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70043

SYNTHESIS AND PRELIMINARY ALKYLATING ACTIVITIES OF CERTAIN NEW 1,4-DIHYDROPYRIDINES, PYRIDINIUM SALTS AND 2,7-DIAZABICYCLO [4.1.0] HEPT-3-ENES

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Last updated: 25 Dec 2024

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Abstract

3-Substituted-1-{2-chloro- or [2-bis (2-chloroethyl)amino]}ethyl-1,4-dihydropyridines 3 and 6 were prepared by reduction of the corresponding pyridinium chlorides 2 and 5 with sodium dithionite in alkaline medium. The l,3-dipolar cycloaddition of either phenylsulphonyl or p-tolylsulphonyl azides to the l,4-dihydropyridines 3 afforded the corresponding 2,7-diazabicyclo[4.1. 0]hept-3-enes 7. The alkylating activities of twelve new compounds (2b-d; 3b,c;  5a-c and 7a-d) were determined kinetically in comparison to chlorambucil as a reference drug. Compounds 5a-c showed higher activities than chlorambucil while 2c,d and 7a,b showed lower activities. The dihydropyridines (the CDS) 3b,c were inactive as alkylating agents as expected.

DOI

10.21608/bfsa.1993.70043

Authors

First Name

Hassan

Last Name

Farag

MiddleName

H.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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First Name

Abdel-Alim

Last Name

Abdel-Alim

MiddleName

M.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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Orcid

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First Name

Mahmoud

Last Name

El-Gendy

MiddleName

M.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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City

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Orcid

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First Name

Nawal

Last Name

El-Koussi

MiddleName

A.

Affiliation

Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut, Egypt

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Volume

16

Article Issue

2

Related Issue

10642

Issue Date

1993-12-01

Receive Date

1993-04-27

Publish Date

1993-12-31

Page Start

141

Page End

150

Print ISSN

1110-0052

Online ISSN

3009-7703

Article File

BFSA_Volume 16_Issue 2_Pages 141-150.pdf

PDF . 495.9kB

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https://bpsa.journals.ekb.eg/article_70043.html

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https://bpsa.journals.ekb.eg/service?article_code=70043

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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 AND PRELIMINARY ALKYLATING ACTIVITIES OF CERTAIN NEW 1,4-DIHYDROPYRIDINES, PYRIDINIUM SALTS AND 2,7-DIAZABICYCLO [4.1.0] HEPT-3-ENES

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Article

Created At

22 Jan 2023