Gandhi, Disha M Rosas, Ricardo Jr Greve, Eric Kentala, Kaitlin D-R Diby, N'Guessan Snyder, Vladyslava A Stephans, Allison Yeung, Teresa H W Subramaniam, Saravanan DiMilo, Elliot
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Published in
Bioorganic & medicinal chemistry
Novel analogs of the allosteric, biased PAR1 ligand ML161 (parmodulin 2, PM2) were prepared in order to identify potential anti-thrombotic and anti-inflammatory compounds of the parmodulin class with improved properties. Investigations of structure-activity relationships of the western portion of the 1,3-diaminobenzene scaffold were performed using...
Suzuki, Toshinori Kishida, Yuki
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Bioorganic & medicinal chemistry
When a neutral solution of thymidine and ascorbic acid was irradiated with UV light of wavelength longer than 300 nm in the presence of salicylic acid as a photosensitizer, six product peaks appeared in an HPLC chromatogram in addition to small amounts of thymidine dimers. The six products were identified as three pairs of diastereomers of 5-(2-deo...
Jeong, Jieun Kim, Kun-Hee Kim, Dong-Young Chandrasekaran, Gopalakrishnan Kim, Minhee Pagire, Suvarna H Dighe, Mahesh Choi, Eun Young Bak, Su-Min Kim, Eun-Young
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Published in
Bioorganic & medicinal chemistry
A new series of 1,3-diketone, heterocyclic and α,β-unsaturated derivatives were synthesized and evaluated for their AhR antagonist activity using zebrafish and mammalian cells. Compounds 1b, 2c, 3b and 5b showed significant AhR antagonist activity in a transgenic zebrafish model. Among them, compound 3b, and 5b were found to have excellent AhR anta...
Suaifan, Ghadeer A R Y Mohammed, Aya A M
Published in
Bioorganic & medicinal chemistry
Fluoroquinolones are considered one of the widely utilized antibiotics, specifically, with the recent development of newer generations such as moxifloxacin, delafloxacin and finafloxacin which possess a wider spectrum of activity and improved bioavailability. However, alarming increase in bacterial resistance reports worldwide incites medicinal che...
Ku, Therese Lopresti, Natalie Shirley, Matthew Mori, Mattia Marchant, Jan Heng, Xiao Botta, Maurizio Summers, Michael F Seley-Radtke, Katherine L
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Bioorganic & medicinal chemistry
Anti-HIV-1 drug design has been notably challenging due to the virus' ability to mutate and develop immunity against commercially available drugs. The aims of this project were to develop a series of fleximer base analogues that not only possess inherent flexibility that can remain active when faced with binding site mutations, but also target a no...
Du, Xinming Qian, Jiawen Wang, Yujie Zhang, Mingming Chu, Yiwei Li, Yingxia
Published in
Bioorganic & medicinal chemistry
Toll-like receptor 2 (TLR2) is a bridge between innate immunity and adaptive immunity. TLR2 agonists have been exploited as potential vaccine adjuvants and antitumor agents. However, no TLR2 agonists have been approved by FDA up to now. To discover drug-like TLR2 selective agonists, a novel series of Pam3CSK4 derivatives were designed based on the ...
Anokhina, Viktoriya S McAnany, John D Ciesla, Jessica H Hilimire, Thomas A Santoso, Netty Miao, Hongyu Miller, Benjamin L
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Bioorganic & medicinal chemistry
Ribosomal frameshifting, a process whereby a translating ribosome is diverted from one reading frame to another on a contiguous mRNA, is an important regulatory mechanism in biology and an opportunity for therapeutic intervention in several human diseases. In HIV, ribosomal frameshifting controls the ratio of Gag and Gag-Pol, two polyproteins criti...
Asawa, Yasunobu Katsuragi, Kiyotaka Sato, Akira Yoshimori, Atsushi Tanuma, Sei-Ichi Nakamura, Hiroyuki
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Bioorganic & medicinal chemistry
A series of carborane-containing NAMPT inhibitors were designed and synthesized based on the structure of compounds 1 and the NAMPT inhibitory activity was evaluated using NAMPT Colorimetric Assay. Among the compounds synthesized, compounds 2b and 2c showed significant NAMPT inhibitory activity with IC50 values of 0.098 ± 0.008 and 0.057 ± 0.001 µM...
Burstein, Sumner H
Published in
Bioorganic & medicinal chemistry
Interactions between cannabinoids and eicosanoids have been observed for the last several decades and account for a variety of cannabinoid actions. These were seen both in vitro and in vivo and may provide a molecular basis for these actions. Some of the topics included in this review are; effects on adenylate cyclase activity, alteration of behavi...
Pereira, Gustavo José Vasco Tavares, Maurício Temotheo Azevedo, Ricardo Alexandre Martins, Barbara Behr Cunha, Micael Rodrigues Bhardwaj, Rajesh Cury, Yara Zambelli, Vanessa Olzon Barbosa, Euzébio Guimarães Hediger, Matthias A
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Published in
Bioorganic & medicinal chemistry
The use of molecules inspired by natural scaffolds has proven to be a very promising and efficient method of drug discovery. In this work, capsaicin, a natural product from Capsicum peppers with antitumor properties, was used as a prototype to obtain urea and thiourea analogues. Among the most promising compounds, the thiourea compound 6g exhibited...
