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167348

SYNTHESIS OF SOME NOVEL PYRROLE AND PYRROLO|2,3-dPYRIMIDINE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS.

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Last updated: 22 Jan 2023

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Abstract

Some novel pyrrole and pyrrolo2,3-dpyrimidine derivatives were synthesized and evaluated tor their anti –inflammatory activities. 2-(4-Substitutedphenylamino)-1-(4-substitutedphenyl) ethanones (3a-i) were reacted either with malononitrile or ethyl Cyanoacetate  to afford 2-amino-1,4-disubsututedphenyl-1H-pyrrole-3-carbonitriles (4a-i) disubstitutedphenyl-tH-pyrrole-3-carboxylates (5a-g) respectively. Compounds (4a, 4i and 5g) were reacted with acetic anhydride, benzoyl chloride, 4 substitutedphenacyl bromides and benzyl chloride to afford compounds (6a-c), (7a-c), (8a-c) and (9a-c) respectively.Compounds (4a and 4i) were also reacted either with formic acid or triethyl orthoformate to give 5-(4- substitutedphenyi)-7-(4 substitutedpheny)-3H-pyrrolof(2,3-d)  pyrimdin-4(7H)-ones (10a,b) and ethy1 N-1,4-disubstitutedphenyl-3-cyano-1H-pyrTol-2-yt-formimidates (1Ha,b) respectively. FHydrazinotysis of (11a,b) afforded (12a,b).
Sixteen of the newly synthestzed compounds were evaluated for their anti-inflammatory and analgesic activities. Most of the screened compounds showed intcresting high anti-inflammatory activity compared to ketoprofen (Biprofened®) as a standard drug The most active compoutnds were further screened for ther ulcerogenic activity. The analgesic activity of the selected compounds was also assessed.

DOI

10.21608/zjps.2011.167348

Authors

First Name

Makarem

Last Name

Korra

MiddleName

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Affiliation

Department of Organic Chemistry, Faculty of Pharmacy, Cairo University.

Email

makarem.korra@yahoo.com

City

-

Orcid

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First Name

Maha

Last Name

Khalifa

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry. Faculty of Pharmacy (girls branch), Al-Azhar University

Email

maha.khalifa@yahoo.com

City

-

Orcid

-

First Name

Hend

Last Name

EL-Sahrawi

MiddleName

-

Affiliation

Department of Pharmaceutical Chemistry. Faculty of Pharmacy (girls branch), Al-Azhar University

Email

hend.el-sahrawi@yahoo.com

City

-

Orcid

-

First Name

Marwa

Last Name

Sarg

MiddleName

-

Affiliation

Department of Organic Chemistry, Faculty of Pharmacy (girls branch), Al-Azhar University

Email

marwa.sarg@yahoo.com

City

-

Orcid

-

First Name

Shaimaa

Last Name

Abd El-Gilil

MiddleName

-

Affiliation

Department of Organic Chemistry, Faculty of Pharmacy (girls branch), Al-Azhar University

Email

shaimaa.abd-el-gilil@yahoo.com

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Orcid

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Volume

20

Article Issue

2

Related Issue

23545

Issue Date

2011-12-01

Receive Date

2011-07-03

Publish Date

2011-12-01

Page Start

6

Page End

18

Print ISSN

1110-5089

Online ISSN

2356-9786

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https://zjps.journals.ekb.eg/article_167348.html

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https://zjps.journals.ekb.eg/service?article_code=167348

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2

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Original Article

Type Code

862

Publication Type

Journal

Publication Title

Zagazig Journal of Pharmaceutical Sciences

Publication Link

https://zjps.journals.ekb.eg/

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Article

Created At

22 Jan 2023