Metabolite Tales Blog

JULY 5, 2023

Previously natural products have provided the source of up to 90% of macrocyclic drugs, not surprising given that 20% of natural product derived ring systems are macrocyclic [2]. Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Chen et al.,

Drugs 52

Drugs Metabolic Stability FDA Approval Treatment 52

Metabolite Tales Blog

JULY 5, 2023

Previously natural products have provided the source of 80-90% of macrocyclic drugs, not surprising given that 20% of natural product derived ring systems are macrocyclic. [2] Not only this, the reduction in rotatable bonds and consequent reduction in susceptibility to metabolism is an additional benefit [4]. Chen et al.,

Metabolic Stability 52

Metabolic Stability Drugs FDA Approval Treatment 52

Metabolite Tales Blog

APRIL 4, 2023

Tapinarof (3,5-dihydroxy-4-isopropylstilbene) is actually a natural product which was found serendipitously when investigating the secondary metabolites of Photorhabdus luminescens , a bioluminescent, Gram-negative bacillus, which lives symbiotically within a soil-living entomopathogenic nematode. 8 This is not the only point of interest.

Small Molecule 52

Small Molecule FDA Approval FDA Drugs 52

Practical Cheminformatics

AUGUST 3, 2023

SIDER - A collection of 1,427 chemical structures with associated side effects divided into categories ranging from “Hepatobiliary disorders” and “Infections and infestations” to less scientific categories such as “Product issues”, “Investigations”, and “Social circumstances”. I have a few ideas.

Drugs 93

Drugs Biochemical Assays Metabolic Stability Screening Hits 93

Metabolite Tales Blog

MARCH 1, 2023

Bicyclic structures containing five membered rings such as indoles, consisting of a six-membered benzene ring fused to a five-membered pyrrole ring, are also increasingly relevant as growing research fields such as psychedelics make use of these scaffolds, often found in natural products.

Metabolic Stability 52

Metabolic Stability Drugs Pharmacokinetics Science 52

Drug Target Review

JANUARY 16, 2025

However, close to 40 percent of all macrocyclic drugs are orally bioavailable, 6 including natural products and derivatives thereof that have provided chemical structure clues with respect to permeability. Cyclic Peptide Design, Chapter 2: Strategies to Enhance Metabolic Stabilities. Pharmaceuticals , 16(7):996, 2023.

Drug Development 52

Drug Development Small Molecule Drugs FDA Approval 52