Month: November 2022

Wang, Rubing published the artcileStructure-Activity Relationship and Pharmacokinetic Studies of 1,5-Diheteroarylpenta-1,4-dien-3-ones: A Class of Promising Curcumin-Based Anticancer Agents, Recommanded Product: (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol, the publication is Journal of Medicinal Chemistry (2015), 58(11), 4713-4726, database is CAplus and MEDLINE.

Forty-three 1,5-diheteroaryl-1,4-pentadien-3-ones were designed as potential curcumin mimics, structurally featuring a central five-carbon dienone linker and two identical nitrogen-containing aromatic rings. They were synthesized using a Horner-Wadsworth-Emmons reaction as the critical step and evaluated for their cytotoxicity and antiproliferative activities toward both androgen-insensitive and androgen-sensitive prostate cancer cell lines and an aggressive cervical cancer cell line. Most of the synthesized compounds showed distinctly better in vitro potency than curcumin in the four cancer cell lines. The structure-activity data acquired from the study validated (1E,4E)-1,5-diheteroaryl-1,4-pentadien-3-ones as an excellent scaffold for in-depth development for clin. treatment of prostate and cervical cancers. 1-Alkyl-1H-imidazol-2-yl, ortho pyridyl, 1-alkyl-1H-benzo[d]imidazole-2-yl, 4-bromo-1-methyl-1H-pyrazol-3-yl, thiazol-2-yl, and 2-methyl-4-(trifluoromethyl)thiazol-5-yl were identified as optimal heteroaromatic rings for the promising in vitro potency. (1E,4E)-1,5-Bis(2-methyl-4-(trifluoromethyl)thiazol-5-yl)penta-1,4-dien-3-one, featuring thiazole rings and trifluoromethyl groups, was established as the optimal lead compound because of its good in vitro potency and attractive in vivo pharmacokinetic profiles.

Journal of Medicinal Chemistry published new progress about 7467-35-8. 7467-35-8 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Alcohol, name is (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol, and the molecular formula is C5H8N2O2, Recommanded Product: (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Chen, Wei published the artcileOne-pot synthesis of 1,2-diphenyl-1H-imidazole derivatives catalyzed by CuI, Safety of 1,2-Diphenyl-1H-benzo[d]imidazole, the publication is Huaxue Shiji (2011), 33(7), 603-606, database is CAplus.

A new strategy for one step synthesis of 1,2-diphenyl-1H-imidazole derivatives, using CuI to catalyze the C-N and C-C coupling reaction, was described. This method is economical, cost efficient, and harmless. Structures of the products were characterized by ¹H-NMR, ¹³C-NMR, MS spectra and elemental anal.

Huaxue Shiji published new progress about 2622-67-5. 2622-67-5 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Benzene,Benzimidazole, name is 1,2-Diphenyl-1H-benzo[d]imidazole, and the molecular formula is C19H14N2, Safety of 1,2-Diphenyl-1H-benzo[d]imidazole.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Manyar, Haresh G. published the artcileThe green catalytic oxidation of alcohols in water by using highly efficient manganosilicate molecular sieves, Category: imidazoles-derivatives, the publication is Green Chemistry (2006), 8(4), 344-348, database is CAplus.

An efficient and green catalytic protocol for the oxidation of alcs. to the corresponding aldehydes is based on use of manganosilicate mol. sieves as efficient heterogeneous catalyst in aqueous conditions and peroxydisulfate as oxidant. The advantageous feature of this oxidation methodol. is the efficiency and selectivity on heterocyclic and aliphatic alcs. The manganosilicate was prepared through a facile complexation procedure leading to uniform mesoporous cubic structure devoid of extra-framework bulk manganese oxide species.

Green Chemistry published new progress about 79047-41-9. 79047-41-9 belongs to imidazoles-derivatives, auxiliary class Imidazole,Chloride,Alcohol, name is (2-Butyl-4-chloro-1H-imidazol-5-yl)methanol, and the molecular formula is C8H13ClN2O, Category: imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Kapale, Suraj S. published the artcileA sustainable approach towards the three-component synthesis of unsubstituted 1H-imidazoles in the water at ambient conditions, Quality Control of 13682-33-2, the publication is Journal of Asian Natural Products Research (2021), 23(7), 712-716, database is CAplus and MEDLINE.

A green protocol for the synthesis of imidazoles I [R = Ph, 4-BrC₆H₄, 2-furyl, etc.; R¹ = R² = H, Ph] was demonstrated. The reaction was realized using com. available lipase enzyme, porcine pancreas lipase (PPL) in water. The reaction conditions were selective and mild which helped to tolerate a wide variety of functional groups to gave desired products I in good chem. yields.

Journal of Asian Natural Products Research published new progress about 13682-33-2. 13682-33-2 belongs to imidazoles-derivatives, auxiliary class Imidazole,Amine,Benzene, name is 4-(1H-Imidazol-2-yl)aniline, and the molecular formula is C9H9N3, Quality Control of 13682-33-2.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Verhoest, Patrick R. published the artcileDiscovery of a Novel Class of Phosphodiesterase 10A Inhibitors and Identification of Clinical Candidate 2-[4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920)(I) for the Treatment of Schizophrenia, Product Details of C9H10N2O, the publication is Journal of Medicinal Chemistry (2009), 52(16), 5188-5196, database is CAplus and MEDLINE.

By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase (PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a unique “selectivity pocket” for PDE10A inhibitors, and interactions within this pocket allowed the design of highly selective and potent PDE10A inhibitors. Further optimization of brain penetration and drug-like properties led to the discovery of 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) (I). This PDE10A inhibitor is the first reported clin. entry for this mechanism in the treatment of schizophrenia.

Journal of Medicinal Chemistry published new progress about 7467-35-8. 7467-35-8 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Alcohol, name is (1-Methyl-1H-benzo[d]imidazol-2-yl)methanol, and the molecular formula is C11H22N2O4, Product Details of C9H10N2O.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Zhang, Jian-Tao published the artcileTwo-dimensional array Debye ring diffraction protein recognition sensing, Formula: C18H34N4O5S, the publication is Chemical Communications (Cambridge, United Kingdom) (2013), 49(56), 6337-6339, database is CAplus and MEDLINE.

We attach 2-D colloidal arrays onto the surface of hydrogels containing biotin. The hydrogel volume shrinks with increasing concentrations of avidin due to the formation of avidin-biotin crosslinks. This causes the Debye diffraction ring diameter to increase, and the 2-D diffraction wavelength to blue-shift.

Chemical Communications (Cambridge, United Kingdom) published new progress about 359860-27-8. 359860-27-8 belongs to imidazoles-derivatives, auxiliary class Other Aliphatic Heterocyclic,Chiral,Amine,Amide,Ether,Inhibitor, name is N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, and the molecular formula is C12H25Br, Formula: C18H34N4O5S.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Prakash, Sekar published the artcileRhenium(I)-Catalyzed ortho-C-H Addition to Bicyclic Alkenes, Application of 1,2-Diphenyl-1H-benzo[d]imidazole, the publication is Chemistry – An Asian Journal (2018), 13(13), 1664-1668, database is CAplus and MEDLINE.

Hydroarylation of bicyclic alkenes was developed using a low-valent Re^I-catalyzed, directing group-assisted C-H bond activation strategy. The addition of sodium acetate significantly improves the reaction efficiency; moreover, bicyclic alkenes such as 7-oxa and aza benzonorbornadienes worked efficiently under this reaction condition. Preliminary mechanistic studies suggest that, after the alkene insertion, the rhenacycle preferentially undergoes protonolysis rather than reductive elimination.

Chemistry – An Asian Journal published new progress about 2622-67-5. 2622-67-5 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Benzene,Benzimidazole, name is 1,2-Diphenyl-1H-benzo[d]imidazole, and the molecular formula is C19H14N2, Application of 1,2-Diphenyl-1H-benzo[d]imidazole.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Yang, Qi published the artcileA simple phenylation of heteroaromatic compounds using diphenyliodonium triflate, Category: imidazoles-derivatives, the publication is Research on Chemical Intermediates (2012), 38(7), 1335-1340, database is CAplus.

2-Ph heteroaromatic arenes I (Y = S, NH, NMe, NC₆H₅, O; X = CH, N) were prepared by phenylation of heteroaromatic compounds with diphenyliodonium trifluoromethanesulfonate as oxidant in the presence of 5 mol% Pd(OAc)₂ catalyst under mild reaction conditions (THF, 60°, 24 h). The proposed reaction mechanism was studied by HPLC.

Research on Chemical Intermediates published new progress about 2622-67-5. 2622-67-5 belongs to imidazoles-derivatives, auxiliary class Benzimidazole,Benzene,Benzimidazole, name is 1,2-Diphenyl-1H-benzo[d]imidazole, and the molecular formula is C8H8O3, Category: imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Sanghavi, N. M. published the artcileEstimation of antazoline hydrochloride in tablets of antazoline hydrochloride, Related Products of imidazoles-derivatives, the publication is Indian Journal of Pharmacy (1974), 36(6), 137-8, database is CAplus.

The method of estimation of antazoline-HCl [2508-72-7] in tablets was based on the formation of a stable yellow nitroso derivative with NaNO2 solution in the presence of dilute HCl which shows maximum absorption at 412 mμ. A graph of optical d. against concentration gave a straight line over a concentration range of 10 μg/ml to 50 μg/ml showing that the reaction was in compliance with Beer’s Law. Known amounts of antazoline-HCl were added to known amounts of previously analyzed samples of antazoline-HCl and analyzed again by the proposed method. The percentage recovery was 98.6. The proposed method was found to be satisfactory within a narrow range of ± 2%. It was also found that other antihistamines like chlorpheniramine [132-22-9], dimenhydrinate [523-87-5], diphenhydramine [58-73-1] did not interfere. Excipients like starch [9005-25-8], gum arabic [9000-01-5], magnesium stearate [557-04-0], etc. did not interfere while paracetamol [103-90-2], phenylephrine-HCl [61-76-7] interfered.

Indian Journal of Pharmacy published new progress about 2508-72-7. 2508-72-7 belongs to imidazoles-derivatives, auxiliary class Inhibitor,Immunology/Inflammation,Histamine Receptor, name is N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, and the molecular formula is C17H20ClN3, Related Products of imidazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem

Brammer, Matthew K. published the artcileCompatibility of doripenem with other drugs during simulated Y-site administration, Synthetic Route of 161796-78-7, the publication is American Journal of Health-System Pharmacy (2008), 65(13), 1261-1265, database is CAplus and MEDLINE.

The compatibility of doripenem diluted for infusion with 82 other drugs during simulated Y-site administration was studied. Five-milliliter samples of doripenem 5 mg/mL in 5% dextrose injection and sep. in 0.9% sodium chloride injection were combined with 5 mL of 82 other drugs, undiluted or diluted in 5% dextrose injection or 0.9% sodium chloride injection. Visual examinations were performed with the unaided eye in fluorescent light and using a Tyndall beam to enhance visualization of small particles and low-level turbidity. The turbidity of each sample was measured, and particulate content was evaluated. Samples were inspected initially and one and four hours after preparation Of the drugs tested, doripenem 5 mg/mL in 5% dextrose injection and in 0.9% sodium chloride injection was incompatible with diazepam, potassium phosphates, and undiluted propofol. Doripenem 5 mg/mL in 0.9% sodium chloride injection but not in 5% dextrose injection was incompatible with amphotericin B-containing drugs due to the diluent. Doripenem was found to be compatible when combined with the other 75 drugs for at least four hours. Doripenem 5 mg/mL in 5% dextrose injection or in 0.9% sodium chloride injection was phys. compatible for four hours at room temperature with 75 drugs during simulated Y-site administration. Three drugs combined with doripenem in 5% dextrose injection or 0.9% sodium chloride injection and 7 drugs combined with doripenem in 0.9% sodium chloride injection resulted in unacceptable precipitation or an increase in measured haze and should not be simultaneously administered with doripenem admixtures

American Journal of Health-System Pharmacy published new progress about 161796-78-7. 161796-78-7 belongs to imidazoles-derivatives, auxiliary class Membrane Transporter/Ion Channel,Proton Pump, name is Sodium (S)-6-methoxy-2-(((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide, and the molecular formula is C17H18N3NaO3S, Synthetic Route of 161796-78-7.

Referemce:
https://en.wikipedia.org/wiki/Imidazole,
Imidazole | C3H4N2 – PubChem