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1.
BMC Womens Health ; 22(1): 526, 2022 12 17.
Article in English | MEDLINE | ID: mdl-36528558

ABSTRACT

BACKGROUND: Endometriosis is a complex chronic disease that affects approximately 10% of women of reproductive age worldwide and commonly presents with pelvic pain and infertility. METHOD & OUTCOME MEASURES: A systematic review of the literature was carried out using the databases Pubmed, Scopus, Cochrane and ClinicalTrials.gov in women with a confirmed laparoscopic diagnosis of endometriosis receiving progestins to determine a reduction in pain symptoms and the occurrence of adverse effects. RESULTS: Eighteen studies were included in the meta-analysis. Progestins improved painful symptoms compared to placebo (SMD = -0.61, 95% CI (-0.77, -0.45), P < 0.00001) with no comparable differences between the type of progestin. After median study durations of 6-12 months, the median discontinuation rate due to adverse effects was 0.3% (range: 0 - 37.1%) with mild adverse effects reported. CONCLUSION: The meta-analysis revealed that pain improvement significantly increased with the use of progestins with low adverse effects. SYSTEMATIC REVIEW REGISTRATION: PROSPERO CRD42021285026.


Subject(s)
Endometriosis , Laparoscopy , Female , Humans , Endometriosis/complications , Endometriosis/drug therapy , Endometriosis/diagnosis , Pelvic Pain/drug therapy , Pelvic Pain/etiology , Progestins/therapeutic use
2.
Bioorg Med Chem Lett ; 27(3): 460-465, 2017 02 01.
Article in English | MEDLINE | ID: mdl-28027871

ABSTRACT

In an endeavor to develop efficacious antiprotozoal agents 4-(7-chloroquinolin-4-yl) piperazin-1-yl)pyrrolidin-2-yl)methanone derivatives (5-14) were synthesized, characterized and biologically evaluated for antiprotozoal activity. The compounds were screened in vitro against the HM1: IMSS strain of Entamoeba histolytica and NF54 chloroquine-sensitive strain of Plasmodium falciparum. Among the synthesized compounds six exhibited promising antiamoebic activity with IC50 values (0.14-1.26µM) lower than the standard drug metronidazole (IC50 1.80µM). All nine compounds exhibited antimalarial activity (IC50 range: 1.42-19.62µM), while maintaining a favorable safety profile to host red blood cells. All the compounds were less effective as an antimalarial and more toxic (IC50 range: 14.67-81.24µM) than quinine (IC50: 275.6±16.46µM) against the human kidney epithelial cells. None of the compounds exhibited any inhibitory effect on the viability of Anopheles arabiensis mosquito larvae.


Subject(s)
Antiprotozoal Agents/chemical synthesis , Chloroquine/chemistry , Piperazines/chemistry , Antimalarials/chemistry , Antimalarials/pharmacology , Antiprotozoal Agents/chemistry , Antiprotozoal Agents/pharmacology , Binding Sites , Cell Line , Cell Survival/drug effects , Entamoeba histolytica/drug effects , Erythrocytes/drug effects , Humans , Inhibitory Concentration 50 , Molecular Docking Simulation , Piperazine , Plasmodium falciparum/drug effects , Protein Structure, Tertiary , Protozoan Proteins/chemistry , Protozoan Proteins/metabolism , Structure-Activity Relationship , Thioredoxin-Disulfide Reductase/chemistry , Thioredoxin-Disulfide Reductase/metabolism
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