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Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)

research Verification of the Major Metabolic Oxidation Path for the Naphthoyl Group in Chemoattractant Receptor-Homologous Molecule Expressed on Th2 Cells (CRTh2) Antagonist 2-(2-(1-Naphthoyl)-8-fluoro-3,4-dihydro-1H-pyrido[4,3-b]indol-5(2H)-yl)acetic Acid (Setipiprant/ACT-129968)

6 citations , September 2015 in “Journal of Medicinal Chemistry”

The document confirms the structures of major metabolites of the CRTh2 antagonist Setipiprant and identifies minor metabolites.

research Dipyridamole-Associated Shock and Pulmonary Edema; Oxcarbazepine-Induced Resistant Ventricular Fibrillation; Finasteride-Induced Pseudoporphyria; Suicidal Ideation Associated with Asenapine; Rediscovering Adverse Anticholinergic Effects; Prevalence of Adverse Drug Events in Ambulatory Care

1 citations , October 2011 in “Hospital Pharmacy”

research Development, Optimization, and In Vitro/In Vivo Evaluation of Azelaic Acid Transethosomal Gel for Antidermatophyte Activity

19 citations , April 2023 in “Antibiotics”

Azelaic acid in a special gel is more effective against skin fungi than regular azelaic acid.

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.

January 2025

Preliminary Pharmacokinetics and Metabolism of Novel Non-Steroidal Antiandrogens in the Rat: Relation of Their Systemic Activity to the Formation of a Common Metabolite

research Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: Relation of their systemic activity to the formation of a common metabolite

16 citations , October 1994 in “The Journal of Steroid Biochemistry and Molecular Biology”

Two non-steroidal antiandrogens, RU 58841 and RU 56187, form a common metabolite at different rates, which may influence their effects; RU 56187 could be used for prostate cancer treatment and RU 58841 for acne treatment.

research Efficacy and tolerability of azathioprine for neuromyelitis optica spectrum disorder: A systematic review and meta-analysis

54 citations , May 2019 in “Multiple Sclerosis and Related Disorders”

Azathioprine can help with relapses and disability in NMOSD but has more side effects and needs more research.

FeCl3-Catalyzed C-N Coupling Reaction Between Cyclic Ethers and Heterocyclic Amines

research FeCl3-catalysed C-N coupling reaction between cyclic ethers and heterocyclic amines

4 citations , December 2014 in “European Journal of Chemistry”

Iron chloride helps create compounds that could be useful in medicine, like treating hair loss.

research 5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives

26 citations , October 2011 in “International Journal of Biological Macromolecules”

Some newly made compounds are promising for treating enlarged prostate, hair loss, viruses, and prostate cancer, and might be better than current drugs.

research Azathioprine‐induced severe myelosuppression accompanied by massive hair loss and painful oral ulcer in an autoimmune hepatitis patient with NUDT15 minor variant: A case report

3 citations , August 2021 in “Clinical Case Reports”

Genetic testing is crucial before giving azathioprine to avoid severe side effects.

research Four-amino acid segment in steroid 5 alpha-reductase 1 confers sensitivity to finasteride, a competitive inhibitor.

83 citations , April 1992 in “Journal of Biological Chemistry”

Four-amino acid part makes enzyme sensitive to finasteride.

research Preparation, physicochemical and clinical evaluation of aminexil niosome in prevention of androgenetic alopecia

January 2019

Niosomes improve aminexil's effectiveness in preventing hair loss without needing propylene glycol.

Natural Bisbenzylisoquinoline Derivatives Protect Zebrafish Lateral Line Sensory Hair Cells from Aminoglycoside Toxicity

research Natural Bizbenzoquinoline Derivatives Protect Zebrafish Lateral Line Sensory Hair Cells from Aminoglycoside Toxicity

44 citations , March 2016 in “Frontiers in cellular neuroscience”

Some natural compounds can protect fish ear cells from damage by certain antibiotics without affecting the antibiotics' ability to fight infections.

research 17-Oximino-5-androsten-3β-yl esters: synthesis, antiproliferative activity, acute toxicity, and effect on serum androgen level

7 citations , August 2010 in “Medicinal Chemistry Research”

Some synthesized compounds were more effective than Finasteride in reducing prostate cancer cell growth and androgen levels.

research Case report: NUDT15 polymorphism and severe azathioprine-induced myelosuppression in a young Chinese female with systematic lupus erythematosus: a case analysis and literature review

1 citations , May 2023 in “Frontiers in Pharmacology”

Genetic screening for NUDT15 polymorphisms is crucial for patients taking azathioprine, especially in Asians.

research NUDT15,FTO, andRUNX1genetic variants and thiopurine intolerance among Japanese patients with inflammatory bowel diseases

40 citations , January 2017 in “Intestinal Research”

Genotyping for NUDT15 p.Arg139Cys can help predict thiopurine side effects in Japanese IBD patients.

research New approach to 3-oxo-4-aza-5α-androst-1-ene-17β-(--butylcarboxamide)

14 citations , May 2005 in “Steroids”

A new method was developed to make finasteride for treating hair loss.

research Computational Evaluation of Dibenzo Compounds as Potential Dual Inhibitors of Androgen Receptor and 5α-Reductase

January 2022 in “Asian journal of Current Research in Clinical Cancer”

Some dibenzo compounds might help treat cancer with fewer side effects.

research Glyburide blocks the relaxation response to BRL 34915 (cromakalim), minoxidil sulfate and diazoxide in vascular smooth muscle.

90 citations , January 1989 in “PubMed”

research Modulation of the 6-position of benzopyran derivatives and inhibitory effects on the insulin releasing process

13 citations , May 2011 in “Bioorganic & Medicinal Chemistry”

Changing the 6-position on benzopyran molecules affects insulin release, with some compounds showing strong inhibitory effects.

4-(Alkylthio)- and 4-(Arylthio)-Benzonitrile Derivatives as Androgen Receptor Antagonists for the Topical Suppression of Sebum Production

research 4-(Alkylthio)- and 4-(arylthio)-benzonitrile derivatives as androgen receptor antagonists for the topical suppression of sebum production

11 citations , March 2009 in “Bioorganic & Medicinal Chemistry Letters”

Chemicals called 4-(alkylthio)- and 4-(arylthio)-benzonitrile derivatives can potentially reduce oil production on skin, which could help treat conditions like acne and hair loss.

research 3a-Phenylhexahydropentalene-1,6-dione

March 2026 in “Molbank”

A rigid compound with a common structural motif was successfully synthesized.

research Sulfur Containing Tyrosine Analogs Can Cause Selective Melanocytotoxicity Involving Tyrosinase-Mediated Apoptosis

16 citations , September 1999 in “Journal of Investigative Dermatology Symposium Proceedings”

research Steroid 5α-Reductase Inhibitors

42 citations , May 2003 in “Mini-reviews in Medicinal Chemistry”

New steroidal compounds could be effective for treating conditions related to 5α-reductase enzyme activity.

research P56 Azathioprine-induced alopecia totalis and knuckle hyperpigmentation in a child with uveitis: test before you leap!

November 2024 in “Rheumatology Advances in Practice”

Monitor for early signs of azathioprine toxicity and check blood counts regularly.

Structural Requirements of Minoxidil Analogs for Enhancing Lysyl Hydroxylase Inhibitory Activity

research An overview on 5α-reductase inhibitors

219 citations , October 2009 in “Steroids”

5α-reductase inhibitors, like Finasteride and Dutasteride, help manage benign prostatic hyperplasia.

research Comparison of Different Alpha-blocker Combinations in Male Hypertensives with Refractory Lower Urinary Tract Symptoms

8 citations , January 2011 in “Korean Journal of Andrology”

The doxazosin plus tamsulosin combination improved symptoms effectively with fewer side effects.

research 3,3-Diphenylpentane skeleton as a steroid skeleton substitute: Novel inhibitors of human 5α-reductase 1

13 citations , August 2007 in “Bioorganic & medicinal chemistry letters”

A new compound effectively inhibits human 5α-reductase 1.

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