Conventional and Microwave‐Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase

Daniela  Secci; Adriana Bolasco; Melissa D'Ascenzio; Flavio Della Sala; Matilde Yáñez; Simone Carradori

doi:10.1002/jhet.1058

Conventional and Microwave‐Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase

Daniela Secci, Adriana Bolasco, Melissa D'Ascenzio, Flavio Della Sala, Matilde Yáñez, Simone Carradori

Research output: Contribution to journal › Article › peer-review

Abstract

A large series of 1,2‐diaryl‐benzimidazole and 2‐aryl‐1H‐benzimidazole derivatives were synthesized with slight differences using both microwave irradiation and conventional heating methods. Usually higher yields and time reactions reduction were obtained with the former method. All compounds were assayed for their in vitro ability to inhibit human cyclooxygenases, and most of them showed an encouraging inhibitory activity and isoform selectivity in the micromolar range.

Original language	English
Pages (from-to)	1187-1195
Journal	Journal of Heterocyclic Chemistry
Volume	49
Issue number	5
DOIs	https://doi.org/10.1002/jhet.1058
Publication status	Published - 29 Oct 2012
Externally published	Yes

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title = "Conventional and Microwave‐Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase",

abstract = "A large series of 1,2‐diaryl‐benzimidazole and 2‐aryl‐1H‐benzimidazole derivatives were synthesized with slight differences using both microwave irradiation and conventional heating methods. Usually higher yields and time reactions reduction were obtained with the former method. All compounds were assayed for their in vitro ability to inhibit human cyclooxygenases, and most of them showed an encouraging inhibitory activity and isoform selectivity in the micromolar range.",

author = "Daniela Secci and Adriana Bolasco and Melissa D'Ascenzio and {Della Sala}, Flavio and Matilde Y{\'a}{\~n}ez and Simone Carradori",

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T1 - Conventional and Microwave‐Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase

AU - Secci, Daniela

AU - Bolasco, Adriana

AU - D'Ascenzio, Melissa

AU - Della Sala, Flavio

AU - Yáñez, Matilde

AU - Carradori, Simone

PY - 2012/10/29

Y1 - 2012/10/29

N2 - A large series of 1,2‐diaryl‐benzimidazole and 2‐aryl‐1H‐benzimidazole derivatives were synthesized with slight differences using both microwave irradiation and conventional heating methods. Usually higher yields and time reactions reduction were obtained with the former method. All compounds were assayed for their in vitro ability to inhibit human cyclooxygenases, and most of them showed an encouraging inhibitory activity and isoform selectivity in the micromolar range.

AB - A large series of 1,2‐diaryl‐benzimidazole and 2‐aryl‐1H‐benzimidazole derivatives were synthesized with slight differences using both microwave irradiation and conventional heating methods. Usually higher yields and time reactions reduction were obtained with the former method. All compounds were assayed for their in vitro ability to inhibit human cyclooxygenases, and most of them showed an encouraging inhibitory activity and isoform selectivity in the micromolar range.

U2 - 10.1002/jhet.1058

DO - 10.1002/jhet.1058

M3 - Article

SN - 0022-152X

VL - 49

SP - 1187

EP - 1195

JO - Journal of Heterocyclic Chemistry

JF - Journal of Heterocyclic Chemistry

IS - 5

ER -

Conventional and Microwave‐Assisted Synthesis of Benzimidazole Derivatives and Their In Vitro Inhibition of Human Cyclooxygenase

Abstract

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