Day: December 5, 2022

Prajapati, Ronak V. published the artcileElemental sulfur and aryl iodides in copper(I)iodide catalyzed sulfenylation of 1-aryl-3-alkyl-1H-pyrazol-5(4H)-ones, Safety of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Results in Chemistry (2021), 100226, database is CAplus.

The construction of C-S bond is considered as an important protocol in organic transformations. An innovative strategy for CuI-catalyzed sulfenylation of 1-aryl-3-alkyl-1H-pyrazol-5(4H)-ones have been developed using elemental sulfur as the sulfur source. This procedure provides a useful and direct approach for the assembly of a wide range of structurally diverse 4-sulfenyl pyrazolones with moderate to excellent yields from simple and readily available starting materials. This method might be potentially applicable to large scale production, and it enriches current sulfenylation methods.

Results in Chemistry published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Safety of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Melancon, Bruce J. published the artcileIsatin replacements applied to the highly selective, muscarinic M₁ PAM ML137: Continued optimization of an MLPCN probe molecule, Synthetic Route of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2013), 23(2), 412-416, database is CAplus and MEDLINE.

This Letter describes the continued optimization of an MLPCN probe mol. I (ML137) with a focused effort on the replacement/modification of the isatin moiety present in this highly selective M₁ PAM. A diverse range of structures were validated as viable replacements for the isatin, many of which engendered sizeable improvements in their ability to enhance the potency and efficacy of acetylcholine when compared to ML137. Muscarinic receptor subtype selectivity for the M₁ receptor was also maintained.

Bioorganic & Medicinal Chemistry Letters published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 763120-58-7.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Naus, Petr published the artcile6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents, Safety of 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2010), 53(1), 460-470, database is CAplus and MEDLINE.

A series of novel 7-deazapurine ribonucleosides, e.g. I, bearing an alkyl, aryl, or hetaryl group in position 6 and H, F, or Cl atom in position 7, has been prepared either by Pd-catalyzed cross-coupling reactions of the corresponding protected 6-chloro-(7-halogenated-)7-deazapurine ribonucleosides with alkyl- or (het)arylorganometallics followed by deprotection, or by single-step aqueous phase cross-coupling reactions of unprotected 6-chloro-(7-halogenated-)7-deazapurine ribonucleosides with (het)arylboronic acids. Significant cytostatic effect was detected with a substantial proportion of the prepared compounds The most potent were 7-H or 7-F derivatives of 6-furyl- or 6-thienyl-7-deazapurines displaying cytostatic activity in multiple cancer cell lines with a geometric mean of 50% growth inhibition concentration ranging from 16 to 96 nM, a potency comparable to or better than that of the nucleoside analog clofarabine. Intracellular phosphorylation to mono- and triphosphates and the inhibition of total RNA synthesis was demonstrated in preliminary study of metabolism and mechanism of action studies.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Safety of 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Naus, Petr published the artcile6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents, Synthetic Route of 724710-02-5, the publication is Journal of Medicinal Chemistry (2010), 53(1), 460-470, database is CAplus and MEDLINE.

A series of novel 7-deazapurine ribonucleosides, e.g. I, bearing an alkyl, aryl, or hetaryl group in position 6 and H, F, or Cl atom in position 7, has been prepared either by Pd-catalyzed cross-coupling reactions of the corresponding protected 6-chloro-(7-halogenated-)7-deazapurine ribonucleosides with alkyl- or (het)arylorganometallics followed by deprotection, or by single-step aqueous phase cross-coupling reactions of unprotected 6-chloro-(7-halogenated-)7-deazapurine ribonucleosides with (het)arylboronic acids. Significant cytostatic effect was detected with a substantial proportion of the prepared compounds The most potent were 7-H or 7-F derivatives of 6-furyl- or 6-thienyl-7-deazapurines displaying cytostatic activity in multiple cancer cell lines with a geometric mean of 50% growth inhibition concentration ranging from 16 to 96 nM, a potency comparable to or better than that of the nucleoside analog clofarabine. Intracellular phosphorylation to mono- and triphosphates and the inhibition of total RNA synthesis was demonstrated in preliminary study of metabolism and mechanism of action studies.

Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, Synthetic Route of 724710-02-5.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Daidone, G. published the artcileNew N-pyrazolyl salicylamides with antifungal activity, Category: pyrazoles-derivatives, the publication is Farmaco, Edizione Scientifica (1985), 40(9), 683-94, database is CAplus and MEDLINE.

Nine pyrazolyl salicylamides I [R = H or Ph; R¹ and R³ = H or Me; R² = H, Ph, CN, or CO₂Et; R¹R² = (CH₂)₄], as well as II (R = R¹ = R⁴ = H, R² = CO₂Et) [98817-30-2], II (R = R⁴ = H, R² = Me, R³ = CO₂Et) [98817-31-3], II (R = H) [98817-32-4], and (R = Me) [98817-33-5], were prepared and tested in vitro against Cryptococcus neoformans and Candida albicans. All compounds, with the exception of I (R = Ph, R¹ = R² = H, R³ = Me) [98817-34-6], were active. I (R = Ph, R¹ = Me, R² = R³ = H) [70803-10-0] was the most active.

Farmaco, Edizione Scientifica published new progress about 23286-70-6. 23286-70-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Ester, name is Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, and the molecular formula is C7H11N3O2, Category: pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics