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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Synthesis and Herbicidal Activities of Novel Thiazole PPO Inhibitors

Author(s): Shu Chen, Guihua Ren, Dan Pei, Fan Zhang, Jie Liu, Donglin Zhang, Ren Yang, Jianjun Shi, Tianming Xu and Chengxia Tan*

Volume 17, Issue 2, 2020

Page: [192 - 198] Pages: 7

DOI: 10.2174/1570180816666190329221521

Price: $65

Abstract

Background: Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is a key enzyme in the biosynthesis of chlorophyll and heme, also the target of different types of herbicides. Thiazole compounds shown excellent biological activity, can be designed by using active groups docking for new PPO inhibitors.

Objective: The objective of this study was to synthsize a series of aryl thiazole compounds as PPO inhibitors.

Methods: In this study, a series of aryl thiazole compounds derivatives 11a-l were obtained from 2- chloro-5-nitrobenzoic acid as the starting material via esterification, Iron powder reduction, diazotization, Hantzsch reaction and final acylation. All synthesized compounds have been tested for their herbicidal activities as a PPO inhibitors.

Results: The Petri dish test indicated that all compounds exhibited good herbicidal activities at 200 mg/L using culture dish. And the post-emergence tests showed that at 150g.ai/ha on weed stem leaf spray treatment, some of the title compounds exhibited 80% inhibition rate against the dicotyledonou weeds Amaranthus retroflexus and Eclipta prostrate.

Conclusion: Good activity was noted for some compounds that compounds 11a, 11b, 11c, 11g, 11h had 80% inhibition on stems and leaves of Amaranthus retroflexus at 150g.ai/ha.

Keywords: Thiazole, PPO, inhibitors, herbicidal activity, amaranthus retroflexus, eclipta prostrate.

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