Large doses of stimulatory analogues of luteinizing hormone-releasing hormone (LH-RH) caused paradoxical antifertility effects. These effects are being utilized for the possible development of contraceptive methods. Several inhibitory analogues of LH-RH have been tested in men and women and shown to be active. The synthetic approach based on inhibitory analogues of LH-RH has been proven to be feasible for development of new methods of birth control. Continued research and testing along these lines may lead to the development of contraceptives based on inhibitory analogues of LH-RH that could be conveniently applied as a nasal spray and could be free of undesirable side effects.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1002/j.1879-3479.1980.tb00507.x | DOI Listing |
Chem Biol Drug Des
January 2025
Laboratory of Natural Product Chemistry, Department of Pharmacy, Birla Institute of Technology and Science, Pilani (BITS Pilani), Pilani, Rajasthan, India.
A set of coumarin-3-carboxamide analogues were designed, synthesized, and evaluated for their ability to impede pancreatic lipase (PL) activity. Out of all the analogues, 5dh and 5de demonstrated promising inhibitory activity against PL, as indicated by their respective IC values of 9.20 and 11.
View Article and Find Full Text PDFChem Biol Drug Des
January 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Target cyclooxygenase 2 (COX-2) and 5-lipoxygenase (5-LOX) inhibitors; 5-([2,5-Dihydroxybenzyl]amino)salicylamides (Compounds 1-11) were examined for potential anticancer activity, with a trial to assess the underlying possible mechanisms. Compounds were assessed at a single dose against 60 cancer cell lines panel and those with the highest activity were tested in the five-dose assay. COMPARE analysis was conducted to explore potential mechanisms underlying their biological activity.
View Article and Find Full Text PDFBioorg Chem
January 2025
Anhui Province Key Laboratory of Bioactive Natural Products, School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012 China; Science & Technology Industrial Parks of Anhui University of Chinese Medicine, Hefei 230012 China. Electronic address:
Eleven cytochalasans (1-11), including six undescribed analogues (1-3 and 5-7) and a new natural product (4), were obtained from the endophytic fungus Boeremia exigua. Their structures and absolute configurations were determined by a combination of extensive spectroscopic techniques, electron circular dichroism (ECD), and single-crystal X-ray diffraction. Boerelasin E (1) represented the first cytochalasan possessing a cis-configured Δ double bond.
View Article and Find Full Text PDFPharmaceuticals (Basel)
January 2025
Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka 72388, Saudi Arabia.
Fructose-driven metabolic disorders, such as obesity, non-alcoholic fatty liver disease (NAFLD), dyslipidemia, and type 2 diabetes, are significant global health challenges. Ketohexokinase C (KHK-C), a key enzyme in fructose metabolism, is a promising therapeutic target. α-Mangostin, a naturally occurring prenylated xanthone, has been identified as an effective KHK-C inhibitor, prompting exploration of its analogs for enhanced efficacy.
View Article and Find Full Text PDFMolecules
January 2025
Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Trg Marka Marulića 19, HR-10 000 Zagreb, Croatia.
Considering our previous experience in the design of new cholinesterase inhibitors, especially resveratrol analogs, in this research, the basic stilbene skeleton was used as a structural unit for new carbamates designed as potentially highly selective butyrylcholinesterase (BChE) inhibitors with excellent absorption, distribution, metabolism, excretion and toxicity ADMET properties. The inhibitory activity of newly prepared carbamates - was tested toward the enzymes acetylcholinesterase (AChE) and BChE. In the tested group of compounds, the leading inhibitors were and , which achieved excellent selective inhibitory activity for BChE with IC values of 0.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!