This site uses cookies and related technologies, as described in our privacy policy, for purposes that may include site operation, analytics, enhanced user experience, or advertising. You may choose to consent to our use of these technologies, or refuse these technologies

Based on structure–activity relationship analysis, compound with a simplified structure but excellent antifouling activities was synthesized

2023-07-17

Page View：

Biofouling poses one of the most serious problems to marine industry and aquaculture development. Five structurally similar compounds were isolated from the crude extract of a marine Streptomyces strain. Antifouling activities of these compounds and four other structurally-related compounds isolated from another marine Streptomyces species were compared to generate structure–activity relationship data. Based on structure–activity relationship analysis, another compound with a simplified structure but excellent antifouling activities was synthesized. The optimized compound was synthesized by Medicilon.

Reference:

Ying Xu, et al. Potent antifouling compounds produced by marine Streptomyces. Bioresour Technol. 2010 Feb;101(4):1331-6. doi: 10.1016/j.biortech.2009.09.046.

Synthetic-Chemistry drugdiscovery medicilon

Return

Relevant News

TAK-931 is a cancer therapeutic with a unique mechanism of action. Antitumor efficacy studies for TAK-931 were carried out at Medicilon

2023-08-21

Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell division cycle 7 (CDC7) has attracted attention as a target. Researchers have developed an oral CDC7-selective inhibitor, TAK-931, as a candidate clinical anticancer drug. TAK-931 demonstrated marked, dose-dependent antitumor activity, without severe body weight loss. Antitumor efficacy studies for TAK-931 were carried out in two pancreatic PDX models, PHTX-249Pa and PHTXM-97Pa, at Medicilon.

Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon

2023-07-11

Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.

Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon

2023-07-11

The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.