Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa

Mederski, Werner W. K. R.; Dorsch, Dieter; Anzali, Soheila; Gleitz, Johannes; Cezanne, Bertram; Tsaklakidis, Christos

doi:10.1016/j.bmcl.2004.04.097

Cited by 78 publications

(37 citation statements)

References 10 publications

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“…All analys is of compounds (21,22,24) are consistent with the proposed structures. The site selectivity in cycloaddition of some nitrogen amb ident nucleophiles with enaminonitrile (6) was also investigate, Thus, reaction of (6) with thiourea in reflu xing ethanol containing catalytic amount of piperid ine afforded a single product for which five isomeric cycloadducts (27), (29),(31),(33) and (35) seemed possible. However, the pyrimidinethione (35) was assigned for the react ion product on its analysis.…”

Section: Chemistrymentioning

confidence: 99%

“…It was interesting to synthesis hybrids possessing biological and pharmacological activit ies due to benzimidazo le [16][17][18][19][20][21][22][23][24][25][26][27][28][29] and certain substituted pyrazoles [30][31][32][33][34][35][36][37][38][39][40][41][42][43][44] hoping that this combination may possess a potential analgesic activity along with possible anticancer effect.…”

Section: Introductionmentioning

confidence: 99%

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Heterocyclic Synthesis Via Enaminonitriles: One-Pot Synthesis of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-A]Pyrimidine and Pyrido[2,3-D]Pyrimidine Derivatives

Khalil¹,

Sayed²,

Raslan³

2012

AJOC

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A simple route for the synthesis of 5-aminopyrazole derivatives (9) was described through the readily accessible acrylamide derivative (7). Reaction of the aminopyrazole with different reagents such as ,-unsaturated nitriles affo rded pyrazol[1,5-a]pyrimid ine (13,15,18). The structure of the enaminonitrile (6) was studied with different reagents such as thiourea and 2-thio xo-(1H)-pyrimid ine-4-one (36) afforded pyrimid inethione derivative (35) and the pyrido[2,3-d]pyrimidi ne derivative (41), respectively.

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Section: Chemistrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Heterocyclic Synthesis Via Enaminonitriles: One-Pot Synthesis of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-A]Pyrimidine and Pyrido[2,3-D]Pyrimidine Derivatives

Khalil¹,

Sayed²,

Raslan³

2012

AJOC

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“…Imidazole ring is an important pharmacophore in drug discovery. Extensive biochemical and pharmacological studies have confirmed that imidazole molecule is associated with a wide range of biological activities including anticancer [8,9], antibacterial [10], antifungal [11], antioxidant [12], antihypertensive [13] and anticoagulant [14], properties. In recent years, there have been important applications of azo dye was permeate into the field of electronic industry as a strong components in the DVD-R (digital versatile disc-recordable) because of its characteristic as stable metal azo dyes.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Spectral, Thermal and Biological Studies of Some Metal Complexes Derived from Heterocyclic Mono Azo Dye Ligand 2'[(2'-Hydroxy-4-methyl phenyl)azo]imidazole

Al-Adilee¹,

Atyha²

2018

Asian J. Chem.

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Asian Journal of Chemistry; Vol. 30, No. 2 (2018), 280-292 in the azo dyes compounds, such as hydroxyl, carboxylic acid, halogens, esters and amines [19,20]. An important uses of azo imidazole compounds used analytical reagents for solvent extraction to determination of some metal ions [21,22]. The heterocyclic azo imidazole compounds have important role in spectral determination field to determine the trace amount of elements especially transition metal ions and heavy metals because of high sensitivity and selectivity [23,24].The present work describes the synthesis and spectral characterizations of 2'[2'-(1-hydroxy-4-methyl phenyl)azo]-imidazole (HMePAI = HL), containing phenolic-OH function and imidazole moiety. The heterocyclic mono azo dye ligand and its metal complexes were studied by various spectral analysis and screened for their biological activities. As well as the study of ligand and Ni(II) complex of prescription drug anticancer by using the lines of cancerous liver cells of the type HePG2 and compared with line of the ordinary cells.

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“…1 Benzimidazole derivatives are structural isosteres of naturally occurring nucleotides, which allows them to interact easily with the biopolymers of the living systems. Therefore, benzimidazole derivatives have shown different therapeutic properties such as antiulcer, 2 antihelminthic, 3 antihypertensive, 4 anticoagulant, 5 antiallergic, 6 analgesic, 7 anti-inflammatory, 8 antimicrobial, 9 antiviral, 10 antiparasitic, 11 and antioxidant.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

Wubulikasimu¹,

Yang²,

Xue³

et al. 2013

Bulletin of the Korean Chemical Society

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A series of novel benzimidazole derivatives bearing a heterocyclic ring as oxadiazole (21-32), thiadiazole (33-34), triazole (35-36) were synthesized and evaluated for their activities against Coxsackie virus B3 and B6 in Vero cells. Compounds 21-26, 31-36 with moieties of 2'-pyridyl, 3'-pyridyl and 4'-pyridyl at the 2-position and oxadiazoles, thiadiazole, or triazole substituent at the 4-or 5-position generally displayed activities against CVB3 and CVB6. Especially compound 24 (IC 50 = 1.08 µg/mL, SI = 61.7 against CVB3) was the promising candidate as lead compound for anti-enteroviral drug. It was observed in the incorporation of heterocyclic rings in benzimidazole at the 5-position could enhance their biological activities.

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Halothiophene benzimidazoles as P1 surrogates of inhibitors of blood coagulation factor Xa

Cited by 78 publications

References 10 publications

Heterocyclic Synthesis Via Enaminonitriles: One-Pot Synthesis of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-A]Pyrimidine and Pyrido[2,3-D]Pyrimidine Derivatives

Heterocyclic Synthesis Via Enaminonitriles: One-Pot Synthesis of Some New Pyrazole, Pyrimidine, Pyrazolo[1,5-A]Pyrimidine and Pyrido[2,3-D]Pyrimidine Derivatives

Synthesis, Spectral, Thermal and Biological Studies of Some Metal Complexes Derived from Heterocyclic Mono Azo Dye Ligand 2'[(2'-Hydroxy-4-methyl phenyl)azo]imidazole

Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position

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