Biological activity | An-Najah Staff

Biological activity

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‎1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine ‎Derivatives as Highly Potent and Selective Human A(2B) ‎Adenosine Receptor Antagonists

Tue, 2014-07-01 09:49 — Abdel Naser Zaid

Journal Title, Volume, Page:

Bioorg Med Chem.;16(5):2419-30. Epub 2007 Nov 28.

Year of Publication:

2008

Link:

http://www.sciencedirect.com/science/article/pii/S0968089607010279

Authors:

Abdel Naser Zaid

College of Pharmacy, An-Najah National University, Nablus, Palestine

Current Affiliation:

Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine

[email protected]

Mojgan Aghazadeh Tabrizi

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Pier Giovanni Baraldi

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Delia Preti

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Romeo Romagnoli

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Giulia Saponaro

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Stefania Baraldi

Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy

Allan R. Moorman

King Pharmaceuticals, Inc., Research and Development, 4000 CentreGreen Way, Suite 300, Cary, North Carolina 27513, Italy

Katia Varani

Dipartimento di Medicina Clinica e Sperimentale-Sezione di Farmacologia, Università di Ferrara, 44100 Ferrara, Italy

Pier Andrea Borea

Dipartimento di Medicina Clinica e Sperimentale-Sezione di Farmacologia, Università di Ferrara, 44100 Ferrara, Italy

Preferred Abstract (Original):

A new series of 1,3-dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives has been identified as potent A(2B) adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A(2B), A(1), A(2A), and A(3) adenosine receptors. N-(4-chloro-phenyl)-2-[3-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-5-methyl-pyrazol-1-yl] (11c) showed a high affinity for the human A(2B) adenosine receptor K(i)=7nM and good selectivity (A(1), A(2A), A(3)/A(2B)>140). Synthesis and SAR of this novel class of compounds is presented herein.

warad's picture

Characterization and Biological Activities of Two Copper(II) Complexes with ‎Dipropylenetriamine and Diamine as Ligands

Fri, 2014-03-14 22:48 — Ismail Warad

Journal Title, Volume, Page:

Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 127 (2014) 225–230

Year of Publication:

2014

Link:

http://www.sciencedirect.com/science/article/pii/S1386142514002030

Authors:

Ismail Warad

Department of Chemistry, An-Najah National University, P.O. Box 7, Nablus, Palestine

Current Affiliation:

Department of Chemistry, An-Najah National University, P.O. Box 7, Nablus, Palestine

[email protected]

Mousa AL-Noaimi

Department of Chemistry, Hashemite University, P.O. Box 150459, Zarqa 13115, Jordan

Mohammad I. Choudhary

Department of Chemistry, Science College, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia

Firas F. Awwadi

Chemistry Department, Faculty of Science, The University of Jordan, Amman 11942, Jordan

Wamidh H. Talib

Department of Clinical Pharmacy and Therapeutics, Applied Science University, Amman 11931, Jordan

Taibi Ben Hadda

Laboratoire LCM, Faculty of Sciences, University Mohammed 1, Oujda 60000, Morocco

Sammer Yousuf

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan

Ashraf Sawafta

Biology and Biotechnology Department, AN-Najah National University, P.O. Box 7, Nablus, Palestine

Preferred Abstract (Original):

Two new mixed-ligand copper(II) complexes, [Cu(dipn)(N single bond N)]Br₂(1–2) [dipn = dipropylenetriamine, NN = ethylenediamine (en) (1) and propylenediamine (pn) (2)], have been synthesized. These complexes were characterized by spectroscopic and thermal techniques. Crystal structure for 2 shows a distorted trigonal–bipyramidal geometry around Cu(II) ion with one solvate water molecule. Antimicrobial and antiproliferative assays were conducted to evaluate the biological activities of these complexes. The complexes exhibit a promising antimicrobial effect against an array of microbes at 200 μg/mL concentration. The antiproliferative assay shows a high potential of these complexes to target Human keratinocyte cell line with IC₅₀ values of 155 and 152 μM. The absorption spectrum of 2 in water was modeled by time-dependent density functional theory (TD-DFT).