Design, Synthesis and Antifungal/Insecticidal Evaluation of Novel Cinnamide Derivatives

Abstract

Twenty novel cinnamamide derivatives were designed and synthesized using as lead compound pyrimorph, whose morpholine moiety was replaced by β-phenylethylamine. All the compounds were characterized by their spectroscopic data. The fungicidal and insecticidal activities were also evaluated. The preliminary results showed that all the title compounds had certain fungicidal activities against seven plant pathogens at a concentration of 50 μg/mL, and compounds 11a and 11l showed inhibition ratios of up to 90% against R. solani. Most of the title compounds exhibited moderate nematicidal activities. In general, the morpholine ring may be replaced by other amines and a chlorine atom in the pyridine ring is helpful to fungicidal activity.

Syntheses, characterization, and anti-cancer activities of pyridine-amide based compounds containing appended phenol or catechol groups

“…Amide-based molecules are considered to be suitable for drug research due to their biological compatibility. Development of new amide derivatives has been actively persuaded due to their potent application in vast biological activities, such as fungicidal, [1][2][3][4] herbicidal, [5][6][7][8] insecticidal, 9,10 anti-cancer, 11,12 and antibacterial, 13 etc. In this context, derivatives of pyridinecarboxamide are reported to show important analgesic, anti-inflammatory and anti-pyretic activities.…”

Ethyl Cinnamate Derivatives as Promising High-Efficient Acaricides against <i>Psoroptes cuniculi</i>: Synthesis, Bioactivity and Structure–Activity Relationship

“…36) Especially, what interests us is that cinnamic acid derivatives also have significant antiparasitic activities on plasmodia, 37) Leishmania 38) and nematode. 39) Furthermore, the acaricidal activity of ethyl cinnamate 40) and trans-cinnamaldehyde 41) as an analogue of cinnamic acid were reported as well. Thus, cinnamic acid derivatives are often used as promising starting compounds for the development of new, highly effective drugs.…”

“…Our interest in the excellent antiparasitic activities [37][38][39][40][41] and the low toxicity 11,12) of cinnamic acid derivatives prompted us to explore their acaricidal activity and extend their pharmacologic activities. This investigation presented the preparation of a series of cinnamic acid ester derivatives and evaluation of their acaricidal activity against P. cuniculi as well as the discussion of their preliminary SAR.…”

Synthesis and Characterization of Novel Cinnamamide Deriverties and Their Antimicrobial Activities

“…Such as medicinal, pharmaceuticals, agricultural, biological [1] and many other activities. In medicinal field several Cinnamamides and their derivatives are reported to show central nervous system depressant, anticonvulsant [2] , muscle relaxant, antiallergic, antineoplastic, antitumor, anesthetic, analgesic and anti-infective activities [3][4][5][6][7] , etc. In the agrochemical field, insecticidal, their avian repellent, herbicidal activities, and several excellent cinnamamide fungicides [8][9] for example dimethomorph, fluormorph and pyrimorph, have been successfully developed.…”