We report a concise synthesis of N-acylated piperidines through a Knoevenagel-Doebner condensation/amide construction/ amination sequence. The design of the piperidines considered the pharmacophoric features found in previously reported inhibitors of FabI, an enzyme implicated in bacterial fatty acid biosynthesis. After the microbiological evaluation at 50 μM, the analogs displayed moderate activity against some pathogens from the ESKAPE group, reaching up to 42 % of growth inhibition for MRSA, 54 % for K.
View Article and Find Full Text PDFEthnopharmacological Relevance: The Yucatan Peninsula has a privileged wealth of vascular plants with which various Mayan herbal formulations have been developed. However, studies on their antipathogenic and antivirulence properties are scarce.
Aim Of The Study: Identify antivirulence properties in Mayan herbal remedies and determine their antipathogenic capacity in burn wounds infected with Pseudomonas aeruginosa.
We prepared a series of cinnamoyl-containing furanones by an affordable and short synthesis. The nineteen compounds hold a variety of substituents including electron-donating, electron-withdrawing, bulky and meta-substituted phenyls, as well as heterocyclic rings. Compounds showed antibiofilm activity in S.
View Article and Find Full Text PDFJ Ethnopharmacol
January 2024
Ethnopharmacological Relevance: Cuachalalate (Amphipterygium adstringens) stem bark has been used to heal wounds and counteract microbial infections since pre-Hispanic times. However, its effect in treating infected burns remains unclear.
Study Objectives: To determine the antipathogenic capacity of a folk remedy (FR) containing cuachalalate stem bark to treat lesions caused by thermal damage and bacterial infection.
Blocking virulence is a promising alternative to counteract infections. In this regard, the phenomenon of cell-cell communication by quorum sensing (QS) is an important anti-virulence target. In this field, fatty acids (FA) have gained notoriety for their role as autoinducers, as well as anti-virulence molecules , like some saturated FA (SAFA).
View Article and Find Full Text PDFCalmodulin (CaM) plays a central role in regulating a myriad of cellular functions in physiological and pathophysiological processes, thus representing an important drug target. In previous reviews, our group has reported relevant information regarding natural anti-CaM compounds up to 2009. Natural sources continue to provide a diverse and unique reservoir of CaM inhibitors for drug and research tool discovery.
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