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207161

SYNTHESIS, BIOLOGICAL EVALUATION AND IN SILICO ADME PREDICTIONS OF SOME NEW COUMARIN-ACETAMIDE DERIVATIVES AS POTENT ANTI-INFLAMMATORY AGENTS

Article

Last updated: 25 Dec 2024

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Abstract

A new series of 4-methyl-7-methoxycoumarin derivatives linked with three amide groups
were prepared starting from 2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy) acetohydrazide,
compound 4. TLC was used to ensure the purity of all new compounds, and IR, 1H NMR, and
mass spectrometry, as well as elemental microanalyses, were used to confirm their structures.
All of the target compounds were tested for anti-inflammatory activity. The results showed that
most of the tested compounds exhibited significant anti-inflammatory activity in comparison to
indomethacin (INM) as a reference drug. The results revealed that compound 8g was the most
active one exceeding the activity of the reference INM. Moreover, compounds 8f and 8k showed
approximately the same results as INM after 5 hr. In silico ADME prediction investigations also
forecasting the drug-like characters of these compounds .

DOI

10.21608/bfsa.2021.207161

Authors

First Name

Mohammed

Last Name

Elbastawesy

MiddleName

A. I.

Affiliation

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-azhar University, Assiut Branch 71524, Assiut, Egypt.

Email

mohamedali.pharm.ast@azhar.edu.eg

City

-

Orcid

0000-0002-3460-0667

First Name

Martha

Last Name

Morcoss

MiddleName

M.

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Nahda University, 62513 Beni-Suef, Egypt

Email

martha.moheb@nub.edu.eg

City

-

Orcid

-

First Name

Mostafa

Last Name

Abdelrahman

MiddleName

H.

Affiliation

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-azhar University, Assiut Branch 71524, Assiut, Egypt.

Email

-

City

-

Orcid

-

First Name

Bahaa

Last Name

Youssif

MiddleName

G.M.

Affiliation

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Assiut, Egypt

Email

-

City

-

Orcid

-

First Name

Alaa

Last Name

Hayallah

MiddleName

M.

Affiliation

Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Assiut, Egypt , Pharmaceutical Chemistry Department, Faculty of Pharmacy, Sphinx University, New Assiut, Egypt

Email

alaa_hayalah@yahoo.com

City

-

Orcid

0000-0001-9517-8650

Volume

44

Article Issue

2

Related Issue

29160

Issue Date

2021-12-01

Receive Date

2021-04-30

Publish Date

2021-12-01

Page Start

427

Page End

441

Print ISSN

1110-0052

Online ISSN

3009-7703

Link

https://bpsa.journals.ekb.eg/article_207161.html

Detail API

https://bpsa.journals.ekb.eg/service?article_code=207161

Order

14

Type

Original Article

Type Code

1,096

Publication Type

Journal

Publication Title

Bulletin of Pharmaceutical Sciences Assiut University

Publication Link

https://bpsa.journals.ekb.eg/

MainTitle

SYNTHESIS, BIOLOGICAL EVALUATION AND IN SILICO ADME PREDICTIONS OF SOME NEW COUMARIN-ACETAMIDE DERIVATIVES AS POTENT ANTI-INFLAMMATORY AGENTS

Details

Type

Article

Created At

22 Jan 2023