scholarly journals Corrigendum to ‘Synthesis, characterization and in vivo skeletal localization of a new 99mTc based multidentate phosphonate Chelate: 5-amino-1,3-bis (ethylamine-(N,N dimethyl diphosphonic acid) acetamido) benzene, (5-aminoisophthalte tetramethlene phosphonic acid)’ Bioorganic & Medicinal Chemistry, volume 15, issue 2, 15 January 2007, pages 1138–1145

2021 ◽  
pp. 116565
Author(s):  
Puja Panwar ◽  
Sweta Singh ◽  
Nitin Kumar ◽  
Harish Rawat ◽  
Anil K. Mishra
Keyword(s):  
Phosphonic Acid ◽  
Medicinal Chemistry ◽  
Diphosphonic Acid

scholarly journals Bone marrow transplantation in dogs after radio-ablation with a new Ho- 166 amino phosphonic acid bone-seeking agent (DOTMP)

Blood ◽  
1993 ◽  
Vol 82 (1) ◽  
pp. 318-325 ◽  
Author(s):  
NJ Parks ◽  
TG Kawakami ◽  
MJ Avila ◽  
R White ◽  
GR Cain ◽  
...  
Keyword(s):  
Bone Marrow ◽  
Phosphonic Acid ◽  
Marrow Cell ◽  
Nuclear Imaging ◽  
Beta Particle ◽  
Skeletal Tissue ◽  
Red Marrow ◽  
Bone Biopsies ◽  
Total Body

beta-emitting 166Ho (t1/2 = 26.78 hours, E(beta)max = 1.8 MeV) complexed with the phosphonic acid chelator, 1,4,7,10 tetraazacyclododecane-1,4,7,10-tetra(methylene phosphonic acid) (DOTMP) at a ligand-to-metal ratio of 1.5:1 binds to bone. This radioactive complex is a marrow-ablating radiopharmaceutical that appears useful for preparation of bone marrow (BM) transplant recipients without the morbidity usually associated with total body irradiation preparatory regimens. We have found with seven splenectomized young adult beagle dogs that a 166Ho radiopharmaceutical dosage of 370 MBq/kg body weight provides an initial skeletal radioactivity burden of at least 1.5 GBq/kg skeleton and results in complete ablation of hematopoietic marrow cell populations within 7 days. The beta particle flux distribution in BM-forming skeletal tissue is not uniform. Red marrow radiation doses varied from 30 to 115 Gy as estimated by direct radioassay and autoradiographic analyses of both bone biopsies and postmortem samples; the median value of 61 Gy agreed with our theoretical expectations. In vivo radioactivity distribution was evaluated with nuclear imaging methods. Apparently, normal hematopoiesis was restored in three dogs with autologous BM transplants performed 5 to 6 days after administration of the marrow ablative radiopharmaceutical, 166Ho-DOTMP. BM biopsies at 7 to 10 months posttransplantation indicate continued normal hematopoietic activity.

scholarly journals Copper(II) Complexes of Organophoshonic Acids-A Comparative Study

2011 ◽  
Vol 8 (s1) ◽  
pp. S271-S281
Author(s):  
B. Venkateswara Rao ◽  
D. M. Puri
Keyword(s):  
Phosphonic Acid ◽  
Octahedral Geometry ◽  
Spectral Studies ◽  
Diphosphonic Acid ◽  
Paramagnetic Resonance ◽  
Diethylene Triamine ◽  
Coordination Sites ◽  
Infrared Spectral ◽  
Electron Paramagnetic ◽  
Derivatives Of

Polynuclear copper(II) derivatives of 1-hydroxyethylidenediphosphonic acid (HEDP), 1-aminoethylidenediphosphonic acid (AEDP, H4L),α-aminobenzylidene diphosphonic acid (ABDP, H4L), 1-amino-2-carboxyethane- 1,1-diphosphonic acid (ACEDP, H5L), 1,3 diaminopropane-1,1,3,3-tetra-phosphonic acid (DAPTP, H8L), Ethylenediamine-N,N'-bis (dimethyl-methylenephosphonic) acid (EDBDMPO, H4L),o-phenylene-diamine-N,N'-bis (dimethylmethylenephosphonic) acid (PDBDMPO, H4L), diethylene triamine –N,N,N',N',N"N-penta (methylene phosphonic) acid (DETAPMPO, H10L) and diethylene triamine –N,N"-bis (dimethyl methylene phosphonic) acid (DETBDMPO, H4L) have been prepared in aqueous medium. The general formula of derivatives from elemental analysis was found to be Cu2L.XH2O (in case of AEDP, ABDP, EDBDMPO, PDBDMPO, DETBDMPO), Cu5L2.XH2O (in case of ACEDP) Cu4L.XH2O, Cu2H4L. XH2O (in case of DAPTP) and Cu5L.XH2O (in case of DETAPMPO). The electronic spectra have shown them to be six coordinated with slight distortion from octahedral geometry. Antiferromagnetism was inferred from magnetic moment data. Infrared spectral studies were carried out to determine coordination sites. EPR (Electron Paramagnetic Resonance) spectra that supports the presence of tetragonal distortion and antiferromagnetic behaviour, have also been studied.

Hydroxyproline-Based DNA Mimics: A Review on Synthesis and Properties

2006 ◽  
Vol 71 (7) ◽  
pp. 929-955 ◽  
Author(s):  
Vladimir A. Efimov ◽  
Oksana G. Chakhmakhcheva
Keyword(s):  
Nucleic Acid ◽  
Nucleic Acids ◽  
Phosphonic Acid ◽  
Peptide Nucleic Acids ◽  
Biological Properties ◽  
High Potential ◽  
Physicochemical And Biological Properties

With the aim to improve physicochemical and biological properties of natural oligonucleotides, many types of DNA analogues and mimics are designed on the basis of hydroxyproline and its derivatives, and their properties are evaluated. Among them, two types of DNA mimics representing hetero-oligomers constructed from alternating monomers of phosphono peptide nucleic acids and monomers on the base of trans-1-acetyl-4-hydroxy-L-proline (HypNA-pPNAs) and oligomers constructed from monomers containing (2S,4R)-1-acetyl-4-hydroxypyrrolidine-2-phosphonic acid backbone (pHypNAs) are of particular interest. In a set of in vitro and in vivo assays, it was shown that HypNA-pPNAs and pHypNAs demonstrated a high potential for the use in nucleic acid based diagnostics, isolation of nucleic acids and antisense experiments. A review with 53 references.

scholarly journals In vitro and in vivo antibacterial activities of FR-31564, a new phosphonic acid antibiotic.

1980 ◽  
Vol 33 (1) ◽  
pp. 36-43 ◽  
Author(s):  
YASUHLRO MINE ◽  
TOSHIAKI KAMIMURA ◽  
SHIGEO NONOYAMA ◽  
MINORU NISHIDA ◽  
SACHIKO GOTO ◽  
...  
Keyword(s):  
Phosphonic Acid ◽  
Antibacterial Activities

scholarly journals The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4095 ◽  
Author(s):  
Luiz C. S. Pinheiro ◽  
Lívia M. Feitosa ◽  
Marilia O. Gandi ◽  
Flávia F. Silveira ◽  
Nubia Boechat
Keyword(s):  
Plasmodium Falciparum ◽  
Mouse Model ◽  
Infected Mouse ◽  
Plasmodium Berghei ◽  
Medicinal Chemistry ◽  
Quinoline Derivatives ◽  
Dihydroorotate Dehydrogenase ◽  
New Compounds

Based on medicinal chemistry tools, new compounds for malaria treatment were designed. The scaffolds of the drugs used to treat malaria, such as chloroquine, primaquine, amodiaquine, mefloquine and sulfadoxine, were used as inspiration. We demonstrated the importance of quinoline and non-quinoline derivatives in vitro with activity against the W2 chloroquine-resistant (CQR) Plasmodium falciparum clone strain and in vivo against Plasmodium berghei-infected mouse model. Among the quinoline derivatives, new hybrids between chloroquine and sulfadoxine were designed, which gave rise to an important prototype that was more active than both chloroquine and sulfadoxine. Hybrids between chloroquine–atorvastatin and primaquine–atorvastatin were also synthesized and shown to be more potent than the parent drugs alone. Additionally, among the quinoline derivatives, new mefloquine derivatives were synthesized. Among the non-quinoline derivatives, we obtained excellent results with the triazolopyrimidine nucleus, which gave us prototype I that inspired the synthesis of new heterocycles. The pyrazolopyrimidine derivatives stood out as non-quinoline derivatives that are potent inhibitors of the P. falciparum dihydroorotate dehydrogenase (PfDHODH) enzyme. We also examined the pyrazolopyridine and pyrazolopyrimidine nuclei.

Persistent luminescence nanoparticles functionalized by polymers bearing phosphonic acid anchors: synthesis, characterizations, and in vivo behavior

Nanoscale ◽  
2021 ◽  
Author(s):  
Thomas Lecuyer ◽  
Nicolas Bia ◽  
Pierre Burckel ◽  
Cedric Loubat ◽  
Alain Graillot ◽  
...  
Keyword(s):  
Phosphonic Acid ◽  
In Vivo Imaging ◽  
Clinical Diagnostics ◽  
Persistent Luminescence ◽  
Further Development

Optical in vivo imaging has become a widely used technique and is still under development for clinical diagnostics and treatment applications. To further development of the field, researchers have put...

Advances on Quinazoline Based Congeners for Anticancer Potential

2021 ◽  
Vol 25 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Garima Kapoor ◽  
Lovekesh Mehta ◽  
Roma Ghai ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Anticancer Compounds ◽  
In Vivo Models ◽  
Appropriate Treatment

: The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop an appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogen-containing heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. The various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

Complexation of 188Re-phosphonates: in vitro and in vivo studies

2003 ◽  
Vol 91 (10) ◽  
Author(s):  
B. L. Faintuch ◽  
S. Faintuch ◽  
E. Muramoto
Keyword(s):  
Phosphonic Acid ◽  
In Vivo Studies

SummaryMDP (methylenediphosphonate) and HEDP (hydroxyethylidene diphosphonate), both diphosphonates, and EDTMP (ethylenediamine tetramethylene phosphonic acid), a tetraphosphonate ligand, have been previously labeled with

A local approach to reduce industrial uranium wound contamination in rats

2004 ◽  
Vol 82 (2) ◽  
pp. 73-78 ◽  
Author(s):  
P Houpert ◽  
V Chazel ◽  
F Paquet
Keyword(s):  
Phosphonic Acid ◽  
Contact Time ◽  
Wound Dressing ◽  
Uranium Oxide ◽  
Chelating Ligands ◽  
Local Approach ◽  
New Approach ◽  
Wound Contamination

The aim of this work is to develop a new approach to partially decontaminate wounds after industrial uranium contamination, during the interval of time between contamination and transfer of the patient to the infirmary. A wound dressing and a paste mixed or not with uranium-chelating ligands, ethane-1-hydroxy-1,1-bisphosphonate (EHBP) and carballylic amido bis phosphonic acid (CAPBP), were tested in vitro on muscles and in vivo on rats after deposit of uranium oxide compounds. The dressing and the paste, composed of carboxymethylcellulose-based hydrocolloids known to be highly absorbent, were applied on simulated wounds a few minutes after the contamination. The incorporation of chelating ligands did not improve the efficacy of the dressing or paste, and the best results were obtained with the dressing. In vivo, after 1 h of contact with the wound, the dressing absorbed about 30% and 60% of a UO4 compound deposited intra- and intermuscularly, respectively. After intramuscular deposit, the efficacy of the dressing was not reduced if the contact time decreased from 1 h to 15 min. Therefore, this wound dressing could be a practical option to treat uranium-contaminated wounds, but its efficacy depends on the localization of the uranium deposit.Key words: uranium, wound, rat, treatment.

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