NEW PHENOTHIAZINE DERIVATIVE DESIGNED ACCORDING TO LIPINSKI’S RULE OF FIVE AND ITS VARIANTS
Bint-e-Haider, Muhammad Qaiser, Hafsa Faizi
Faculty of Pharmacy, University of Sargodha, Sargodha 40100 Pakistan
Keywords: Drug designing, Therapeutic derivative, Phenothiazine
Abstract

Some of the new 10H phenothiazine derivatives had been synthesized for their anti psychotic activity as dopamine antagonists. They had been synthesized with the help of software Marvin sketch. 10 parameters were analyzed for each of them which could make them drug like molecule. All parameters were found to be within range. Newly designed structures justify all the aspects of anti psychotic activity by satisfying Lipinski’s Rule. Three carbon distance from two amine atoms keeps the polar surface area within range (>10). Log P value and conformational energy of these derivatives shows that they are structurally constrained molecules. They have also satisfied the stereo chemistry and hence safer derivatives. The limit for total numbers of atoms and H-bond donor and Acceptor are also seem to be fulfilled. So these derivatives have maximum chances that they could be drug like molecules which may have valuable anti psychotic activity. They could be investigated further for clinical use in conditions like schizophrenia, mania and other psychotic disorders.

Article Information

Identifiers and Pagination:
Year:2013
Volume:5
First Page:34
Last Page:40
Publisher Id:JAppPharm (2013 ). 5. 34-40
Article History:
Received:February 17, 2013
Accepted:March 25, 2013
Collection year:2013
First Published:April 1, 2013


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Prof. Dr. Cornelia M. Keck (Philipps-Universität Marburg)
Marburg, Germany

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Welcome to the research group of Prof. Dr. Cornelia M. Keck in Marburg. Cornelia M. Keck is a pharmacist and obtained her PhD in 2006 from the Freie Universität (FU) in Berlin. In 2009 she was appointed as Adjunct Professor for Pharmaceutical and Nutritional Nanotechnology at the University Putra Malaysia (UPM) and in 2011 she obtained her Venia legendi (Habilitation) at the Freie Universität Berlin and was appointed as a Professor for Pharmacology and Pharmaceutics at the University of Applied Sciences Kaiserslautern. Since 2016 she is Professor of Pharmaceutics and Biopharmaceutics at the Philipps-Universität Marburg. Her field of research is the development and characterization of innovative nanocarriers for improved delivery of poorly soluble actives for healthcare and cosmetics. Prof. Keck is executive board member of the German Association of Nanotechnology (Deutscher Verband Nanotechnologie), Vize-chairman of the unit „Dermocosmetics“ at the German Society of Dermopharmacy, active member in many pharmaceutical societies and member of the BfR Committee for Cosmetics at the Federal Institute for Risk Assessment (BfR).

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