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Publikováno v:
Bioorganic & Medicinal Chemistry. 27:2245-2252
We have designed (S)-(5-(azetidin-2-ylmethoxy)pyridine-3-yl)methyl cyclopentadienyltricarbonyl technetium carboxylate ([99mTc]CPTT–A–E) with high affinity for nicotinic acetylcholine receptors (nAChRs) using (2(S)-azetidinylmethoxy)-pyridine (A-8
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:1670-1676
Glucagon-like peptide-1 (GLP-1) has emerged as a major therapeutic target for the treatment of type 2 diabetes. The nonapeptide GLP-1 (28-36) amide is one of the biological C-terminal products of GLP-1 modified by the neutral endopeptidase (NEP) 24.1
Autor:
Wiesław Malinka, Berenika Szczęśniak-Sięga, Szczepan Mogilski, Jan Janczak, Barbara Filipek, Jadwiga Maniewska, Rafal J. Wiglusz
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:1619-1628
Gastrotoxicity continues to be a major issue in therapy with nonsteroidal anti-inflammatory drugs (NSAIDs). Medicine is yet to develop absolutely safe analgesics. Numerous strategies are employed to discover new, safer NSAIDs, for example selective i
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:1211-1225
Excessive phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) plays a major role in the dysregulation of mRNA translation and the activation of tumor cell signaling. eIF4E is exclusively phosphorylated by mitogen-activated protein
Autor:
Cosmas O. Okoro, John Apraku
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:161-166
Inspite of progress made for the discovery of novel antiepileptic drugs, epilepsy remains an unmet medical need. We synthesized nine trifluoromethylated enaminone derivatives and tested them for their anticonvulsant activity using maximal electroshoc
Autor:
Kazuma Ogawa, Daisuke Yamada, Takeshi Takarada, Kenji Mishiro, Akira Odani, Nurmaya Effendi, Kazuhiro Shiba, Seigo Kinuya, Ryuichi Nishii
Publikováno v:
Bioorganic & Medicinal Chemistry. 27:383-393
Several malignant tumors and fibrotic diseases are associated with PDGFRβ overexpression and excessive signaling, making this receptor attractive for molecular targeting and imaging approaches. A series of benzo[d]imidazole-quinoline derivatives wer
Autor:
Jun Tanaka, Tsuneaki Ogata, Tsuyoshi Shinozuka, Eri Tokumaru, Nobuaki Watanabe, Satoko Wakimoto, Hideki Yamamoto, Kazushi Araki, Ryoko Sawamura, Makoto Mori, Yoshiyuki Onishi, Kunihiko Fujii, Masanori Kuroha, Yoshiro Tani, Tomoharu Tsukada, Jun Ohsumi, Kazunori Fujimoto, Kousei Shimada, Yumi Matsui
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:5079-5098
The lead identification of a novel potent selective PPARγ agonist, DS-6930 is reported. To avoid PPARγ-related adverse effects, a partial agonist was designed to prevent the direct interaction with helix 12 of PPARγ-LBD. Because the TZD group is k
Autor:
Hiroyuki Kagechika, Shinya Fujii, Yuko Kazui, Mari Ishigami-Yuasa, Aya Tanatani, Ayumi Yamada
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:5118-5127
The androgen receptor (AR) is a ligand-inducible transcription factor belonging to the nuclear receptor superfamily, and is a target molecule for development of drugs to treat prostate cancer. However, AR antagonists in clinical use, such as flutamid
Publikováno v:
Bioorganic & Medicinal Chemistry. 26:4863-4870
In the studied a series novel of lazabemide derivatives were designed, synthesized and evaluated as inhibitors of monoamine oxidase (MAO-A or MAO-B). These compounds used lazabemide as the lead compound, and the chemistry structures were modified by
Publikováno v:
Bioorganic & Medicinal Chemistry. 51:116497
Antibody-drug conjugates (ADCs) have emerging as efficient agents to target deliver cytotoxic drugs and reduce their off-target side effects. Triptolide has attracted attention to be used in ADC development. Herein, three rationally designed triptoli