Development of Novel Biologically Active Compounds Based on Synthetic Organic Chemistry

Abstract

The aging population has had an impact on society in recent decades. Aging-associated health issues are a particularly challenging aspect to regulate. Therefore, the extension of healthy life expectancy by the application of biologically active compounds is an attractive research topic in the ˆelds of medicinal chemistry, chemical biology, and also organic synthesis. Herein, the ˆrst total synthesis of acaulide, acaulone A and 10-keto-acaudiol A is described. These compounds were originally isolated from a culture of Acaulium sp. H-JQSF. Acaulide exhibits anti-osteoporosis activity in a prednisolone-induced osteoporotic zebraˆsh model; hence, this natural product is expected to be a new lead compound for anti-osteoporosis drugs. The characteristic acaulide skeletons were synthesized via late-stage Michael addition inspired by the proposed biosynthetic pathways. The conformational analysis of the 14-membered macrodiolide revealed the speciˆc conformation that enabled the late-stage stereoselective functionalization.

Evaluation of the Effects of Heteroaryl Ethylene Molecules in Combination with Antibiotics: A Preliminary Study on Control Strains

“…These compounds serve as building blocks for designing novel therapeutic agents [ 44 ], targeting previously untreatable diseases. The easy-end versatile synthetic process allows for the optimization of drug properties, such as solubility [ 45 ], stability [ 46 ], and bioavailability [ 47 ], leading to better drug formulations.…”

Computational formulation study of insulin on biodegradable polymers

“… 2 Biologicals are highly specific, whereas synthetic organic agents are likely to cause mild to moderate adverse reactions. 3 Drugs can be administered in various ways, but oral delivery is the most common method due to the ease of compliance of patients. To reap the benefits of oral bioavailability, drugs must pass through the digestive system.…”