research Design and synthesis of novel Azasteroids and Pseudoazulenyl nitrones
This review explores the synthesis and potential of azasteroids as novel drugs, discussing challenges in their production and reporting no new clinical results.
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30 / 1000+ results research 13C-NMR study of 4-azasteroids in solution and solid state
This study examined 4-azasteroids using 13C-NMR spectroscopy, detailing the NMR spectrum assignments and reporting a new molecular complex of finasteride with dioxane.
research Direct access to novel chromeno-pyrimidine-N-oxides via tandem base catalyzed double nucleophilic addition/dehydration reaction
This study reports a new one-pot method for synthesizing chromeno-pyrimidine-N-oxides with high yield from 4-chloro-3-formylcoumarin and aromatic carboximide oximes, confirmed by X-ray analysis.
![Synthesis and In Vitro Study of 17β-[N-Ureylene-N,N′-Disubstituted]-4-Methyl-4-Aza-5α-Androstan-3-Ones as Selective Inhibitors of Type I 5α-Reductase](/images/assets/d19df8a7-8de6-4430-8a0d-4ffa1f502985/small/15608.jpg)
research Synthesis and in vitro study of 17β-[N-ureylene-N,N′-disubstituted]-4-methyl-4-aza-5α-androstan-3-ones as selective inhibitors of type I 5α-reductase
This study found that among 17 beta-(N-ureylene-N,N'-disubstituted)-4-azasteroids, those with an N'-phenyl moiety were the most effective inhibitors of human type I 5 alpha-reductase.
research Alternative synthesis of the anti-baldness compound RU58841
A new, less toxic and more efficient method to create the anti-baldness compound RU58841 was developed in 2014.
research Synthesis of 4-amidinoimidazoles incorporating a cyanamide moiety : novel precursors for biologically important purines
research Design, Synthesis, and Evaluation of Aryl Hydantoins and Ureas as Antischistosomal Agents
This study identified AH01 derivatives and related compounds with high antischistosomal efficacy and reduced antiandrogenic effects, suggesting potential new directions for schistosomiasis drug development.
research 3a-Phenylhexahydropentalene-1,6-dione
In this study, researchers successfully synthesized a rigid 3a-arylhexahydropentalene-1,6-dione from the easily accessible starting material cyclopent-2-en-1-one, highlighting a structural motif common in natural products and pharmaceuticals.
research Synthetic Approaches for Pharmacologically Active Decorated Six-Membered Diazines
This chapter reviews various synthetic methods for creating pharmacologically active diazines, particularly focusing on pyrimidines, and discusses their potential in clinical applications. It also examines novel synthetic strategies that improve the drug-like qualities and safety profiles of these compounds.
research Rational Design and Synthesis of 4-((1R,2R)-2-Hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a Novel, Nonsteroidal Androgen Receptor Antagonist Devoid of Phototoxicity for Dermatological Indications
This study suggests that PF-0998425 is an effective androgen receptor antagonist for sebum control and androgenetic alopecia with rapid metabolism reducing the risk of systemic side effects.
research Breaking the ‘rule-of-five’ to access bridged bicyclic heteroaromatic bioisosteres
In this study, researchers introduced a visible-light-mediated intramolecular cycloaddition method that selectively forms 6-azabicyclo[3.1.1]heptanes, suggesting these structures could offer promising new scaffolds for drug discovery and medicinal chemistry.
research Aromatic C-nitrosation of a bioactive molecule. Nitrosation of minoxidil
Minoxidil reacts to nitrosation 7 times more than phenol, mainly due to its -NH₂ groups, leading to the creation of N-nitrosominoxidil.
research New Nonsteroidal Molecules as Blockers of the Steroidogenic Pathway
This study found that two novel nonsteroidal derivatives inhibited specific enzymes in vitro and in vivo, leading to dihydrotestosterone accumulation in androgen-dependent glands, suggesting potential therapeutic use for mood improvement in the elderly.
research Ultrasound-Assisted Facile Synthesis and Anticancer Evaluation of Novel N-(2-substituted phenyl-4-oxathiazolidine-3-carbonothioyl) benzamide
This study found that four synthesized thiazolidinone derivatives showed potential anticancer activity against MCF7 and HeLa cell lines, suggesting their further investigation for anticancer drug development.
research Atroposelective Synthesis of Biaryl N‐Oxides via Cu‐Catalyzed De Novo Heteroaromatic N‐Oxide Ring Formation
This study presents a Cu-catalyzed atroposelective method achieving high stereoselectivity for synthesizing chiral biaryl N-oxides, with product 3e showing promising therapeutic efficacy against triple-negative breast cancer in cell lines MDA-MB-231 and MDA-MB-468.
research Synthesis and structure–activity studies of side-chain derivatized arylhydantoins for investigation as androgen receptor radioligands
This study identified the N-(iodopropenyl) derivative 13 as a promising candidate for development as a radioiodinated androgen receptor ligand due to its binding affinity.
research Synthesis, Anticancer and Molecular Docking Studies of 2-(4-chlorophenyl)-5-aryl-1,3,4-Oxadiazole Analogues
This study reported that among 10 tested 2-(4-chlorophenyl)-5-aryl-1,3,4-oxadiazole compounds, compound 4c showed the highest activity against cancer cell lines, with a 95.37% average growth rate.
research Breaking the “rule-of-five” to access Bridged Bicyclic Heteroaromatic Bioisosteres
This study introduces a novel visible light-mediated intramolecular [2+2] cycloaddition process that forms 6-azabicyclo[3.1.1]heptanes, offering a new synthesis route for bioisosteric mimetics used in drug discovery, potentially expanding medicinal chemistry applications beyond traditional limitations.
research Novel azaandrostane derivatives for the synthesis of 17β‐(N‐tert‐butyl carbamoyl)‐4‐aza‐5α‐androst‐1‐ene‐3‐one
This study reports a new industrial process for making finasteride using novel protective groups, demonstrated through spectral data of newly prepared compounds.
research 267 Single- and multiple-ascending dose studies of DS-2325a, a KLK5 inhibitor for the treatment of Netherton syndrome
In these two clinical trials, DS-2325a, a KLK5 inhibitor, was found to be generally safe and well tolerated in healthy volunteers, with mild and non-serious adverse events, suggesting its potential for further development as a treatment for Netherton Syndrome.
research Development, Optimization, and In Vitro/In Vivo Evaluation of Azelaic Acid Transethosomal Gel for Antidermatophyte Activity
This study found that azelaic acid entrapped in transethosomes exhibited enhanced antidermatophyte activity and improved treatment outcomes in guinea pig models of dermatophytosis compared to free azelaic acid.
research Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents
This review discusses three classes of thiazole-bearing compounds in drug development and presents preclinical findings but reports no new experimental results, highlighting the need for further drug discovery.
research Metabolite screening of aromatic amine hair dyes usingin vitrohepatic models
This study found no evidence that the tested hair dye ingredients undergo hepatic metabolism to reactive oxidized metabolites in human liver microsomes and hepatocytes.
research Synthesis and 5α-Reductase Inhibitory Activity of C21 Steroids Having 1,4-diene or 4,6-diene 20-ones and 4-Azasteroid 20-Oximes
This study reported that while no synthesized compounds surpassed finasteride in 5α-reductase inhibitory activity, certain 4-azasteroid-2-oximes exhibited notable inhibition.
research ZnO@PDA@Ag Nanocomposite-Mediated Delivery of 9-Bromonoscapine, an Anticancer Agent, for Enhanced Lung Cancer Therapy
In this study, a biocompatible zinc oxide nanocomposite loaded with the anticancer drug 9-Br-Nos demonstrated effective drug delivery and cytotoxicity against lung cancer cells in vitro, while also proving non-toxic to healthy cells, suggesting its potential for targeted lung cancer treatment.
research BindingDB Entry 50021519: Discovery of (2S)-N-(6-Cyano-5-(trifluoromethyl)pyridin-3-yl)-3-(6-(4-cyanophenyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)-2-hydroxy-2-methylpropanamide as a Highly Potent and Selective Topical Androgen Receptor Antagonist for Androgenetic Alopecia Treatment.
research Functionalization of Alkenes with Difluoromethyl Nitrile Oxide to Access the Difluoromethylated Derivatives
This study reports that difluoromethyl nitrile oxide can rapidly functionalize various alkenes at room temperature, leading to products that can transform into valuable medicinal chemistry building blocks like CF2H-isoxazolines for bioactive molecule modification.
research Preparation, Characterization and Molecular Docking Study of some New Pyrazole Derivatives Derived from 2-Mercaptobenzothiazole.
This study found that certain pyrazole derivatives may serve as effective 5α-reductase inhibitors with potential use in the treatment of androgenetic alopecia, based on molecular docking analyses.
research Acute and 30-day oral toxicity studies of a novel coccidiostat – ethanamizuril
In this study, ethanamizuril was found to cause alopecia, biochemical changes, and organ damage at higher doses in rats, with a no-observed-adverse-effect level of 20 mg/kg over 30 days.