ylboronic acid, and the molecular formula is C4H5BN2O2, Computed Properties of 762263-64-9.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Hearn, Brian R. published the artcileC-15 Thiazol-4-yl Analogues of (E)-9,10-Didehydroepothilone D: Synthesis and Cytotoxicity, Application In Synthesis of 4604-72-2, the publication is Organic Letters (2006), 8(14), 3057-3059, database is CAplus and MEDLINE.

The syntheses and biol. evaluation of six epothilone D analogs are reported. These side-chain variants of the (E)-9,10-didehydroepothilone scaffold contain C15 thiazole appendages that are derived from bromomethyl ketone intermediates. Although each of these analogs is less cytotoxic than the parent (E)-9,10-didehydroepothilone D, three maintain IC₅₀ values in the double-digit nanomolar range against both susceptible and resistant cell lines.

Organic Letters published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Application In Synthesis of 4604-72-2.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Zhai, Xin published the artcileSynthesis and antibacterial activity of novel oxazolidinone analogs containing substituted thiazole/fused-bicyclic groups, Related Products of pyrazines, the publication is Chemical Research in Chinese Universities (2006), 22(4), 459-464, database is CAplus.

Sixteen novel oxazolidinone analogs containing substituted thiazole/fused-bicyclic (imidazo[1,2-b]pyridazine/imidazo[2,1-b]thiazole) groups were designed and synthesized. A new method for the preparation of the key intermediate is proposed. The structures of the target compounds were confirmed by ¹H NMR, IR and MS, and their in vitro antibacterial activities against Staphylococcus aureus were evaluated. Among them, I displays a promising antibacterial activity comparable to that of linezolid.

Chemical Research in Chinese Universities published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C12H9N3O4, Related Products of pyrazines.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Bonati, F. published the artcileAntibacterial activity of substituted thioamides in relation to chemical constitution, COA of Formula: C5H5N3S, the publication is International Congress of Chemotherapy, Proceedings (1964), 1963(1), 183-5, database is CAplus.

A large number of the title compounds were tested in vitro against Mycobacterium tuberculosis H37Rv, Staphylococcus aureus (Oxford strain), Escherichia coli (1st. Sieroterap. Milanese 95), Proteus vulgaris (I.S.M. 2), and Pseudomonas aeruginosa (I.S.M. 32). Structural formulas and inhibitory concentrations of the compounds are indicated for M. tuberculosis, S. aureus, and Ε. coli. For simple thioamides, inhibitory activity was almost absent for the 4 test organisms other than M. tuberculosis. The test compounds (Mannich bases) contained either 1 or 2 N atoms in their heterocyclic rings. The inhibitory concentrations for P. vulgaris and P. aeruginosa were very similar to those for Ε. coli. In antitubercular activity, the ethyl isonicotinic thioamide was superior to other thioamides, while the activity of Mannich bases derived from 3-pyridine thiocarboxamide and from pyrazinethiocarboxamide was superior to that of various other compounds

International Congress of Chemotherapy, Proceedings published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, COA of Formula: C5H5N3S.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Greksakova, O. published the artcileAntitubercular agents. VIII. Spectral study of some pyrazinecarboxylic acid derivatives, Product Details of C5H5N3S, the publication is Cesko-Slovenska Farmacie (1967), 16(10), 515-19, database is CAplus.

Physicochem. characteristics of pyrazinecarboxamide (pyrazineamide), 5-methoxy-2-pyrazinecarboxamide, 5-butoxy-2-pyrazinecarboxamide and pyrazinecarboxylic acid thioamide were studied by uv spectroscopy. The differences at various pH are not caused by accepting or delivering the proton. Character of the two electronic oscillations in the mol. of each (energy and polarity and their changes caused by the polarity of the solvent) demonstrates the differences.

Cesko-Slovenska Farmacie published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Product Details of C5H5N3S.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem

Cote, L. published the artcileNicotinamide antagonists, Recommanded Product: Pyrazine-2-carbothioamide, the publication is Experimental Medicine and Surgery (1953), 96-102, database is CAplus.

cf. C.A. 46, 9714c. Acetylpyrazine, cyanopyrazine, pyrazine thiocarboxamide, and mercaptopyrazine were reversible nicotinamide antagonists for Lactobacillus arabinosus, while 37 related compounds were inactive. No significant inhibition of the nicotinamide growth response could be demonstrated in rats or chicks.

Experimental Medicine and Surgery published new progress about 4604-72-2. 4604-72-2 belongs to pyrazines, auxiliary class Pyrazine,Amine,Amide, name is Pyrazine-2-carbothioamide, and the molecular formula is C5H5N3S, Recommanded Product: Pyrazine-2-carbothioamide.

Referemce:
https://en.wikipedia.org/wiki/Pyrazine,
Pyrazine | C4H4N2 – PubChem