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research Synthesis and Evaluation of 2‘-Substituted 4-(4‘-Carboxy- or 4‘-carboxymethylbenzylidene)-N-acylpiperidines: Highly Potent and in Vivo Active Steroid 5α-Reductase Type 2 Inhibitors

22 citations , June 2002 in “Journal of Medicinal Chemistry”

Compounds 15, 20, and 25 are strong inhibitors of human steroid 5α-reductase type 2.

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

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

5 citations , February 1997 in “Bioorganic & Medicinal Chemistry”

New compounds were made that effectively block a specific enzyme related to androgen conditions.

research Novel 5α-Reductase Inhibitors: Synthesis, Structure−Activity Studies, and Pharmacokinetic Profile of Phenoxybenzoylphenyl Acetic Acids

18 citations , December 2005 in “Journal of Medicinal Chemistry”

A brominated phenoxy compound effectively inhibits a human enzyme and shows potential for clinical use.

research The biochemical and phenotypic characterization of females homozygous for 5 alpha-reductase-2 deficiency.

54 citations , November 1995 in “The Journal of Clinical Endocrinology & Metabolism”

Females with 5 alpha-reductase-2 deficiency have less body hair, no acne, normal fertility, and delayed menarche.

research Determination of rat 5α-reductase type 1 isozyme activity and its inhibition by novel steroidal oxazolines

4 citations , August 2010 in “Acta Biologica Hungarica”

New steroidal compounds moderately block an enzyme related to testosterone conversion, less effectively than finasteride.

5-Alpha-Reductase Type 2 Deficiency: Is There a Genotype-Phenotype Correlation? A Review

research 5-α-Reductase type 2 deficiency: is there a genotype-phenotype correlation? A review

39 citations , April 2018 in “Hormones”

No consistent link between genotype and phenotype in 5-α-Reductase type 2 deficiency.

research Synthesis, Biological Evaluation and in silico Studies of Novel 5α-aza-Bhomo-3,5-secosteroids as Potential 5-reductase Inhibitors

October 2016 in “Letters in Drug Design & Discovery”

Attenuation of 5α-Reductase-Mediated Progesterone Metabolism Promotes Differentiation of Human Endometrial Stromal Cells for the Establishment of Pregnancy

research Attenuation of 5α-reductase-mediated progesterone metabolism promotes differentiation of human endometrial stromal cells for the establishment of pregnancy

January 2020 in “Nihon Yakuri Gakkai nenkai yoshishu”

Reducing 5α-reductase activity helps endometrial cells differentiate, aiding pregnancy.

C19 and C21 5β/5α Metabolite Ratios in Subjects Treated with the 5α-Reductase Inhibitor Finasteride: Comparison of Male Pseudohermaphrodites with Inherited 5α-Reductase Deficiency

research C₁₉and C₂₁5β/5αMetabolite Ratios in Subjects Treated with the 5α-Reductase Inhibitor Finasteride: Comparison of Male Pseudohermaphrodites with Inherited 5α-Reductase Deficiency*

55 citations , March 1990 in “The Journal of Clinical Endocrinology and Metabolism”

Finasteride may treat baldness but less effective for those with 5α-reductase deficiency.

research Caffeic acid N-[3,5-bis(trifluoromethyl)phenyl] amide as a non-steroidal inhibitor for steroid 5α-reductase type 1 using a human keratinocyte cell-based assay and molecular dynamics

December 2022 in “Scientific Reports”

Compound 4 is a promising treatment for hair loss with low toxicity.

research Regulation of the metabolic phenotype of human hepatocytes by glucocorticoids and androgens

December 2016 in “University of Birmingham Institutional Research Archive (University of Birmingham)”

Glucocorticoids reduce fat production in liver cells, while androgens increase it in females; manipulating certain enzymes can influence these effects.

research 5α-Reductase Inhibitory Components as Antiandrogens From Herbal Medicine

19 citations , June 2010 in “Journal of acupuncture and meridian studies”

A plant extract was found to effectively block an enzyme related to male hormone-related diseases.

What Is the Role of 5α-Reductase Inhibitors in the Treatment of Androgenetic Alopecia? An Evidence-Based Review

research Qual o papel dos inibidores da 5α-redutase no tratamento da alopecia androgenética? Uma revisão baseada na evidência

March 2020 in “Rpmgf”

5α-reductase inhibitors are effective for treating hair loss in androgenetic alopecia.

New 5α-Reductase Inhibitors: In Vitro and In Vivo Effects

research New 5?-reductase inhibitors: In vitro and in vivo effects

45 citations , February 2005 in “Steroids”

Four new compounds were more effective than finasteride in treating prostate issues and hair loss, with one being 100 times more active and safe for use.

research Control of testosterone 5alpha-reductase activity in the human hyperplastic prostate

January 1978 in “Enlighten: Theses (The University of Glasgow)”

Inhibiting testosterone 5alpha-reductase may help treat benign prostatic hyperplasia.

research Expression, characterization, and structural analysis of human liver delta4-3-ketosteroid 5beta-reductase (AKR1D1) and its disease-related mutant P133R

January 2009 in “ScholarlyCommons (University of Pennsylvania)”

The P133R mutation in AKR1D1 enzyme causes harmful bile acid buildup, explaining related health issues.

research 5α-Reductase Inhibitors – The Finasteride Story

3 citations , October 2010 in “Wiley-VCH Verlag GmbH & Co. KGaA eBooks”

Finasteride safely treats enlarged prostate and male-pattern baldness.

Activity of 17β-(N-Alkyl/Arylformamido) and 17β-[(N-Alkyl/Aryl) Alkyl/Arylamido]-4-Methyl-4-Aza-5α-Androstan-3-Ones as 5α-Reductase Inhibitors in the Hamster Flank Organ and Ear

research Activity of 17β-(N-Alkyl/arylformamido) and 17β-[(N-Alkyl/aryl) alkyl/arylamido]-4-methyl-4-aza-5α-androstan-3-ones as 5α-Reductase Inhibitors in the Hamster Flank Organ and Ear11The research has been supported by Endorecherche that is seeking patent protection for the new compounds. F. Labrie is President of Endorecherche.

10 citations , August 1998 in “Journal of Investigative Dermatology”

The compounds tested could potentially treat hair loss and alopecia.

research Central 5-alpha reduction of testosterone is required for testosterone's inhibition of the hypothalamo-pituitary–adrenal axis response to restraint stress in adult male rats

51 citations , July 2013 in “Brain Research”

Testosterone needs to be converted to DHT to reduce stress response in male rats.

Synthesis and Biological Evaluation of 4-(4-(Alkyl- and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-Steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

research Synthesis and Biological Evaluation of 4-(4-(Alkyl-and Phenylaminocarbonyl)benzoyl)benzoic Acid Derivatives as Non-steroidal Inhibitors of Steroid 5α-Reductase Isozymes 1 and 2

8 citations , March 2002 in “Archiv Der Pharmazie”

The compound 4c effectively inhibits the enzyme linked to hair loss.

A 5α-Reductase Inhibitor, Finasteride, Increases Differentiation and Proliferation of Embryonal Carcinoma Cell-Derived Neural Cells

research A 5α-reductase inhibitor, finasteride, increases differentiation and proliferation of embryonal carcinoma cell-derived-neural cells

4 citations , September 2010 in “Medical Hypotheses”

research In silico structural prediction of human steroid 5α-reductase type II

3 citations , March 2016 in “Medicinal Chemistry Research”

Scientists found out the structure of a human enzyme linked to prostate cancer and hair loss, which could help in designing drugs.

research Null Mutation of 5α-Reductase Type I Gene Alters Ethanol Consumption Patterns in a Sex-Dependent Manner

11 citations , November 2014 in “Behavior Genetics”

research Comparative GC-MS Based In vitro Assays of 5α-Reductase Activity Using Rat Liver S9 Fraction

8 citations , March 2012 in “Mass spectrometry letters”

The S9 fraction with GC-IDMS is effective for measuring 5α-reductase activity.

Chemical Mechanism of the Covalent Modification of 5-Alpha-Reductases by Finasteride as Probed by Secondary Tritium Isotope Effects

research Chemical Mechanism of the Covalent Modification of 5.alpha.-Reductases by Finasteride as Probed by Secondary Tritium Isotope Effects

12 citations , March 1995 in “Journal of the American Chemical Society”

Finasteride modifies 5-alpha-reductases through a two-step process, affecting inhibitor potency and possibly causing side effects.

research 5α Reductase Deficiency—a Rare Cause of Ambiguous Genitalia and Gender Dysphoria

1 citations , October 2024 in “JCEM Case Reports”

5α-reductase deficiency can cause ambiguous genitalia and gender dysphoria, treatable with testosterone.

research In Silico Screening of DrugBank Compounds as Potential Inhibitors for Human Steroid 5α-Reductase 2 for Androgen-Related Diseases

December 2023 in “Biointerface Research in Applied Chemistry”

Stiripentol shows promise as a potential treatment for androgen-related diseases but needs more testing.

research Generation of comparative pharmacophoric model for steroidal 5α-reductase I and II inhibitors: A 3D-QSAR study on 6-azasteroids

13 citations , January 2015 in “Steroids”

The study created a model to help design new inhibitors for steroidal 5α-reductase enzymes.

Methylated CpG Dinucleotides in 5-Alpha Reductase 2 Gene Might Explain the Finasteride-Resistance in BPE Patients

research Methylated CpG dinucleotides in 5-α reductase 2 gene might explain the finasteride-resistance in BPE patients

July 2020 in “European urology open science”

Methylated gene parts may cause finasteride-resistance in some enlarged prostate patients.

research Synthesis, Characterization and Evaluation of 5α, 6β-Dihalo Androsterone Derivatives as 5α-Reductase Inhibitors

May 2022 in “Current Enzyme Inhibition”

Compound 7b is a promising candidate for treating benign prostatic hyperplasia and prostate cancer.

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