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221.
Polepally AR Kumar VV Bhamidipati R Kota J Naveed SA Reddy KH Mamidi RN Selvakumar N Mullangi R Srinivas NR 《Biomedical chromatography : BMC》2008,22(9):960-976
The discovery of small-molecule novel chemical entities (NCEs) is often a complex play between appropriate structural requirements and optimization of the desired efficacy, safety and pharmacokinetic properties. One of the typical structural variants such as having an active carbon-carbon double bond (alpha, beta-unsaturated carbonyl group) in xenobiotics may lead to stability issues. Such functionalities are extremely reactive, paving way to nucleophilic attack by endogenously occurring and ubiquitous nucleophiles like thiols. While it is easy to make a unilateral decision to not pursue the development of xenobiotics with such functionalities, we question the wisdom of such a decision. In this report, we present in vitro methodologies with appropriate examples to illustrate the ease of assessing the reactivity of the xenobiotics containing double bonds with a known nucleophile. The protocols involve simple reaction procedures followed by measurements using standard laboratory equipments (UV spectrophotometer, HPLC and LC-MS). Our data suggests that not all xenobiotics with carbon-carbon double bonds readily form a Michael's adduct product with glutathione. Hence, the criterion for dropping discovery compounds because of alpha,beta-unsaturated double bonds needs to be reconsidered. Copyright (c) 2008 John Wiley & Sons, Ltd. 相似文献
222.
Keiji Fushimi Kota Anzai Shinji Tokuyama Yoshikazu Kiriiwa Noriyuki Matsumoto Atsushi Sekiya Daisuke Hashizume Kazuo Nagasawa Hirofumi Hirai Hirokazu Kawagishi 《Tetrahedron》2012,68(4):1262-1265
Five novel compounds (1–3, 5, and 6), and two known ones (4 and 7) were isolated from the culture broth of Agrocybe praecox. Their structures were determined by the interpretation of spectroscopic data. Compounds 1–4 inhibited hypocotyl growth of lettuce, and 1, 3, and 4 inhibited the root growth. 相似文献
223.
Iori Yamada Kota Shiba Tania Guadalupe Peaflor Galindo Motohiro Tagaya 《Molecules (Basel, Switzerland)》2022,27(18)
Theranostics (bifunction of therapeutics and diagnostics) has attracted increasing attention due to its efficiency that can reduce the physical and financial burden on patients. One of the promising materials for theranostics is calcium phosphate (CP) and it is biocompatible and can be functionalized not only with drug molecules but also with rare earth ions to show photoluminescence that is necessary for the diagnostic purpose. Such the CP-based hybrids are formed in vivo by interacting between functional groups of organic molecules and inorganic ions. It is of great importance to elucidate the interaction of CP with the photofunctional species and the drug molecules to clarify the relationship between the existing state and function. Well-designed photofunctional CPs will contribute to biomedical fields as highly-functional ormultifunctional theranostic materials at the nanoscales. In this review, we describe the hybridization between CPs and heterogeneous species, mainly focusing on europium(III) ion and methylene blue molecule as the representative photofunctional species for theranostics applications. 相似文献