抗原变异可使得多种致病微生物易于逃避宿主免疫应答。表达在感染红细胞表面的恶性疟原虫红细胞表面蛋白1（PfPMP1）与感染红细胞、内皮细胞、树突状细胞以及胎盘的单个或多个受体作用，在黏附及免疫逃避中起关键的作用。每个单倍体基因组var基因家族编码约60种成员，通过启动转录不同的var基因变异体为抗原变异提供了分子基础。

疟原虫var基因转换速率变化导致抗原变异[英]／Paul H, Robert P, Christodoulou Z, et al//Proc Natl Acad Sci U S A

https://chemistry.mdma.ch/hiveboard/rhodium/pdf/archive/merbst/quinoline1999.pdf

Quinoline, quinazoline and acridone alkaloids

Multicomponent reactions have gained significant importance as a tool for the synthesis of a wide variety of useful compounds, including pharmaceuticals. In this context, the multiple component approach is especially appealing in view of the fact that products are formed in a single step, and the diversity can be readily achieved simply by varying the reacting components. The eco-friendly, solvent-free multicomponent approach opens up numerous possibilities for conducting rapid organic synthesis and functional group transformations more efficiently. Additionally, there are distinct advantages of these solvent-free protocols since they provide reduction or elimination of solvents thereby preventing pollution in organic synthesis “at source”. The chemo-, regio- or stereoselective synthesis of high-value chemical entities and parallel synthesis to generate a library of small molecules will add to the growth of multicomponent solvent-free reactions in the near future. In this review we summarized the results reported mainly within the last 10 years. It is quite clear from the growing number of emerging publications in this field that the possibility to utilize multicomponent technology allows reaction conditions to be accessed that are very valuable for organic synthesis. Therefore, diversity oriented synthesis (DOS) is rapidly becoming one of the paradigms in the process of modern drug discovery. This has spurred research in those fields of chemical investigation that lead to the rapid assembly of not only molecular diversity, but also molecular complexity. As a consequence multi-component as well as domino or related reactions are witnessing a new spring.

/pdf/recent-developments-in-solvent-free-multicomponent-reactions-4ugdax2te0.pdf

Recent developments in solvent-free multicomponent reactions: a perfect synergy for eco-compatible organic synthesis

The synthesis of novel 7-(4-halophenyl)-8,9-dihydro-7H-12-oxa-9,11-diaza-benzo[a]anthracene derivatives has been reported. The key intermediate 3-amino-9-chloro-1-(4-halophenyl)-1H-benzo[h]chromene-2-carbonitrile (3) was obtained by treating 4-halobenzylidenmalononitriles (1a-c) and ethyl 4-halobenzylidenmalonates (1d-f) with 4-chloro-1-naphthol (2) in ethanolic piperidine solution. Antimicrobial activity was shown for most of the synthesized compounds.

Synthesis of halogen derivatives of benzo[h]chromene and benzo[a]anthracene with promising antimicrobial activities.

Photodynamic therapy (PDT) is a promising alternative approach for improved cancer treatment. In PDT, a photosensitizer (PS) is administered that can be activated by light of a specific wavelength, which causes selective damage to the tumor and its surrounding vasculature. The success of PDT is limited by the difficulty in administering photosensitizers (PSs) with low water solubility, which compromises the clinical use of several molecules. Incorporation of PSs in nanostructured drug delivery systems, such as polymeric nanoparticles (PNPs), solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs), gold nanoparticles (AuNPs), hydrogels, liposomes, liquid crystals, dendrimers, and cyclodextrin is a potential strategy to overcome this difficulty. Additionally, nanotechnology-based drug delivery systems may improve the transcytosis of a PS across epithelial and endothelial barriers and afford the simultaneous co-delivery of two or more drugs. Based on this, the application of nanotechnology in medicine may offer numerous exciting possibilities in cancer treatment and improve the efficacy of available therapeutics. Therefore, the aim of this paper is to review nanotechnology-based drug delivery systems for photodynamic therapy of cancer.

Nanotechnology-Based Drug Delivery Systems for Photodynamic Therapy of Cancer: A Review

Studies on Cinnamonitriles: The Reaction of Cinnamonitriles with Cyclopentanone

L-Arginine grafted alginate hydrogel beads: A novel pH-sensitive system for specific protein delivery

A new and easy synthesis of silylated furanoid glycals in one step from nucleosides

A new synthetic route was developed to create azo based dispersed dyes which are derived from 3-(3-Chloropheney)-2-((4-substituted) diazenyl)-3-oxopropanenitrile and 3-substituted 5-amino-4-arylazopyrazoles. The new dyestuff was used to dye unmodified polypropylene fabrics under both aqueous and supercritical carbon dioxide mediums. A pilot scale experiment was performed on the dyestuff 3a to prove the potentiality of the dyestuff toward polypropylene fabric. The new dyes were characterized by MS, IR and NMR spectral data and found to be in good agreement with the proposed structures. The colour uptake expressed as colour strength (K/S) was assessed and the values obtained showed that the dyed polypropylene fabrics using scCO2 method was significantly better than the aqueous one. The colour fastness properties of all the dyed fabrics were evaluated and exhibited excellent results. Moreover, it is also a green approach for using industrial emissions of CO2 instead of water in the textile dyeing process.

Optimization of an eco-friendly dyeing process in both laboratory scale and pilot scale supercritical carbon dioxide unit for polypropylene fabrics with special new disperse dyes

Naphtho[2,1-b:3,4-b']dipyrans, naphtho[1,2-b:5,6-b']dipyrans and naphtho[1,2-b:6,5-b']dipyrans were synthesized by the reaction of cinnamonitriles with 2,3-, 1,5-, 1,6-naphthalenediols, respectively. Polysubstituted pyridines, 2H-pyrans and 4H-pyrans were also synthesized from cinnamonitriles, 2-hydroxyacetophenone and 3-acetyl-4-hydroxy-1-methylcarbostyril, respectively

Mamdouh A. Sofan

Papers

Studies on Cinnamonitriles: The Reaction of Cinnamonitriles with Cyclopentanone

L-Arginine grafted alginate hydrogel beads: A novel pH-sensitive system for specific protein delivery

A new and easy synthesis of silylated furanoid glycals in one step from nucleosides

Optimization of an eco-friendly dyeing process in both laboratory scale and pilot scale supercritical carbon dioxide unit for polypropylene fabrics with special new disperse dyes

Nitriles in heterocyclic synthesis: a novel route for the synthesis of naphthodipyrans, pyridines: 2H- and 4H-pyrans