Antithrombotic drugs market

Chaudhari, Kritika; Hamad, Bashar; Syed, Basharut A.

doi:10.1038/nrd4365

Cited by 29 publications

(27 citation statements)

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“…[1][2]-methyl]-1-methyl-1H-benzoimidazole-5-carbonyl}-(3-chloro-4-uoro-phenyl)-amino]propionic acid ethyl ester (9a). [1][2]-methyl]-1-methyl-1H-benzoimidazole-5-carbonyl}-(3-chloro-4-uoro-phenyl)-amino]propionic acid ethyl ester (9a).…”

Section: -((3-chloro-4-uoro-phenyl)-{2-[(4-cyano-phenylamino)mentioning

confidence: 99%

“…1 Arterial and venous thrombotic events are major causes of CVDs. According to the World Health Organization, CVD mortality may be expected to reach about 25 million by 2030.…”

Section: Introductionmentioning

confidence: 99%

“…mp 113-115 C;1 H NMR (500 MHz, DMSO-d 6 ) d (ppm) 7.64 (dd, J ¼ 6.9 Hz, J ¼ 2.3 Hz, 1H), 7.57 (s, 1H), 7.49 (d, J ¼ 8.6 Hz, 2H), 7.42 (t, J ¼ 9.1 Hz, 1H), 7.37 (t, J ¼ 5.1 Hz, 1H), 7.20 (d, J ¼ 5.1 Hz, 1H), 7.16-7.11 (m, 1H), 6.86 (d, J ¼ 8.6 Hz, 2H), 4.94- 8b was obtained in 83% yield as brown solid.…”

mentioning

confidence: 99%

“…mp 119-121 C;1 H NMR (500 MHz, CDCl 3 ) d (ppm) 7.69 (s, 1H), 7.39 (d, J ¼ 8.5 Hz, 1H), 7.34 (d, J ¼ 8.1 Hz, 1H), 7.31 (d, J ¼ 8.6 Hz, 1H), 7.26 (d, J ¼ 7.7 Hz, 1H), 7.23 (d, J ¼ 6.0 Hz, 1H), 6.98 (d, J ¼ 6.2 Hz, 2H), 6.83 (t, J ¼ 8.4 Hz, 1H), 4.68-4.64 (m, 1H), 4.58(d, J ¼ 4.3 Hz, 2H), 4.20 (t, J ¼ 7.0 Hz, 2H), 4.11 (q, J ¼ 7.1 Hz, 2H), 2.73 (t, J ¼ 7.0 Hz, 2H), 1.63 (d, J ¼ 6.8 Hz, 6H), 1.25 (t, J ¼ 7.2 Hz,3H); ESI-HRMS: calcd for C 30 H 29 ClF 2 -N 5 O 3 [M + H] + , 580.1922, found 580.1916, C 30 H 28 ClF 2 N 5 O 3 Na, [M + Na] + , 602.1741, found 602.1724. 8m was obtained in 80% yield as brown solid.…”

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confidence: 99%

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Design, synthesis, biological evaluation and molecular docking of novel dabigatran derivatives as potential thrombin inhibitors

Dong

Ren

et al. 2015

RSC Adv.

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A series of dabigatran derivatives were designed and synthesized to discover effective thrombin inhibitors.All the target compounds were characterized by 1 H NMR, 13 C NMR and HRMS. These compounds were evaluated in vitro and showed potent anticoagulant activities against thrombin. Among these compounds, the ethyl group substitution at N-1 of benzimidazole exhibited better anticoagulant activity against thrombin. Especially, compound 10i showed an IC 50 of 2.04 nM. Docking simulations demonstrated that compound 10i could bind tightly with the crystal structure of the thrombin active site.Based on the results obtained, compound 10i may act as a candidate compound for further development of direct thrombin inhibitors.

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Section: -((3-chloro-4-uoro-phenyl)-{2-[(4-cyano-phenylamino)mentioning

confidence: 99%

“…1 Arterial and venous thrombotic events are major causes of CVDs. According to the World Health Organization, CVD mortality may be expected to reach about 25 million by 2030.…”

Section: Introductionmentioning

confidence: 99%

mentioning

confidence: 99%

mentioning

confidence: 99%

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Design, synthesis, biological evaluation and molecular docking of novel dabigatran derivatives as potential thrombin inhibitors

Dong

Ren

et al. 2015

RSC Adv.

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“…Thrombin and factor Xa (FXa) are two key enzymes of the blood coagulation cascade, and inhibitors targeting these two enzymes have excellent potential as potent anticoagulant therapeutics. 3 In search for novel anticoagulants with superior benefits, numerous exogenous molecules have been purified and characterized from natural sources. 4 High-resolution screening (HRS) techniques in which separation methods are coupled to bioassays that eliminate traditional, labor-intensive purification and screening tasks, as well as facilitate rapid identification of active compounds from complex mixtures, are becoming increasingly popular.…”

Section: Introductionmentioning

confidence: 99%

Microfluidic Chip–Based Online Screening Coupled to Mass Spectrometry

Kool

et al. 2016

SLAS Discovery

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Thrombin and factor Xa (FXa) are critical enzymes of the blood coagulation cascade and are excellent targets of anticoagulant agents. Natural sources present an array of anticoagulants that can be developed as antithrombotic drugs. High-resolution, online screening techniques have been developed for the identification of drug leads from complex mixtures. In this study, we have developed and optimized a microfluidic online screening technique coupled to nano-liquid chromatography (LC) and in parallel with a mass spectrometer for the identification of thrombin and FXa inhibitors in mixtures. Inhibitors eluting from the nano-LC were split postcolumn in a 1:1 ratio; half was fed into a mass spectrometer (where its mass is detected), and the other half was fed into a microfluidic chip (which acts as a microreactor for the online assays). With our platform, thrombin and FXa inhibitors were detected in the assay in parallel with their mass identification. These methods are suitable for the identification of inhibitors from sample amounts as low as sub-microliter volumes.

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The medicinal panorama of benzimidazoles and their scaffolds as anticancer and antithrombotic agents: A review

Chalkappa,

Aralihalli,

Sudileti

et al. 2023

Archiv der Pharmazie

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Nitrogen‐containing heterocyclic scaffolds have become a prospective pharmacophore with therapeutic importance due to their biological similarities with natural and synthetic drugs. Among all nitrogen heterocyclic compounds, benzimidazoles and their derivatives are privileged molecules structurally akin to naturally available nucleotides, enabling them to intercommunicate with numerous biopolymers in biological systems. This reason enlightens modern researchers worldwide to assess their potential significance in the context of synthetic and biological chemistry. Therefore, it is crucial to merge the latest data with the prior documentation to apprehend the ongoing situation of the benzimidazole moiety in various therapeutic zones of research. The current work displays that the benzimidazole center is a versatile nucleus that offers the necessary data of synthetic alterations for pre‐existing compounds to provide new scaffolds to resist numerous therapeutic sectors, including those associated with anticancer and antithrombosis. Due to the potential significance of benzimidazoles, this review aims to emphasize the latest innovations in synthesizing several other notable benzimidazole substrates and their significant pharmacological prospects for the future, including anticancer and antithrombosis.

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Antithrombotic drugs market

Cited by 29 publications

References 0 publications

Design, synthesis, biological evaluation and molecular docking of novel dabigatran derivatives as potential thrombin inhibitors

Design, synthesis, biological evaluation and molecular docking of novel dabigatran derivatives as potential thrombin inhibitors

Microfluidic Chip–Based Online Screening Coupled to Mass Spectrometry

The medicinal panorama of benzimidazoles and their scaffolds as anticancer and antithrombotic agents: A review

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