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64208

A NEW SCAFFOLD FOR D3 DOPAMINERGIC AFFINITY CONTAINING ARYLPIPERAZINE FRAGMENT: MOLECULAR MODELING, SYNTHESIS, IN VITRO AND IN VIVO PHARMACOLOGICAL EVALUATION

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Last updated: 04 Jan 2025

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Abstract

A new series of N-(6-substitutedbenzo[d]thiazol-2-yl)-2-(4-
arylpiperazin-1-yl) acetamides (3a-f) and 2-(3-(4-arylpiprazin-1-
yl)propylthio)benzo[d]thiazoles/-oxazoles/-imidazole (6a-f) was
synthesized by connecting arylpiperazine through a semi-rigid or
flexible spacer to a heterocyclic moiety, respectively. The
radioligand binding experiments for the D1, D2, D3 and D5 subtypes
expressed in CHO cells were examined for the target compounds
3a-f, 6a, 6b, 6d and 6f. Compound 6a showed the best binding
affinity for dopamine D3 receptor and is considered as a new
scaffold for D3 dopaminergic affinity. Furthermore, molecular
modeling of the best-fitted conformer of target compounds 3a, 6b,
6c, 6d and 6f to 
1-adrenoceptor ( 
1-AR) antagonist hypothesis
was performed using CATALYST software, HipHop modules. Based
on the results of simulation studies, these target compounds were
evaluated for their in vivo hypotensive activity on blood pressure of
normotensive cats.

DOI

10.21608/bfsa.2007.64208

Authors

First Name

Dalal

Last Name

Abou El Ella

MiddleName

A.

Affiliation

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, El-Khalifa El-Maamoon St., 11566, Abbassia, Cairo, Egypt

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Orcid

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First Name

Franziska

Last Name

U. Müller

MiddleName

K.

Affiliation

Biological Screening Units, Institute of Pharmacy, Philosophenweg 14, D-07743 Jena, Germany

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Orcid

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Volume

30

Article Issue

2

Related Issue

9610

Issue Date

2007-12-01

Receive Date

2007-11-17

Publish Date

2007-12-31

Page Start

259

Page End

273

Print ISSN

1110-0052

Online ISSN

3009-7703

Link

https://bpsa.journals.ekb.eg/article_64208.html

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https://bpsa.journals.ekb.eg/service?article_code=64208

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13

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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

A NEW SCAFFOLD FOR D3 DOPAMINERGIC AFFINITY CONTAINING ARYLPIPERAZINE FRAGMENT: MOLECULAR MODELING, SYNTHESIS, IN VITRO AND IN VIVO PHARMACOLOGICAL EVALUATION

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Article

Created At

22 Jan 2023