Synthesis of Neurotensin Mimics

Abstract

Aim of the synthesis of the analogs of the lead compound, i.e., mimic2 is structure. Activity Relationship studies. We focused our studies at two points: 1. To synthesize analog/s more potent than the mimic2. 2. To synthesize completely nonpeptide NT mimetics. In our present studies we were able to achieve both of these objectives. Mimic3 and 4 both are non-peptidic and found to be ten times more potent than the mimic2 (the lead compound). We also synthesized mimic5, which has methoxy group as substituent in the indole ring. Although its biological evaluation is still under investigation. However, we hope it would prove to be more potent than mimic3 and mimic4 because of the presence of methoxy group as substituent which is electron donating. It is well known fact that many biologically active natural products do have methoxy group/s in their structure. This work has been presented in the 10th National Science of Pakistan at Quaid e Azam University, Islamabad. (October 22- October 26, 1999) and also in 8th International Symposium on Natural Products held in Karachi (January 18-January 22, 2000). Financial grant of Pakistan Science foundation for this project was duly acknowledged.