The aim of this work was to develop lead pharmacodynamic hybrids, NO-sartans, possessing the characteristics of a typical AT1-antagonist and of a "slow NO donor", by adding NO-donor side chains to losartan. These new compounds, 2a and 2b, displayed vasorelaxing effects, due to the release of NO, and antagonized the vasocontractile effects of angiotensin II, with potency values similar to that of losartan. In vivo, the antihypertensive effects of 2a were similar to those of losartan and captopril.
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http://dx.doi.org/10.1021/jm049681p | DOI Listing |
J Med Chem
January 2025
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
The tedious synthesis and limited throughput biological evaluation remain a great challenge for discovering new proteolysis targeting chimera (PROTAC). To rapidly identify potential PROTAC lead compounds, we report a platform named Auto-RapTAC. Based on the modular characteristic of the PROTAC molecule, a streamlined workflow that integrates lab automation with "click chemistry" joint building-block libraries was constructed.
View Article and Find Full Text PDFPLoS One
January 2025
Department of ENT, Head and Neck Surgery, Sri Ramachandra Institute of Higher Education and Research (Deemed to be University), Chennai, Tamil Nadu, India.
J Enzyme Inhib Med Chem
December 2025
Department of Organic Chemistry, Medical University of Lublin, Lublin, Poland.
The ever-increasing drug-resistant tuberculosis (TB) has invigorated the focus on the discovery and development of novel therapeutic agents and treatment options. Thiazolidinone-based compounds have shown good antitubercular properties . Here, we report the design and synthesis of a number of new derivatives inspired by the structure of thiazolidine-2,4-dione (TZD).
View Article and Find Full Text PDFZhongguo Ying Yong Sheng Li Xue Za Zhi
January 2025
Department of Life Science, SSSUHE, Kalaburagi, Karnataka, India.
The aim of this study is to explore and evaluate recent innovations in drug delivery systems (DDS) for biologics, focusing on enhancing stability and targeted delivery to improve the efficacy and safety of next-generation therapeutics. The most recent developments in a variety of DDS, such as nanoparticles, microneedles, hydrogels, and biodegradable polymers, were examined in depth. Information from peer-audited diaries, clinical preliminaries, and mechanical reports were blended to survey the presentation of these frameworks concerning dependability, designated conveyance, patient consistence, and controlled discharge.
View Article and Find Full Text PDFSci Rep
January 2025
Institute of Visual Informatics, Universiti Kebangsaan Malaysia, 43600, Bangi, Selangor, Malaysia.
Worldwide, Cancer remains a significant health concern due to its high mortality rates. Despite numerous traditional therapies and wet-laboratory methods for treating cancer-affected cells, these approaches often face limitations, including high costs and substantial side effects. Recently the high selectivity of peptides has garnered significant attention from scientists due to their reliable targeted actions and minimal adverse effects.
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