Name: Dipak Harel
Diploma / M.Sc degree: University of Pune, India
(June 2006)

PhD Project: Synthesis and antileishmanial activity of chromenes derived from natural product


Homepage: http://www.uni-muenster.de/Chemie.pz/forschen/ag/wuensch/mitarbeiter/index.html

Abstract of Research Project

Leishmaniasis is a vector-born parasitic disease of the tropics and sub- tropics which is manifested in four major clinical forms (cutaneous, mucocutaneous, visceral and post kala azar dermal leishmaniasis) with approximately two million new cases every year and one tenth of the world's population at risk of infection. The disease is endemic throughout parts of Europe, North Africa, the middle east and central and South America and occurs in epidemics with high mortality in East Africa and parts of the Indian subcontinent.

Leishmania is exclusively transmitted to humans by the female Phaebotomus sandfly. Unfortunately, there are no effective vaccines against the parasite yet. Thus, control of disease relies primarily on chemical treatment. Recently, methoxylated flavonoids and chromene derivatives are isolated from Ageratum conyzoides L. (Asteraceae) showed moderate antiprotozoal activity.

Chromenes belong to a large class of molecules known as benzopyrans and the chromene moiety is an integral part of many natural products. In order to find a new drug with more potent activity against Leishmania parasites, we are engaged in a program to synthesize and investigate some new synthetic compounds based on naturally occurring potent chromene derivatives.


Publications

D. Harel, D. Schepmann, H. Prinz, R. Brun, T. J. Schmidt, B. Wünsch
Antiprotozoal agents derived from the natural product encecalol angelate: Synthesis, biological evaluation and structure activity relationship of chromene derivatives
Journal of Medicinal Chemistry 56 (2013), 7442-7448.

D. Harel, D. Schepmann, R. Brun, T. J. Schmidt, B. Wünsch
Enantioselective synthesis of encecaline-derived potent antimalarial agents
Organic & Biomolecular Chemistry 11 (2013), 7342–7349.

D. Harel, D. Schepmann, B. Wünsch
Combination of two σ1 ligands: Synthesis and σ receptor affinity of aminoethyl substituted benzothiophenes
European Journal of Medicinal chemistry 69 (2013), 490-497.

D. Harel, S. A. Khalid, M. Kaiser, R. Brun, B. Wünsch, T. J. Schmidt
Encecalol angelate, an unstable chromene from Ageratum conyzoides L.: Total Synthesis and Investigation of its Antiprotozoal Activity
J. Ethnopharm. 137 (2011), 620-625.


Dipak Harel
eMail: Dipak Harel