Tag: M.W=100-150

Novacek, L. published the artcileAntituberculotics. XI. Functional derivatives of 5-substituted 2-pyrazinecarboxylic acid, Recommanded Product: Pyrazine-2-carbothioamide, the publication is Cesko-Slovenska Farmacie (1972), 21(4), 145-9, database is CAplus.

Of several amides, thioamides, hydrazides, and hydrazones of 5-halo-, 5-alkoxy-, and 5-hydrazino-2-pyrazinecarboxylic acids tested, 5-hydrazino-2-pyrazinecarboxylic acid hydrazide [21279-75-4], N2, N5-divanillylidene-5-hydrazino-2-pyrazinecarboxylic acid hydrazide (I) [36805-05-7] and 5-bromo-2-pyrazinecarboxamide [36070-84-5] were the most effective against Mycobacterium tuberculosis and M. kansasii in vitro. When tested on mice in vivo, 5-methoxy-2-pyrazinecarboxamide [19222-85-6] and 2-pyrazinecarboxylic acid hydrazide [768-05-8] had less antitubercular activity than did pyrazinamide [98-96-4].

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, Recommanded Product: Pyrazine-2-carbothioamide.

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

Vontor, T. published the artcileAntituberculotics. XLI. Functional derivatives of 5-alkyl-2-pyrazinecarboxylic acid, Application of Pyrazine-2-carbothioamide, the publication is Cesko-Slovenska Farmacie (1987), 36(6), 277-80, database is CAplus.

Amides of 5-alkyl-2-carboxypyrazines (I, R = Pr, iso-Pr, Bu, iso-Bu; R¹ = H; X = O) were converted into hydrazides (I, R¹ = NH₂; X = O) by hydrazinolysis and also into thioamides (I, R¹ = H; X = S) (II) by reaction the with P₂S₅. Minimal inhibitory concentrations of I were determined in cultures of Mycobacterium, tuberculosis, M. kansasii, M. avium, and M. fortuitum. The greatest in vitro tuberculostatic activity was seen with II (R = Pr). In mice exptl., infected with M. tuberculosis, therapeutic effects were obtained with I (R = iso-Pr; R¹ = H; X = O) and II (R = iso-Pr). Acute i.p. toxicities in mice for these 2 compounds were 325 and 196 mg/kg, resp. Structure-activity relations are discussed.

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 C21H37BO, Application of Pyrazine-2-carbothioamide.

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

Dwyer, Michael P. published the artcileDiscovery of pyrazolo[1,5-a]pyrimidine-based CHK1 inhibitors: A template-based approach-Part 1, Product Details of C4H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(1), 467-470, database is CAplus and MEDLINE.

The synthesis and hit-to-lead SAR development of a pyrazolo[1,5-a]pyrimidine hit I is described leading to a series of potent, selective CHK1 inhibitors such as compound II. The further utility of the pyrazolo[1,5-a]pyrimidine template for the development of potent, selective kinase inhibitors is detailed.

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, Product Details of C4H5BN2O2.

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

Yang, Jianzhong published the artcile3H-1,2,4-Dithiazol-3-one compounds as novel potential affordable antitubercular agents, Application In Synthesis of 4604-72-2, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(5), 1424-1427, database is CAplus and MEDLINE.

Small mols. with oxathiazol-2-one moiety were recently reported as potent inhibitors of Mycobacterium bovis var. bacilli Calmette-Guerin (BCG), among which HT1171 (I) was the most potent and selective proteasome inhibitor. Herein we synthesized a series of novel compounds by bioisosteric replacement of the oxathiazol-2-one ring with 3H-1,2,4-dithiazol-3-one, and also fifteen 1,3,4-oxathiazol-2-one mols. in order for potency comparison and structure-activity relationship elucidation since their antibacterial effects on the virulent strains were not evaluated before. All the compounds were assessed for antitubercular activities on the virulent H37Rv strain by a serial dilution method. Among the tested compounds, 3H-1,2,4-dithiazol-3-one derivative II was found to be the most active with a lowest MIC₉₀ value of 1 μg/mL. Furthermore, the cytotoxicities of all the compounds against normal human liver cell line L02 were determined by an MTT method. Compound II displayed a lower inhibitory ratio than HT1171 at the concentration of 100 μM, indicating its better safety profile.

Bioorganic & Medicinal Chemistry 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 C4H11NO, Application In Synthesis of 4604-72-2.

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

Mollin, J. published the artcileN-substituted pyridinethiocarboxamides and related compounds as potential antituberculotics, Name: Pyrazine-2-carbothioamide, the publication is Chemical Papers (1988), 42(6), 811-16, database is CAplus.

Pyridine- and pyrazinethiocarboxamides, e.g. I (R = H, Et, R¹ = CONHC₆H₄Cl-3, CONHC₆H₄Cl-4; R = H, R¹ = H, COEt, CSNHMe, CSNHPh), have been acylated with acid anhydrides and added to isocyanates and isothiocyanates. Antimycobacterial activity of the reaction products was examined The influence of substituents on the antimycobacterial activity was compared to the analogous thiobenzamide derivatives

Chemical Papers 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, Name: Pyrazine-2-carbothioamide.

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

Reddy, B. Venkata published the artcileStudies on synthesis and antifungal activity of pyrazine connected 1,2,4-triazol derivatives, Synthetic Route of 4604-72-2, the publication is European Journal of Biomedical and Pharmaceutical Sciences (2017), 4(8), 1022-1026, database is CAplus.

Encouraged by the broad spectrum of biol. activities of pyrazine and 1,2,4-triazoles, a series of 4-(benzylidene-amino)-5-(4-methyl-2-pyrazin-2-yl-thiazol-5-yl)-4H-[1,2,4]triazole-3-thiol and its derivatives I [R = H, Me, Br, etc.] were synthesized by involving various intermediates like 4-methyl-2-pyrazin-2-yl-thiazole-5-carboxylic acid Et ester, 4-methyl-2-pyrazin-2-yl-thiazole-5-carboxylic acid hydrazide, potassium N-(4-methyl-2-pyrazine-2-yl-thiazole-5-carbonyl)-hydrazine carbodithioate and 3-methyl-5-(4-methyl-2-pyrazin-2-yl-thiazol-5-yl)-[1,2,4]-triazol-4-ylamine and from pyrazine-2-carbothioic amide as raw material. Structures of the synthesized compounds I were elucidated by IR, ¹H-NMR and mass spectral data. All of the compounds I were tested for antifungal activity and found that all the compounds I exhibited marginal to good antifungal activity.

European Journal of Biomedical and Pharmaceutical Sciences 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, Synthetic Route of 4604-72-2.

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

Rooney, C. S. published the artcileInhibitors of glycolic acid oxidase. 4-Substituted 3-hydroxy-1H-pyrrole-2,5-dione derivatives, COA of Formula: C5H5N3S, the publication is Journal of Medicinal Chemistry (1983), 26(5), 700-14, database is CAplus and MEDLINE.

The title compounds I (R = aryl, aryloxy, heterocycle, etc.; R¹ = H, Me, or Ph) and related ones were prepared and evaluated as orally absorbable inhibitors of glycolic acid oxidase (GAO) [9028-71-1] and to examine their effect on oxalate production in animals. Inhibitors of GAO are of interest as potentially useful drugs for treatment of Ca oxalate renal lithiasis and the primary hyperoxalurias. Rat liver perfusion with 3 of the most potent I have shown effective inhibition of the conversion of glycolate to oxalate in this organ. 4-(4‘-Bromo[1,1‘-biphenyl]-4-yl)-3-hydroxy-1H-pyrrole-2,5-dione (I; R = C₆H₄-4-(4-BrC₆H₄); R¹ = H) [77529-42-1] administered orally to ethylene glycol treated rats showed reduction in oxalate excretion in urine. QSAR are discussed.

Journal of Medicinal Chemistry 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

Kumar, R. Uday published the artcileMetal free synthesis of diaryl selenides using SeO₂ as a selenium source, Formula: C4H5BN2O2, the publication is Tetrahedron Letters (2016), 57(37), 4138-4141, database is CAplus.

A simple, efficient, and eco-friendly synthetic protocol has been developed for the preparation of diaryl selenium compds RSeR (R = C₆H₅, 3-FC₆H₄, 2-thienyl, etc.). The use of selenium dioxide as selenium source for the synthesis of diaryl selenides has been described for the first time. Compared with other selenium sources the new source SeO₂ gives an environment-friendly and low-cost synthetic route, which may be useful for large-scale synthesis.

Tetrahedron 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, Formula: C4H5BN2O2.

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

Zeng, Qingbei published the artcileSynthesis and SAR studies of benzimidazolone derivatives as histamine H₃-receptor antagonists, Computed Properties of 762263-64-9, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(21), 6001-6003, database is CAplus and MEDLINE.

A novel series of benzimidazolone-containing histamine H₃-receptor antagonists were prepared and their structure-activity relationship was explored. These benzimidazolone analogs demonstrate potent H₃-receptor binding affinities, no P 450 enzyme inhibition, and strong H₃ functional activity. Compound I exhibits the best overall profile with H₃K_i = 0.95 nM and rat AUC = 12.9 μM h.

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 C12H9NO, Computed Properties of 762263-64-9.

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

Ertas, Merve published the artcilePotent ribonucleotide reductase inhibitors: Thiazole-containing thiosemicarbazone derivatives, SDS of cas: 4604-72-2, the publication is Archiv der Pharmazie (Weinheim, Germany) (2019), 352(11), 1900033, database is CAplus and MEDLINE.

The antioxidant, antimalarial, antibacterial, and antitumor activities of thiosemicarbazones have made this class of compounds important for medicinal chemists. In addition, thiosemicarbazones are among the most potent and well-known ribonucleotide reductase inhibitors. In this study, 24 new thiosemicarbazone derivatives were synthesized, and the structures and purity of the compounds were determined by IR, ¹H NMR, ¹³C NMR, mass spectroscopy, and elemental anal. The IC₅₀ values of these 24 compounds were determined with an assay for ribonucleotide reductase inhibition. Compounds 19, 20, and 24 inhibited ribonucleotide reductase enzyme activity at a higher level than metisazone as standard The cytotoxic effects of these compounds were measured on the MCF7 (human breast adenocarcinoma) and HEK293 (human embryonic kidney) cell lines. Similarly, compounds 19, 20, and 24 had a selective effect on the MCF7 and HEK293 cell lines, killing more cancer cells than cisplatin as standard The compounds (especially 19, 20, and 24 as the most active ones) were then subjected to docking experiments to identify the probable interactions between the ligands and the enzyme active site. The complex formation was shown qual. The ADME (absorption, distribution, metabolism, and excretion) properties of the compounds were analyzed using in-silico techniques.

Archiv der Pharmazie (Weinheim, Germany) 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, SDS of cas: 4604-72-2.

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