https://pubs.rsc.org/en/content/articlepdf/2019/NP/C8NP00092A

Marine natural products.

Over the past decade, the most significant, conceptual advances in the field of fluorination were enabled most prominently by organo- and transition-metal catalysis. The most challenging transformation remains the formation of the parent C-F bond, primarily as a consequence of the high hydration energy of fluoride, strong metal-fluorine bonds, and highly polarized bonds to fluorine. Most fluorination reactions still lack generality, predictability, and cost-efficiency. Despite all current limitations, modern fluorination methods have made fluorinated molecules more readily available than ever before and have begun to have an impact on research areas that do not require large amounts of material, such as drug discovery and positron emission tomography. This Review gives a brief summary of conventional fluorination reactions, including those reactions that introduce fluorinated functional groups, and focuses on modern developments in the field.

/pdf/introduction-of-fluorine-and-fluorine-containing-functional-1i8kwiad20.pdf

Introduction of Fluorine and Fluorine-Containing Functional Groups

The discovery of Toll-like receptors (TLRs) offers the possibility to treat diseases by stimulating immune functions in a targeted manner. Krieg reviews the potential of synthetic DNAs that activate TLR9 and are in clinical development in cancer, infectious disease and asthma/allergy. In the decade since the discovery that mouse B cells respond to certain unmethylated CpG dinucleotides in bacterial DNA, a specific receptor for these 'CpG motifs' has been identified, Toll-like receptor 9 (TLR9), and a new approach to immunotherapy has moved into the clinic based on the use of synthetic oligodeoxynucleotides (ODN) as TLR9 agonists. This review highlights the current understanding of the mechanism of action of these CpG ODN, and provides an overview of the preclinical data and early human clinical trial results using these drugs to improve vaccines and treat cancer, infectious disease and allergy/asthma.

Therapeutic potential of Toll-like receptor 9 activation

Human pharmaceuticals in the aquatic environment: a challenge to Green Chemistry.

Fluorine in medicinal chemistry: A review of anti-cancer agents

Important fluorinated drugs in experimental and clinical use

Aziridine alkaloids as potential therapeutic agents.

The destruction of dichloromethane by a nonthermal plasma in atmospheric-pressure gas streams of nitrogen with variable amounts of added oxygen has been investigated. The identities and concentrati...

The Chemistry of Dichloromethane Destruction in Atmospheric-Pressure Gas Streams by a Dielectric Packed-Bed Plasma Reactor

Resistant strains of Plasmodium falciparum and the unavailability of useful antimalarial vaccines reinforce the need to develop new efficacious antimalarials. This study details a pharmacophore model that has been used to identify a potent, soluble, orally bioavailable antimalarial bisquinoline, metaquine (N,N‘-bis(7-chloroquinolin-4-yl)benzene-1,3-diamine) (dihydrochloride), which is active against Plasmodium berghei in vivo (oral ID50 of 25 μmol/kg) and multidrug-resistant Plasmodium falciparum K1 in vitro (0.17 μM). Metaquine shows strong affinity for the putative antimalarial receptor, heme at pH 7.4 in aqueous DMSO. Both crystallographic analyses and quantum mechanical calculations (HF/6-31+G*) reveal important regions of protonation and bonding thought to persist at parasitic vacuolar pH concordant with our receptor model. Formation of drug−heme adduct in solution was confirmed using high-resolution positive ion electrospray mass spectrometry. Metaquine showed strong binding with the receptor in a 1...

Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: design, construction, characterization, and pharmacology of metaquine.

The compositions of the essential oils obtained from seven species of Melaleuca grown in the municipal district of Vicosa, State of Minas Gerais, Brazil, were analysed by both GC and GC-MS. The various Melaleuca species showed differences within their relative essential oil compositions. Each of the oils analysed revealed a dominant compo- nent: terpinen-4-ol (53.7 ± 0.2%) for M. alternifolia; 1,8-cineole for M. armillaris (80.2 ± 0.0%), M. ericifolia (79.5 ± ± ± ± 0.4%), M. cajuputi, subspecies cajuputi (43.7 ± 0.5%) and M. cajuputi subspecies platyphylla (41.0 ± 8.5%); viridiflorol (71.0 ± ± ± ± ± 0.9%) for M. quinquenervia; and methyl eugenol (96.6 ± 0.7%) for M. leucadendra. Copyright © 2007 John Wiley & Sons, Ltd.

Fyaz M.D. Ismail

Papers

Important fluorinated drugs in experimental and clinical use

Aziridine alkaloids as potential therapeutic agents.

The Chemistry of Dichloromethane Destruction in Atmospheric-Pressure Gas Streams by a Dielectric Packed-Bed Plasma Reactor

Mapping antimalarial pharmacophores as a useful tool for the rapid discovery of drugs effective in vivo: design, construction, characterization, and pharmacology of metaquine.

Comparative study of the essential oils of seven Melaleuca (Myrtaceae) species grown in Brazil