ArticleInternational journal of antimicrobial agents2010
Candidate vaginal microbicides with activity against Chlamydia trachomatis and Neisseriagonorrhoeae.
Article in International journal of antimicrobial agents, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 33 citations in OpenAlex.
- Combination of compound screening with an animal model identifies pentamidine to prevent Chlamydia trachomatis infection.Cell reports. Medicine · 2024Article
- Anti-Virulence Therapeutic Approaches forAntibiotics (Basel, Switzerland) · 2021Review
- Attenuation ofVirulence · 2020Article
- Lactoferrin in Aseptic and Septic Inflammation.Molecules (Basel, Switzerland) · 2019Review
- Aminomethyl Spectinomycins as Therapeutics for Drug-Resistant Gonorrhea and Chlamydia Coinfections.Antimicrobial agents and chemotherapy · 2018Article
- The salicylidene acylhydrazide INP0341 attenuates Pseudomonas aeruginosa virulence in vitro and in vivo.The Journal of antibiotics · 2017Article
- In Vitro Activity of Quaternary Ammonium Surfactants against Streptococcal, Chlamydial, and Gonococcal Infective Agents.Antimicrobial agents and chemotherapy · 2016Article
- A small-molecule compound belonging to a class of 2,4-disubstituted 1,3,4-thiadiazine-5-ones suppresses Salmonella infection in vivo.The Journal of antibiotics · 2016Article
- N-acylated derivatives of sulfamethoxazole and sulfafurazole inhibit intracellular growth of Chlamydia trachomatis.Antimicrobial agents and chemotherapy · 2014Article
- Formulation of the microbicide INP0341 for in vivo protection against a vaginal challenge by Chlamydia trachomatis.PloS one · 2014Article
- Small-molecule inhibitors suppress the expression of both type III secretion and amylovoran biosynthesis genes in Erwinia amylovora.Molecular plant pathology · 2014Article
- Cytosporone B, an inhibitor of the type III secretion system of Salmonella enterica serovar Typhimurium.Antimicrobial agents and chemotherapy · 2013Article
- Article
- In vitro anti-HIV-1 activity of salicylidene acylhydrazide compounds.International journal of antimicrobial agents · 2012Article
- Pre-clinical pharmacokinetics and anti-chlamydial activity of salicylidene acylhydrazide inhibitors of bacterial type III secretion.The Journal of antibiotics · 2012Article
- Protection of mice from a Chlamydia trachomatis vaginal infection using a Salicylidene acylhydrazide, a potential microbicide.The Journal of infectious diseases · 2011Article
- Identification of bacterial target proteins for the salicylidene acylhydrazide class of virulence-blocking compounds.The Journal of biological chemistry · 2011Article
- Synthesis of [4-(2-hydroxyphenyl)thiazol-2-yl]methanones as potential bioisosteres of salicylidene acylhydrazides.Molecules (Basel, Switzerland) · 2010Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
Abstract
Vaginal microbicides with activity towards organisms that cause sexually transmitted infections have been proposed as a strategy to reduce transmission. Small-molecule inhibitors of Chlamydia trachomatis serovar D belonging to the class of salicylidene acylhydrazides (INPs) have been shown to work through a mechanism that involves iron restriction. Expanding on this work, ten INPs were tested against a lymphogranuloma venereum strain of C. trachomatis (serovar L2), Neisseria gonorrhoeae, and hydrogen peroxide-producing Lactobacillus crispatus and Lactobacillus jensenii. Seven INPs had minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations of <50 microM towards C. trachomatis L2. Three INPs had a MIC <12.5 microM against N. gonorrhoeae. Inhibition was reversed by iron, holo-transferrin and holo-lactoferrin but not by the iron-poor forms of these compounds. The compounds exhibited no bactericidal activity toward Lactobacillus. The INPs were not cytotoxic to HeLa 229 cells. When INP 0341 was tested in a mouse model of a Chlamydia vaginal infection there was a significant reduction in the number of mice shedding C. trachomatis up to 4 days after infection (P<0.01). In summary, select INPs are promising vaginal microbicide candidates as they inhibit the growth of two common sexually transmitted organisms in vitro, are active in a mouse model against C. trachomatis, are not cytotoxic and do not inhibit organisms that compose the normal vaginal flora.
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