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Synthesis of 2,8-Dioxabicyclo[3.3.1]nonane Derivatives and Their Neuroprotective Activities
Chem Pharm Bull (Tokyo). 2024;72(1):56-60. doi: 10.1248/cpb.c23-00693.ABSTRACTTwenty natural-product-like 2,8-dioxabicyclo[3.3.1]nonane derivatives were synthesized and their neuroprotective activities were tested using human monoamine oxidases (MAO) A and B and acetyl and butyryl cholinesterases (ChE). Compound 1s showed inhibitory activity for MAO-A, MAO-B and acetylcholinesterase (AChE) (IC50 values 34.0, 2.3 and 11.0 µM, respectively). The inhibition mode of (-)-1s for MAO-B was investigated. Chiral HPLC of (±)-1s separated the enantiomers and (-)-1s showed MAO-B inhibitory activity. Molecular docking simulation of (...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Hitoshi Kamauchi Akifumi Takanashi Mitsuaki Suzuki Kouki Izumi Koichi Takao Yoshiaki Sugita Source Type: research

Dual Engineering of Olivetolic Acid Cyclase and Tetraketide Synthase for the Formation of Longer Alkyl-Chain Olivetolic Acid Analogs and Their Antibacterial Activities
This article reviews the structure-based dual engineering of both enzymes responsible for the formation of the resorcinyl core of Δ9-THC and describes the effect of C-6 alkyl-length extension of olivetolic acid, along with related analogs, on the antibacterial activities against Bacillus subtilis and Staphylococcus aureus.PMID:38171898 | DOI:10.1248/cpb.c23-00692 (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Hiroyuki Morita Source Type: research

Elucidation of Degradation Behavior of Nitrazepam, a Benzodiazepine Drug, under Basic Conditions: Study on Degradability of Drugs in Stomach (IV)
This study investigates the stability of nitrazepam (NZP), a benzodiazepine drug, under basic conditions, since alkaline putrefactive amines and ammonia are produced once bodies are left to decompose for a long period postmortem after a murder involving NZP or an accidental overdose of NZP. The degradation of NZP in an aqueous alkaline solution was investigated by LC/photodiode array detector (PDA) where the NZP degradation product was isolated and purified by solid-phase extraction using Oasis® MCX, and its chemical structure was determined by LC/time-of-flight (TOF)-MS, NMR spectroscopy, and single-crystal X-ray crystal...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Koichi Saito Mai Yokota Rie Ito Miho Sakamoto Kimio Higashiyama Source Type: research

Development of an Artificial Nucleic Acid Skeleton Allowing for Unnatural-Type Triplex DNA Formation with Duplex DNA Having a TA Inversion Site
In this study, we focused on a benzimidazole skeleton and introduced a hydroxyl group to enable one-point hydrogen bonding. We have synthesized artificial nucleoside analogues with hydroxyl group on the benzimidazole and incorporated their amidite derivatives into triplex forming oligonucleotides (TFOs). The gel shift assay was performed to evaluate the triplex DNA formation ability of synthesized TFOs, and TFOs containing hydroxybenzimidazole were successfully recognized TA base pairs for all four different sequences. Moreover, compared to the results for the TFOs containing benzimidazole, which suggested hydrogen bonding...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Akihiro Ito Lei Wang Ryotaro Notomi Shigeki Sasaki Yosuke Taniguchi Source Type: research

Preparation and in Vitro Characterization of Fatty-Acid Modified Pirarubicin Nanosuspensions Stabilized by Albumin
This study aimed to develop a nanosuspension to deliver THP to tumor tissues more efficiently. Fatty-acid-modified THPs (FA-THPs; octanoic acid, dodecanoic acid, palmitic acid-THPs) were synthesized to increase the hydrophobicity of THP. Nanosuspensions of these FA-THPs were then prepared using an antisolvent precipitation technique. Among the FA-THPs, the most efficiently drug-loaded nanosuspension was obtained from palmitic acid-THP (pal-THP) using an aqueous antisolvent containing bovine serum albumin as a stabilizer. The pal-THP nanoparticles in the nanosuspension were confirmed to be of optimal size (100-125 nm) for d...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takashi Hasegawa Kenji Tsukigawa Kindness Commey Mina Sakuragi Shuhei Imoto Kazuaki Taguchi Koji Nishi Masaki Otagiri Keishi Yamasaki Source Type: research

Analysis of Factors Related to Variation in Dissolution Profiles Estimated from Continuously Conducted Dissolution Tests of Generic Products
This study analyzed the factors contributing to the changes in the dissolution profiles of approved products during their life cycles. Cumulative data on the dissolution similarity of 1675 products of 127 ingredients tested by official laboratories in Japan were assessed according to Japanese bioequivalence guidelines with slight modifications. The products showing dissimilarities in dissolution profiles were analyzed for reporting year, therapeutic category, co-development, physical properties of the active pharmaceutical ingredient (API), and suspected reasons for dissolution change. The increase in the number of dissimi...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Tokio Morita Hiroyuki Yoshida Yasuhiro Abe Koji Tomita Akihiko Nakamura Chikako Hada Chiyori Nakai Keishi Kina Makoto Takahashi Nozomi Uemura Tetsuya Yoneda Maki Yasui Yoriko Shintani Naomi Tomita Aoi Inagaki Ken-Ichi Izutsu Yoji Sato Source Type: research

Development of Small-Molecule Anti-HIV-1 Agents Targeting HIV-1 Capsid Proteins
Chem Pharm Bull (Tokyo). 2024;72(1):41-47. doi: 10.1248/cpb.c23-00618.ABSTRACTThe capsid of human immunodeficiency virus type 1 (HIV-1) forms a conical structure by assembling oligomers of capsid (CA) proteins and is a virion shell that encapsulates viral RNA. The inhibition of the CA function could be an appropriate target for suppression of HIV-1 replication because the CA proteins are highly conserved among many strains of HIV-1, and the drug targeting CA, lenacapavir, has been clinically developed by Gilead Sciences, Inc. Interface hydrophobic interactions between two CA molecules via the Trp184 and Met185 residues in ...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Takuya Kobayakawa Masaru Yokoyama Kohei Tsuji Sayaka Boku Masaki Kurakami Masayuki Fujino Takahiro Ishii Yutaro Miura Soshi Nishimura Kouki Shinohara Kenichi Yamamoto Peter Bolah Osamu Kotani Tsutomu Murakami Hironori Sato Hirokazu Tamamura Source Type: research

Development of Fast Disintegrating Tablets Containing Loxoprofen Sodium by HYDROFLASH Manufacturing Method
Chem Pharm Bull (Tokyo). 2024;72(1):48-55. doi: 10.1248/cpb.c23-00520.ABSTRACTIn order to create and offer superior pharmaceuticals for consumers who wish to be relieved of headache and fever as soon as possible, we established HYDROFLASH manufacturing method that enables us to offer fast disintegration tablets containing loxoprofen sodium (LX), which are difficult to disintegrate. As a result of screening excipients, tablets using mannitol showed the fastest disintegration time, about 2 min. From the result of viscosity measurement, we found that LX produced higher viscosity when dissolved in water. This suggests that tab...
Source: Chemical and Pharmaceutical Bulletin - January 3, 2024 Category: Drugs & Pharmacology Authors: Aya Kuwata Tetsuo Ono Yuri Tsuchiya Etsuo Yonemochi Source Type: research