β-Acarbose. I The Synthesis of 1-Epivalienamine

1997 ◽  
Vol 50 (3) ◽  
pp. 193 ◽  
Author(s):  
Joseph C. McAuliffe ◽  
Robert V. Stick
Keyword(s):  
Derivatives Of ◽  
Potential Use

Improvements and modifications to a literature procedure for the synthesis of multigram amounts of a derivative of 1-epivalienamine are described. As well, various other derivatives of 1-epivalienamine, of potential use in the synthesis of carba sugars, are reported.

scholarly journals Biguanide-Based Synthesis of 1,3,5-Triazine Derivatives with Anticancer Activity and 1,3,5-Triazine Incorporated Calcium Citrate Nanoparticles

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 1028
Author(s):  
Monnaya Chalermnon ◽  
Sarocha Cherdchom ◽  
Amornpun Sereemaspun ◽  
Rojrit Rojanathanes ◽  
Tanatorn Khotavivattana
Keyword(s):  
Anticancer Activity ◽  
Cell Lines ◽  
Anticancer Agent ◽  
Drug Loading ◽  
Calcium Citrate ◽  
Colorectal Cancer Cell Lines ◽  
Triazine Derivatives ◽  
Further Development ◽  
Derivatives Of ◽  
Potential Use

Twelve derivatives of biguanide-derived 1,3,5-triazines, a promising class of anticancer agent, were synthesised and evaluated for their anticancer activity against two colorectal cancer cell lines—HCT116 and SW620. 2c and 3c which are the derivatives containing o-hydroxyphenyl substituents exhibited the highest activity with IC50 against both cell lines in the range of 20–27 µM, which is comparable to the IC50 of cisplatin reference. Moreover, the potential use of the calcium citrate nanoparticles (CaCit NPs) as a platform for drug delivery system was studied on a selected 1,3,5-triazine derivative 2a. Condition optimisation revealed that the source of citrate ions and reaction time significantly influence the morphology, size and %drug loading of the particles. With the optimised conditions, “CaCit-2a NPs” were successfully synthesised with the size of 148 ± 23 nm and %drug loading of up to 16.3%. Furthermore, it was found that the release of 2a from the synthesised CaCit-2a NPs is pH-responsive, and 2a could be control released under the acidic cancer environment. The knowledge from this study is perceptive for further development of the 1,3,5-triazine-based anticancer drugs and provide the platform for the incorporation of other drugs in the CaCit NPs in the future.

Total synthesis of indole and dihydroindole alkaloids. X.1,2 The preparation of novel oxygenated catharanthine derivatives

1977 ◽  
Vol 55 (18) ◽  
pp. 3227-3234 ◽  
Author(s):  
James P. Kutney ◽  
Gordon H. Bokelman ◽  
Masahiro Ichikawa ◽  
Edwin Jahngen ◽  
Alummoottil V. Joshua ◽  
...  
Keyword(s):  
Double Bond ◽  
Total Synthesis ◽  
Osmium Tetroxide ◽  
Electrophilic Attack ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Potential Use

Detailed investigations involving the electrophilic attack of various reagents on the 3,4-double bond of catharanthine derivatives (e.g. 3, R = O) furnished a series of novel derivatives of potential use in the syntheses of naturally occurring bisindole alkaloids. These studies include such reagents as peracid, osmium tetroxide, and positive iodine.

SYNTHESIS OF 3-AMINO-2,3-DIDEOXY-D-lyxo-HEXOSE

1965 ◽  
Vol 43 (11) ◽  
pp. 3074-3079 ◽  
Author(s):  
Hans H. Baer ◽  
Frank Kienzle
Keyword(s):  
Aspartic Acid ◽  
Catalytic Hydrogenation ◽  
Title Compound ◽  
Amine Hydrochloride ◽  
Derivatives Of ◽  
Potential Use

Catalytic hydrogenation of methyl 4,6-O-benzylidene-2,3-dideoxy-3-nitro-β-D-threo-hexo-pyranos-2-enide (I) afforded methyl 4,6-O-benzylidene-2,3-dideoxy-3-nitro-β-D-lyxo-hexo-pyranoside (II). Acid debenzylidenation and further hydrogenation gave in turn methyl 2,3-dideoxy-3-nitro-β-D-lyxo-hexopyranoside (III) and the corresponding amine hydrochloride (IV). Several crystalline derivatives of IV were prepared, and the configuration at C-3 was proved by degradation of the N-benzoate (VII) to N-benzoyl-D-aspartic acid. The title compound (V) was obtained as a chromatographically homogeneous sirup.Some methyl 3-deoxy-3-nitro-β-L-hexopyranosides were prepared for potential use as starting materials in analogous syntheses in the L-series.

Properties and uses of neem, Azadirachta indica

1990 ◽  
Vol 68 (1) ◽  
pp. 1-11 ◽  
Author(s):  
Opender Koul ◽  
Murray B. Isman ◽  
C. M. Ketkar
Keyword(s):  
Azadirachta Indica ◽  
Third World ◽  
Agricultural Crops ◽  
Neem Tree ◽  
The Third ◽  
Economic Exploitation ◽  
Human Use ◽  
The Third World ◽  
Derivatives Of ◽  
Potential Use

The versatility of the neem tree Azadirachta indica A. Juss. is reviewed. This species, native to India, grows in nutrient-poor soils in arid habitats and has tremendous potential for human use. Various derivatives of the tree have potential use in toiletries, pharmaceuticals, the manufacture of agricultural implements and furniture, cattle and poultry feeds, nitrification of soils for various agricultural crops, and pest control. Since neem is a natural renewal resource producing extensive useful biomass, its propagation and economic exploitation will be beneficial, particularly to the Third World. In recent years, some useful commercial products have been developed from A. indica, and mere is considerable scope for future product development. Potentially profitable lines of research on this plant species are suggested.

scholarly journals Investigations of Azulene Derivatives as Self-Indicating Chromophores for Applications in Protecting Group Strategies and Solid-Phase Purification

2021 ◽  
Author(s):  
◽  
Thomas Bevan
Keyword(s):  
Electronic Properties ◽  
Solid Phase ◽  
Protecting Groups ◽  
Protecting Group ◽  
Blue Colour ◽  
Derivatives Of ◽  
Potential Use

<p>Azulene is a hydrocarbon that exhibits an intense blue colour. Derivatives of azulene exhibit different colours depending on the position and electronic properties of the substituents. The chemical and chromophoric properties of azulene and guaiazulene derivatives are investigated for the potential use in applications such as chromophoric protecting groups and self-indicating scavenger resins. Investigations were carried out on the scope of known reactions on the 3- position of guaiazulene for this purpose...</p>

scholarly journals Natural Products: A Potential Source of Malaria Transmission Blocking Drugs?

2020 ◽  
Vol 13 (9) ◽  
pp. 251
Author(s):  
Phanankosi Moyo ◽  
Grace Mugumbate ◽  
Jacobus N. Eloff ◽  
Abraham I. Louw ◽  
Vinesh J. Maharaj ◽  
...  
Keyword(s):  
Natural Products ◽  
Mosquito Vector ◽  
Blocking Drug ◽  
Transmission Blocking ◽  
Antimalarial Agents ◽  
Challenges And Opportunities ◽  
Sexual Stages ◽  
Derivatives Of ◽  
Effective Transmission ◽  
Potential Use

The ability to block human-to-mosquito and mosquito-to-human transmission of Plasmodium parasites is fundamental to accomplish the ambitious goal of malaria elimination. The WHO currently recommends only primaquine as a transmission-blocking drug but its use is severely restricted by toxicity in some populations. New, safe and clinically effective transmission-blocking drugs therefore need to be discovered. While natural products have been extensively investigated for the development of chemotherapeutic antimalarial agents, their potential use as transmission-blocking drugs is comparatively poorly explored. Here, we provide a comprehensive summary of the activities of natural products (and their derivatives) of plant and microbial origins against sexual stages of Plasmodium parasites and the Anopheles mosquito vector. We identify the prevailing challenges and opportunities and suggest how these can be mitigated and/or exploited in an endeavor to expedite transmission-blocking drug discovery efforts from natural products.

scholarly journals Structural properties of methoxy derivatives of benzyl bromide, determined from powder X-ray diffraction data

2005 ◽  
Vol 20 (4) ◽  
pp. 345-352 ◽  
Author(s):  
Zhigang Pan ◽  
Eugene Y. Cheung ◽  
Kenneth D. M. Harris ◽  
Edwin C. Constable ◽  
Catherine E. Housecroft
Keyword(s):  
Structural Properties ◽  
Diffraction Data ◽  
Benzyl Bromide ◽  
Building Blocks ◽  
X Ray Diffraction ◽  
X Ray ◽  
Structure Solution ◽  
Derivatives Of ◽  
Potential Use

Structure determination of 3,5-dimethoxybenzyl bromide and 3,4,5-trimethoxybenzyl bromide has been carried out from laboratory powder X-ray diffraction data using the direct-space Genetic Algorithm technique for structure solution followed by Rietveld refinement. These two compounds are of interest for their potential use as building blocks for the synthesis of dendritic materials. Although the two molecules differ only in the presence/absence of the methoxy group at the 4-position of the aromatic ring, the structural properties of the two materials are significantly different.

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