Category: imidazoles-derivatives

Amrutkar, Sunil V. published the artcileSynthesis and antifungal activity of 1-alkyl/H-2-[(4-alkyl/aryl-piperazin-1-yl)-methyl]-benzimidazole derivatives, Computed Properties of 4760-35-4, the publication is International Journal of Pharmacy and Pharmaceutical Sciences (2010), 2(2), 84-92, database is CAplus.

Substituted benzimidazoles were condensed with various substituted piperazine to synthesize a library of benzimidazole derivatives Thus, 2-(chloromethyl)benzimidazoles were prepared from appropriate 1,2-phenylenediamines by boiling for 8 h with ClCH₂CO₂H in concentrated HCl. Subsequent condensation with piperazines was achieved by boiling in dioxane with Et₃N as base. The antifungal activity of the synthesized compounds was studied by disk diffusion against Candida albicans using ketoconazole as reference standard The compound showed antifungal activity comparable to ketoconazole.

International Journal of Pharmacy and Pharmaceutical Sciences published new progress about 4760-35-4. 4760-35-4 belongs to imidazoles-derivatives, auxiliary class Chloride,Benzimidazole, name is 2-(Chloromethyl)-1-methyl-1H-benzo[d]imidazole, and the molecular formula is C9H9ClN2, Computed Properties of 4760-35-4.

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

McReynolds, Katherine D. published the artcileNon-Natural glycosphingolipids and structurally simpler analogues bind HIV-1 recombinant Gp120, Recommanded Product: N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide, the publication is Bioorganic & Medicinal Chemistry (2002), 10(3), 625-637, database is CAplus and MEDLINE.

Interactions of recombinant gp120 (rgp120) with non-natural glycosphingolipids (GSLs) and structurally simpler analogs (e.g., I) have been studied using a competitive adhesion assay. Conjugates of cellobiosyl ceramide and melibiosyl ceramide were synthetically prepared as water-soluble GSL analogs. These ligands were screened against a panel of biol. relevant analogs, and the results show that their interactions with rgp120 are comparable to natural cellular receptors. Glycolipid interactions with rgp120 were probed further by the synthesis and testing of structurally simpler analogs that were obtained by reductive amination of lactose, cellobiose, and melibiose with a biotinylated amino ethylene glycol moiety. RGp120 did not recognize conjugates lacking a lipid component. However, palmitoylation of the secondary amino alditols yielded compounds with comparable rgp120 affinity to the natural cellular receptor, galactosyl ceramide (GalCer). Taken together, the SAR showed that both a hydrophobic and a hydrophilic component are required for rgp120 recognition. Moreover, structural variability in the carbohydrate headgroup did not significantly alter rgp120 recognition indicating that this interaction is not highly specific.

Bioorganic & Medicinal Chemistry 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 C18H34N4O5S, Recommanded Product: N-(2-(2-(2-(2-Aminoethoxy)ethoxy)ethoxy)ethyl)-5-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamide.

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

Butt, Fayaz Ahmad published the artcileImidazolium Based Surface Active Ionic Liquids: Promising Boosters to Enhance the Radical Scavenging and Antioxidant Activity of Conventional Surfactant Solubilised Quercetin, Computed Properties of 79917-90-1, the publication is Catalysis Letters (2022), 152(5), 1276-1285, database is CAplus.

Surface Active Ionic Liquids (SAILs) are emerging as promising alternatives to conventional amphiphiles. Their unique specialties endow the SAIL/SAIL plus conventional surfactant based micellar/mixed micellar systems with unique solubilization, catalytic and electrocatalytic properties. Herein we demonstrate that as a partner of conventional surfactant based mixed micellar systems, imidazolium based SAILs significantly boost the radical scavenging activity (RSA) and antioxidant activity of water insoluble flavonoids. Specifically, we report the RSA and antioxidant activity kinetics of quercetin toward 1,1-diphenyl-2-picrylhydrazyl (DPPH) in aqueous micellar media of SAIL, 1-Butyl-3-methyl-imidazolium dodecylsulfate (BMIMDS), its conventional anionic surfactant analog-sodium dodecylsulfate (SDS), conventional nonionic surfactant-Brij56 and the variedly composed BMIMDS plus Brij56 mixed micellar solutions The presented results clearly suggest that in comparison to the conventional micellar systems, the radical scavenging ability and activity of quercetin for DPPH is appreciably better in appropriately composed SAIL plus conventional surfactant mixed micellar systems. These results further suggest that the RSA of quercetin toward DPPH is a function of its aqueous phase to micellar phase partitioning, locus of solubilization and more importantly its orientation vis-a-vis the later within the micelles. The 1:1 Brij56 plus BMIMDS mixed micellar system seems to offer the best environs for the optimal RSA and kinetics for antioxidant activity of quercetin toward DPPH. The kinetic details and the mechanistic insights presented herein shall stimulate an intense research activity toward use of SAIL and SAIL based micellar systems as promising delivery systems for water insoluble flavonoids for their potential applications as pharmaceuticals and food ingredients.

Catalysis Letters published new progress about 79917-90-1. 79917-90-1 belongs to imidazoles-derivatives, auxiliary class Ionic Liquid,Ionic Liquid, name is 3-Butyl-1-methyl-1H-imidazol-3-ium chloride, and the molecular formula is C8H15ClN2, Computed Properties of 79917-90-1.

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

Saha, Prasenjit published the artcileCobalt-catalyzed intramolecular C-N and C-O cross-coupling reactions: synthesis of benzimidazoles and benzoxazoles, Name: 1,2-Diphenyl-1H-benzo[d]imidazole, the publication is Organic & Biomolecular Chemistry (2010), 8(24), 5692-5699, database is CAplus and MEDLINE.

Cobalt(II)-complex catalyzes efficiently the intramol. C-N and C-O cross-couplings of Z-N’-(2-halophenyl)-N-phenylamidines, e.g. I, and N-(2-bromophenyl)benzamides, e.g. II, to afford the corresponding substituted benzimidazoles and benzoxazoles, e.g. III [X = NPh, O], in the presence of K₂CO₃ at moderate temperature The protocol is general, air stable and affords the products selectively in moderate to high yield.

Organic & Biomolecular Chemistry 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, Name: 1,2-Diphenyl-1H-benzo[d]imidazole.

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

Davood, Asghar published the artcileEfficient synthesis of imidazole derivatives: an important synthon for the preparation of biologically active compounds, Application In Synthesis of 45533-87-7, the publication is Turkish Journal of Chemistry (2008), 32(3), 389-395, database is CAplus.

4(5)-Chloroimidazole-5(4)-carboxaldehydes are important precursors for the preparation of biol. active compounds A simple, novel, and efficient method for the synthesis of these compounds was developed starting from aldehydes, (HOCH₂)₂CO, and NH₄OH. The chem. described is amenable to large-scale use and is flexible enough to allow the preparation of analogs.

Turkish Journal of Chemistry published new progress about 45533-87-7. 45533-87-7 belongs to imidazoles-derivatives, auxiliary class Imidazole,Alcohol,Imidazole, name is (2-Methyl-1H-imidazol-4-yl)methanol, and the molecular formula is C5H8N2O, Application In Synthesis of 45533-87-7.

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

Thomas, Andrew P. published the artcileNew nonpeptide angiotensin II receptor antagonists. 1. Synthesis, biological properties and structure-activity relationships of 2-alkylbenzimidazole derivatives, Synthetic Route of 79047-41-9, the publication is Journal of Medicinal Chemistry (1992), 35(5), 877-85, database is CAplus and MEDLINE.

Based on 2-[4-{2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-ylmethyl}phenyl]benzoic acid, a known angiotensin II receptor antagonist, a series of 1H-benzimidazol-1-yl analogs and 4-[(2-alkyl-1H-benzimidazol-1-yl)methyl]benzoic acids (I, R¹ = alkyl; R² = H, Cl, F, OMe, NO₂; R³ = H, Br, Cl, F, Me, OMe) were prepared The antihypertensive structure-activity relationship of these benzimidazolyl derivatives and some rigid analogs, such as 2-(3-butyl-1-chloro-5H,11H-imidazo[5,1-c][1,4]benzoxazepin-8-yl)benzoic acid (II), was determined

Journal of Medicinal 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 C3H9ClOS, Synthetic Route of 79047-41-9.

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

Nystroem, Lina published the artcileAvidin-Biotin Cross-Linked Microgel Multilayers as Carriers for Antimicrobial Peptides, Formula: C18H34N4O5S, the publication is Biomacromolecules (2018), 19(12), 4691-4702, database is CAplus and MEDLINE.

Herein, we report on the formation of cross-linked antimicrobial peptide-loaded microgel multilayers. Poly(Et acrylate-co-methacrylic acid) microgels were synthesized and functionalized with biotin to enable the formation of microgel multilayers cross-linked with avidin. Microgel functionalization and avidin crosslinking were verified with IR spectroscopy, dynamic light scattering, and z-potential measurements, while multilayer formation (up to four layers) was studied with null ellipsometry and quartz crystal microbalance with dissipation (QCM-D). Incorporation of the antimicrobial peptide KYE28 (KYEITTIHNLFRKLTHRLFRRNFGYTLR) into the microgel multilayers was achieved either in one shot after multilayer formation or through addition after each microgel layer deposition. The latter was found to strongly promote peptide incorporation. Further, antimicrobial properties of the peptide-loaded microgel multilayers against Escherichia coli were investigated and compared to those of a peptide-loaded microgel monolayer. Results showed a more pronounced suppression in bacterial viability in suspension for the microgel multilayers. Correspondingly, LIVE/DEAD staining showed promoted disruption of adhered bacteria for the KYE28-loaded multilayers. Taken together, cross-linked microgel multilayers thus show promise as high load surface coatings for antimicrobial peptides.

Biomacromolecules 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 C18H34N4O5S, Formula: C18H34N4O5S.

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

Sloboda-Rozner, Dorit published the artcileA Water-Soluble and “Self-Assembled” Polyoxometalate as a Recyclable Catalyst for Oxidation of Alcohols in Water with Hydrogen Peroxide, COA of Formula: C8H13ClN2O, the publication is Journal of the American Chemical Society (2003), 125(18), 5280-5281, database is CAplus and MEDLINE.

A water-soluble polyoxometalate, Na₁₂[WZnZn₂(H₂O)₂(ZnW₉O₃₄)₂], synthesized from readily available zinc nitrate and sodium tungstate in the presence of nitric acid, is an effective catalyst for the preparation of ketones and carboxylic acids by selective alc. oxidation with hydrogen peroxide in biphasic (water-alc.) reaction media. Carboxylic acids are obtained by oxidation of primary alcs. with hydrogen peroxide in the presence of Na₁₂[WZnZn₂(H₂O)₂(ZnW₉O₃₄)₂]; addition of catalytic amounts of TEMPO to oxidation mixtures yields increased proportions of the aldehyde in addition to the carboxylic acid. Secondary alcs. are oxidized in preference to primary alcs. to give ketones; carbon-carbon bond cleavage byproducts are seen in one case. The catalyst generated in situ is as active as the isolated catalyst; in addition, the catalyst can be separated and recycled without losses in either selectivity or in activity.

Journal of the American Chemical Society 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 C12H25Br, COA of Formula: C8H13ClN2O.

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

Kracmar, J. published the artcileUltraviolet spectrophotometry in drug control. XX. Study on the effect of substitution and solvents in more recent medicinal substances with the chromophores of benzene rings in the molecules, Related Products of imidazoles-derivatives, the publication is Cesko-Slovenska Farmacie (1976), 25(7), 243-57, database is CAplus.

Thirty RPh, RC6H4-alkyl, RC6H4-halo, RC6H4O-alkyl, RC6H4OH, RC6H4N alkyl2, RC6H4NO2, RC6H4NH2NHaryl, and RC6H4Ch:N(N:N) drugs were characterized by the absorption bands E, K, B, and R, and vibration structures of the bands K and B. Absorption maximum at 235 nm were used for quant. determination of active substances in drugs. More specific long-wave absorption maximum were used for determination of substances having several absorption maximum Agreement with Beer’s law at the recommended absorption maximum was verified.

Cesko-Slovenska Farmacie 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

Kracmar, J. published the artcileUV spectrophotometry in drug analysis. Part 19. New drugs with substituted benzene chromophores, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride, the publication is Pharmazie (1976), 31(9), 614-17, database is CAplus.

Data are given on the uv-spectrophotometric properties of 14 drugs and related compounds containing substituted benzene chromophores. The substituents are alkyl, alkoxy, OH, NO2, NH2, and azomethine. Further, a study of solvent effects (alcs. and H2O, acidic and basic solutions) is reported.

Pharmazie 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, Recommanded Product: N-Benzyl-N-((4,5-dihydro-1H-imidazol-2-yl)methyl)aniline hydrochloride.

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