Tag: M.W=150-200

Garuti, Laura published the artcileSynthesis and antiviral/antiproliferative activity of some N-sulphonylbenzimidazoles, Recommanded Product: Methyl 1H-benzo[d]imidazole-2-carboxylate, the main research area is benzimidazolyl sulfone antiviral antiproliferative preparation.

Some benzimidazolyl sulfones were synthesized and evaluated for their antiviral and antiproliferative properties. I (R = CHMe2) displayed significant and selective activity against human cytomegalovirus (CMV), I (R = 3-NO2-C6H4) showed activity against varicella zoster virus (VZV). The compounds were further evaluated for inhibitory effect on the proliferation of murine leukemia cells and human T-lymphocyte cells. Marked cytotoxicity was noted with different derivatives Some structure-activity relationships are discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Recommanded Product: Methyl 1H-benzo[d]imidazole-2-carboxylate.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Volynets, Galyna published the artcileIdentification of protein kinase fibroblast growth factor receptor 1 (FGFR1) inhibitors among the derivatives of 5-(5,6-dimethoxybenzimidazol-1-yl)-3-hydroxythiophene-2-carboxylic acid, Application of 5,6-Dimethoxy-1H-benzo[d]imidazole, the main research area is dimethoxy benzimidazolyl hydroxythiophene carboxylate preparation FGFR1 inhibitor cancer.

Abstract: Fibroblast growth factor receptor 1 (FGFR1) plays an important role in tumorigenesis, suggesting that inhibitors of this protein kinase may become important compounds for the development of anticancer agents. Using mol. docking approach, we have identified a novel class of FGFR1 inhibitors belonging to the derivatives of 5-(5,6-dimethoxybenzimidazol-1-yl)-3-hydroxythiophene-2-carboxylic acid. It was revealed that the most promising compound 5-(5,6-dimethoxybenzimidazol-1-yl)-3-[2-(methanesulfonyl)benzyloxy]thiophene-2-carboxylic acid Me ester inhibits FGFR1 with an IC50 value of 150 nM in in vitro kinase assay. The structure-activity relationships have been studied, and the binding mode of this chem. class has been proposed. Graphic abstract: [Figure not available: see fulltext.].

Monatshefte fuer Chemie published new progress about Antitumor agents. 72721-02-9 belongs to class imidazoles-derivatives, name is 5,6-Dimethoxy-1H-benzo[d]imidazole, and the molecular formula is C9H10N2O2, Application of 5,6-Dimethoxy-1H-benzo[d]imidazole.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Zheng, Xiaozhang published the artcileStructure-Based Discovery of Novel Amide-Containing Nicotinamide Phosphoribosyltransferase (Nampt) Inhibitors, Category: imidazoles-derivatives, the main research area is amide containing nicotinamide phosphoribosyltransferase inhibitor preparation cancer.

Crystal structures of several urea- and thiourea-derived compounds in complex with the nicotinamide phosphoribosyltransferase (Nampt) protein were utilized to design a potent amide-containing inhibitor bearing an aza-indole moiety (Nampt BC IC50 = 9.0 nM, A2780 cell proliferation IC50 = 10 nM). A Nampt cocrystal structure was subsequently obtained and enabled the design of addnl. amide-containing inhibitors which incorporated various other fused 6,5-heterocyclic moieties and biaryl sulfone or sulfonamide motifs. Addnl. modifications of these mols. afforded many potent biaryl sulfone-containing Nampt inhibitors which also exhibited favorable in vitro ADME properties (microsomal and hepatocyte stability, MDCK permeability, plasma protein binding). An optimized compound was a potent inhibitor of multiple cancer cell lines (IC50 <10 nM vs U251, HT1080, PC3, MiaPaCa2, and HCT116 lines), displayed acceptable mouse PK properties (F = 41%, CL = 52.4 mL/min/kg), and exhibited robust efficacy in a U251 mouse xenograft model. Journal of Medicinal Chemistry published new progress about Antitumor agents. 588720-29-0 belongs to class imidazoles-derivatives, name is Imidazo[1,5-a]pyridine-7-carboxylic acid, and the molecular formula is C8H6N2O2, Category: imidazoles-derivatives.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Garuti, L. published the artcileSynthesis and antiviral assays of some 2-substituted benzimidazole-N-carbamates, Application of Methyl 1H-benzo[d]imidazole-2-carboxylate, the main research area is benzimidazolecarbamate preparation antiviral activity; carbamate benzimidazole preparation antiviral activity.

The title compounds were synthesized and tested in vitro for antiviral activity. Carbamates I (R = i-PrNHCO, R1 = MeO; R = MeSCH2, R1 = i-PrO) were active at noncytotoxic concentrations The results confirmed the importance of the substituents at the 2-position of benzimidazole; an isopropylcarboxamide group led to the best activity.

Farmaco published new progress about Antiviral agents. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Application of Methyl 1H-benzo[d]imidazole-2-carboxylate.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Kiselyov, Alexander S. published the artcile2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: Novel dual inhibitors of VEGFR-1/2 kinases, COA of Formula: C9H10N2O2, the main research area is azolyl arylbenzamide preparation VEGFR kinase inhibitor SAR.

Novel potent derivatives of (azol-1-yl)methyl-N-arylbenzamides with improved solubility (>3 mM) are described as ATP-competitive inhibitors of vascular endothelial growth factor receptor 2 (VEGFR-2). Many compounds display VEGFR-2 inhibitory activity reaching IC50 < 100 nM in the enzymic assay. The compounds also inhibit the related tyrosine kinase, VEGFR-1, with similar potencies. Several compounds containing bulky lipophilic substituents at the benzamide pharmacophore yielded 10- to 17-fold selectivity for the VEGFR-2 vs. VEGFR-1 kinase. Bioorganic & Medicinal Chemistry Letters published new progress about Molecular modeling. 72721-02-9 belongs to class imidazoles-derivatives, name is 5,6-Dimethoxy-1H-benzo[d]imidazole, and the molecular formula is C9H10N2O2, COA of Formula: C9H10N2O2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Vaultier, Michel published the artcileFormation of a 1,2,4-oxadiazoline from an aziridine: mechanism of the reaction and photochemical conversion into a benzimidazole derivative, Application In Synthesis of 5805-53-8, the main research area is aziridinedicarboxylate cleavage nitrite; phenylaziridinedicarboxylate cleavage nitrite; rearrangement photolysis phenyloxadiazoline; oxadiazoline phenyl rearrangement benzimidazole; benzimidazolecarboxylate.

Reaction of NaNO2 with the aziridine I in the presence of BzOH gave 75% oxadiazoline II, which on photolysis in C6H6 gave 86% benzimidazole III. The formation of II probably involved addition of NaNO2 to PhCH:N+PhCH(CO2Me)2 BzO-, followed by cyclization, and demethoxycarbonylation by a β-lactam path.

Journal of the Chemical Society, Chemical Communications published new progress about Photorearrangement. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Application In Synthesis of 5805-53-8.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Boegesoe, Klaus P. published the artcileAntihypertensive activity in a series of 1-piperazino-3-phenylindans with potent 5-HT2-antagonistic activity, Recommanded Product: 1-(2-Chloroethyl)-1H-benzo[d]imidazol-2(3H)-one, the main research area is piperazinophenylindan preparation antihypertensive structure activity; irindalone preparation antihypertensive; hydroxytryptamine antagonist piperazinophenylindan.

A series of trans-1-piperazino-3-phenylindans, e.g., I (R = H, F; R1 = H, 2-F, 4-F, 4-Cl, 4-OH, 4-OMe; n,m = 2,3; X = NH, O, CH2, NH, NMe, NEt, NCHMe2; X1 = O, S) were synthesized with the goal of replacing their established neuroleptic profile with that of peripheral 5-hydroxytryptamine (5-HT2) antagonism. Compounds with an unsubstituted for F-substituted in the 6-position in the indan ring, and which had a five- or six-membered heterocyclic ring attached by an ethylene chain to the piperazine ring, satisfied this objective. Some of the compounds had potent antihypertensive activity in conscious spontaneously hypertensive rats. In pithed rats they antagonized the pressor effect induced by 5-HT in doses 100-1000 times lower than doses needed to antagonize the pressor effect of phenylephrine. The effect was stereoselective and associated with enantiomers with 1R,3S absolute configuration. 1S,3R Enantiomers inhibited the uptake of dopamine and norepinephrine in vitro. The compound with the best antihypertensive activity was irindalone. Its pharmacol. profile resembled that of the standard compound ketanserin. There was a close structural correspondence between ketanserin and irindalone in a conformation that was identified as a D-2 receptor-relevant configuration of its neuroleptic parent tefludazine. This suggests that the dopaminergic (D-2) and the serotoninergic (5-HT2) pharmacophores are structurally closely related.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 52548-84-2 belongs to class imidazoles-derivatives, name is 1-(2-Chloroethyl)-1H-benzo[d]imidazol-2(3H)-one, and the molecular formula is C9H9ClN2O, Recommanded Product: 1-(2-Chloroethyl)-1H-benzo[d]imidazol-2(3H)-one.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Feng, Zihao published the artcileConstruction and investigation of chiral and photoluminescent Metal-Organic framework based on Zn(II) ions and achiral methoxy-functionalized benzimidazolate linkers, SDS of cas: 72721-02-9, the main research area is dimethoxy benzimidazolate zinc metal organic framework preparation crystal structure; chiral photoluminescent dimethoxy benzimidazolate zinc MOF preparation crystal structure.

A Zn(II)-based metal-organic framework, namely MeOBim-Zn (1), has been prepared by the reaction between 5,6-dimethoxy-1H-benzo[d]imidazole (MeOBimH) and Zn(NO3)2 in the presence of aqueous ammonia through solvothermal method and characterized by single-crystal x-ray diffraction, TGA and FT-IR. 1 Exhibits a (10,3)-a chiral network constructing from achiral MeOBim- linker and Zn(II) ions via spontaneous resolution In addition, 1 shows photoluminescent emission at 433 nm upon photoexcitation at 365 nm and this emission may originate from dissipation of metal-perturbed π(MeOBim-) to π*(MeOBim-) intraligand (IL) excited state.

Inorganic Chemistry Communications published new progress about Crystal structure. 72721-02-9 belongs to class imidazoles-derivatives, name is 5,6-Dimethoxy-1H-benzo[d]imidazole, and the molecular formula is C9H10N2O2, SDS of cas: 72721-02-9.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Diez-Barra, Enrique published the artcileN,N’-linked 1,2-ethanediyl-poly(benzimidazolin-2-ones) and the x-ray crystal structure of a benzimidazolin-2-one trimer, SDS of cas: 52548-84-2, the main research area is benzimidazolone oligomer mol crystal structure.

Seven dimers, three trimers, a cyclic tetramer, and an open chain benzimidazolin-2-one heptamer have been prepared and characterized by 1H, 13C NMR and by MS. The crystal and mol. structure of the trimer, 1,3-bis[2-(2-oxobenzimidazol-1-yl)ethyl]-2-oxobenzimidazole, has been solved by x-ray anal. The mols. are hydrogen bonded to four others in a continuous two-dimensional network by N-H···O=C and C-H···O=C interactions in which all N-H donors and O=C acceptors are involved.

Tetrahedron published new progress about Crystal structure. 52548-84-2 belongs to class imidazoles-derivatives, name is 1-(2-Chloroethyl)-1H-benzo[d]imidazol-2(3H)-one, and the molecular formula is C9H9ClN2O, SDS of cas: 52548-84-2.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Lopyrev, V. A. published the artcileTransmission of the substituent effects in 2-substituted benzimidazoles studied by proton and carbon-13 nuclear magnetic resonance, Application of Methyl 1H-benzo[d]imidazole-2-carboxylate, the main research area is benzimidazole NMR substituent effect; transmission electronic effect benzimidazole substituent; solvent effect benzimidazole NMR; LFER benzimidazole NMR.

Substituent effects on the 1H and 13C NMR chem. shifts in 2-substituted benzimidazoles and their anions and cations were studied quant. The transmission of electron effects of substituents from C-2 to C-5(6) is approx. 20% less effective than in the opposite direction. The solvent effects on 1H chem. shifts and transmission effects in the charged forms of 2-substituted benzimidazoles were also studied.

Organic Magnetic Resonance published new progress about Linear free energy relationship. 5805-53-8 belongs to class imidazoles-derivatives, name is Methyl 1H-benzo[d]imidazole-2-carboxylate, and the molecular formula is C9H8N2O2, Application of Methyl 1H-benzo[d]imidazole-2-carboxylate.

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem