China
Africa
Explore chapters and articles related to this topic
Antihistamines, Decongestants, and Expectorants during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
Brompheniramine, chlorpheniramine, dexchlorpheniramine, and triprolidine are propylamine derivatives. Brompheniramine was weakly associated with birth defects in 65 offspring exposed during the first trimester, but the association is not likely causative (Heinonen et al., 1977). In a larger study of 270 infants born following first-trimester exposure to brompheniramine, birth defects were not increased in frequency among 270 infants whose mothers took brompheniramine during embryogenesis (Aselton et al., 1985; Jick et al., 1981). Analysis of pheniramine (either brompheniramine or chlorpheniramine) in the National Birth Defects Prevention Study found no causal relationship between birth defects and first trimester exposure to these pheniramines (Gilboa et al., 2009). Meta-analysis of available data on brompheniramine indicate it is not a human teratogen (Seto et al., 1993) and this finding is supported by a recent review (Gilbert et al., 2005) that included more information than the meta-analysis (Table 11.3).
Synthetic Nanoparticles for Anticancer Drugs
Published in Harishkumar Madhyastha, Durgesh Nandini Chauhan, Nanopharmaceuticals in Regenerative Medicine, 2022
Nanoparticles (NPs) are having a considerable impact on modern medical applications. They are used for drug delivery systems and targeted therapy. Nanoparticles are composed of metal, nonmetal atoms, or a mixture of both. CSA-13 is an example of a synthetic NP, which is composed of an iron oxide anion, an aminosilane group, and the antibacterial peptide LL-37. Propylamine groups, which are placed in the core of the magnetic NPs structure, were synthesized using the modified Stöber method (Geetha et al. 2013).
Therapeutic Medicinal Mushroom (Ganoderma Lucidum): A Review of Bioactive Compounds and their Applications
Published in Megh R. Goyal, Durgesh Nandini Chauhan, Plant- and Marine-Based Phytochemicals for Human Health, 2018
Chen et al. (2010) using headspace solid-phase microextraction combined with gas chromatography-mass spectrometry (HS-SPME-GCMS) enabled detection of fifty-eight volatile compounds in G. lucidum mycelium. The main volatile flavor compounds included 1-octen-3-ol, ethanol, hexanal, 1-hexanol, sesquirosefuran, 3-octanol, and 3-octanone.23 Similar chromatographic technology (HS-SPME-GC-MS) was used to detect volatile aroma compounds in G. lucidum from Turkey. They detected acids, alcohols, aldehydes, phenols, L-Alanine, D-Alanine, 3-Methyl, 2-Butanamine, 2-Propanamine, and identified 1-Octen-3-ol and 3-Methyl butanal as the major aroma compounds.151 C-19 fatty acids were also detected in the ethanolic extract of G. lucidum spores by Gao and coworkers.35 During their research, 2-naphthyl esters of nonadecanoic and cis-9-nonadecenoic acids isolated by multiple column chromatography and preparative HPLC and characterized by 1Hand 13C-NMR and MS spectral data from the G. lucidum spores were identified as the bioactive constituents responsible for the antitumor activity.35
Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Mingxia Song, Rui Yan, Yanhui Zhang, Dongfu Guo, Naiming Zhou, XianQing Deng
Compounds 3k, 3l, 3m, and 3n were substituted on 3-position of 1,2,4-triazole ring with methyl, phenyl, para-chlorophenyl, and biphenyl, respectively. Encouragingly, the introduction of methyl, phenyl, and para-chlorophenyl groups significantly increased the H3R antagonistic activities, giving the two prominent compounds 3l and 3m with nanomolar IC50 values. While the biphenyl substituted compound 3n showed weaker activity when compared to 3h. Replacing the three-carbon link in the compound 3h with two-carbon, four-carbon and five-carbon links, gave the compounds 3o, 3p, and 3q, respectively. It could be seen that the length of the link had a direct impact on H3 receptor antagonistic activities of the 3-(4-(4H-1,2,4-triazol-4-yl)phenoxy)-propylamine derivatives. The activity order of the link length of carbon was 3 > 2 > 4 ≫ 5.
Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Jonathan Elie, Omid Feizbakhsh, Nathalie Desban, Béatrice Josselin, Blandine Baratte, Amandine Bescond, Julien Duez, Xavier Fant, Stéphane Bach, Dominique Marie, Matthieu Place, Sami Ben Salah, Agnes Chartier, Sabine Berteina-Raboin, Apirat Chaikuad, Stefan Knapp, Fabrice Carles, Pascal Bonnet, Frédéric Buron, Sylvain Routier, Sandrine Ruchaud
As expected, compounds without any heteroatom attached to the imidazopyridazine core in C-6 (compound 30) or lacking the indazole part in C-3 (compounds 27–29), lost their activity for Haspin. It was evidence that these two elements play a crucial role maintaining potent inhibitory activity and that they define the key pharmacophore. Modulation of the propyl amine in C-6 led to variation in Haspin inhibition. Methylation of the NH group confirmed that the labile proton was not essential (compound 8). Cycloalkylamines as well as piperidine were used as substituents in C-6 without any significant changes in activity (compounds 9–11). The cyclopentyl group seemed preferred, with an improved activity for compound 9 at IC50 = 31 nM. Finally, a second hydrophilic function was introduced on the small amino alkyl side chain in compound 12 and resulted in activity that remained identical to that of other derivatives of this subfamily.
Effect of silica nano-spheres on adhesion of oral bacteria and human fibroblasts
Published in Biomaterial Investigations in Dentistry, 2020
Pawel Kallas, Hua Kang, Håkon Valen, Håvard Jostein Haugen, Martin Andersson, Mats Hulander
Standard microscope glass slides were treated in an UV-O3 cleaner (BHK INC., Claremont, CA) for 15 min to remove organic contaminants and then washed in basic piranha solution (MQ water, NH4OH and 30% H2O2; 5:1:1) for 15 min at 80 °C. After that, surfaces where rinsed with MQ water and dried under N2 (g) flow. Immediately after, the surfaces were placed in a sealed container together with 3-(ethoxydimethylsilyl)propylamine in methanol (50/50; 200 µl each) in a watch glass for 30 min to amine-functionalize the substrates through evaporation of the silane onto the surfaces. Surfaces with homogenous distribution of nanoparticles were then prepared by submerging only half of the amine functionalized surface into a colloidal solution with 40 nm sized SiO2 nanoparticles (∼10 nM nanoparticle concentration) in 5 mM sodium citrate buffer (pH 4) for 15 min before thoroughly rinsing with MQ water and drying under a stream of N2 (g).