155030-66-3

Upstream product

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• 153052-69-8 (2R)-1-(benzyloxy)-1-oxopropan-2-yl (2S)-4-methyl-2-(methylamino)pentanoate 
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• 53363-89-6 N-t-butoxycarbonyl-N-methyl-L-leucine 
• 154733-50-3 (R)-benzyl 3-(4-aminophenyl)-2-hydroxypropanoate 
• 68671-47-6 p-nitrophenyl-D-lactic acid 

Relevant academic research and scientific papers

METHODS FOR PRODUCTION OF PF1022A DERIVATIVES AND FLOW PLATFORMS USEFUL FOR THE SAME

Provided herein are improved methods of producing a derivative of PF1022A, for example a compound of Formula I: Formula I wherein R1 and R2 are each independently hydrogen or nitro, and at least one of R1 and R2

ENDOPARASITIC DEPSIPEPTIDES

The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof wherein each of R1, R2, R3, R4, L1, and L2 are as defined herein. The present invention also contemplates compositions, methods of treatment, and uses as a medicament to treat an animal for an endoparasitic infection with a Formula (1 ) compound.

ENDOPARASITIC DEPSIPEPTIDES

The present invention provides cyclic depsipeptides of Formula (1), stereoisomers thereof, and veterinary acceptable salts thereof (1) wherein each of R1, R2, R3, R4, L1, and L2, are as defined herein. The present invention also contemplates compositions and methods of treatment as an endoparasiticide with a Formula (1) compound.

New heteroaromatic derivatives of the anthelmintic cyclooctadepsipeptide PF1022A by click-chemistry

The cyclooctadepsipeptide PF1022A (1) and its semisynthetic, commercial analogue emodepside (2) have been established as excellent anthelmintics with resistance breaking properties. For a second generation anthelmintic cyclooctadepsipeptide with improved

Structure-activity relationship of anthelmintic cyclooctadepsipeptides

The relationship between cyclooctadepsipeptides and their anthelmintic efficacy was examined by converting the natural products, PF1022A, PF1022E and PF1022H. Some analoguessubstituted at the para position of the phenyllactate moiety showed higher or equivalent activity against the parasitic nematode, Ascaridia galli in chicken when compared with the parent compounds. It is suggested that lipophilicity and the polar surface area, in addition to structural requirements of the derivatives, influenced the anthelmintic efficacyin vivo.