Chemistry of Antiprotozoal Agents

Chabala, John C.; Miller, Max W.

doi:10.1007/978-1-4684-1233-8_2

Cited by 3 publications

(4 citation statements)

References 100 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…and are currently used as control agents in cattle or poultry (2). A new generation of fluorinated 4-quinolones, with a broad spectrum of antibacterial activity (e.g., enrofloxacin), are currently under development (6).…”

mentioning

confidence: 99%

See 1 more Smart Citation

Inhibition of Cryptosporidium parvum in neonatal Hsd:(ICR)BR Swiss miceby polyether ionophores and aromatic amidines

Blagburn

Sundermann

Lindsay

et al. 1991

Antimicrob Agents Chemother

View full text Add to dashboard Cite

show abstract

mentioning

confidence: 99%

“…The bisamidines (pentamidine and related compounds) are a diverse group of agents with demonstrated parasiticidal activity (2). Pentamidine and its analogs possess a broad spectrum of activity against intracellular and extracellular protozoa and against Pneumocystis carinii (1,9,17).…”

mentioning

confidence: 99%

Inhibition of Cryptosporidium parvum in neonatal Hsd:(ICR)BR Swiss miceby polyether ionophores and aromatic amidines

Blagburn

Sundermann

Lindsay

et al. 1991

Antimicrob Agents Chemother

View full text Add to dashboard Cite

show abstract

“…Another direction in the chemistry of N-arylmaleimides, which is well represented in the literature, is the building of thiomorpholine rings when they interact with 1,4-N,Sbinucleophiles [38,44] (Scheme 14). This framework is a common pharmacophoric element and it exhibits selective enzyme inhibition for many receptors and other types of molecular targets [45][46][47][48][49][50][51].…”

Section: Reactions With S-and O-containing Dinucleophilesmentioning

confidence: 99%

Recyclization of Maleimides by Binucleophiles as a General Approach for Building Hydrogenated Heterocyclic Systems

Vandyshev

Shikhaliev

2022

Molecules

View full text Add to dashboard Cite

The building of heterocyclic systems containing hydrogenated fragments is an important step towards the creation of biologically-active compounds with a wide spectrum of pharmacological activity. Among the numerous methods for creating such systems, a special place is occupied by processes using N-substituted maleimides as the initial substrate. This molecule easily reacts in Diels-Alder/retro-Diels-Alder reactions, Michael additions with various nucleophiles, and co-polymerization processes, as have been described in numerous detailed reviews. However, information on the use of maleimides in cascade heterocyclization reactions is currently limited. This study is devoted to a review and analysis of existing literature data on the processes of recyclization of N-substituted maleimides with various C,N-/N,N-/S,N-di- and polynucleophilic agents, such as amidines, guanidines, diamines, aliphatic ketazines, aminouracils, amino- and mercaptoazoles, aminothiourea, and thiocarbomoyl pyrazolines, among others. The significant structural diversity of the recyclization products described in this study illustrates the powerful potential of maleimides as a building block in the organic synthesis of biologically-active compounds with hydrogenated heterocyclic fragments.

show abstract

“…A comprehensive review of current cryptosporidial research recommended further testing of five agents: alborixin, arprinocid, cyclosporin A, lasalocid, and maduramicin (8). Interestingly, alborixin, maduramicin, and lasalocid are membraneactive polyether ionophores which have been effective in the control of coccidiosis in poultry and cattle (7). These same ionophores have been evaluated against C. parvum in vivo and have demonstrated some efficacy.…”

mentioning

confidence: 99%

Evaluation of maduramicin and alborixin in a SCID mouse model of chronic cryptosporidiosis

Mead

You

Pharr

et al. 1995

Antimicrob Agents Chemother

View full text Add to dashboard Cite

Two polyether ionophores, maduramicin and alborixin, were evaluated for anticryptosporidial activity in a severe combined immune deficient (SCID) mouse model of cryptosporidiosis. Groups of SCID mice were inoculated with 10(6) oocysts of bovine origin by oral gavage. Maduramicin or alborixin was administered beginning 4 weeks postinfection at 3 mg/kg of body weight per day. Maduramicin treatment resulted in a 96% reduction in fecal parasite load over the 3-week treatment period (P < 0.003). This reduction correlated with decreases in tissue parasite loads observed in histological sections of the small intestine (P < 0.000002) and the colon (P < 0.000006). A significant decrease in oocyst shedding was also observed after a 3-week treatment with alborixin (71% reduction, P < 0.01). Maduramicin was also evaluated in a relapsing model of cryptosporidiosis in which the infection was observed to recur after treatments were discontinued. Some toxicity, as demonstrated by weight loss, was observed with both maduramicin and alborixin. Both drugs exhibited significant anticryptosporidial activities with concomitant moderate toxicity. These polyether ionophores should be valuable as positive controls in compound evaluation studies and as lead compounds for chemical optimization (modification).

show abstract

Chemistry of Antiprotozoal Agents

Cited by 3 publications

References 100 publications

Inhibition of Cryptosporidium parvum in neonatal Hsd:(ICR)BR Swiss miceby polyether ionophores and aromatic amidines

Inhibition of Cryptosporidium parvum in neonatal Hsd:(ICR)BR Swiss miceby polyether ionophores and aromatic amidines

Recyclization of Maleimides by Binucleophiles as a General Approach for Building Hydrogenated Heterocyclic Systems

Evaluation of maduramicin and alborixin in a SCID mouse model of chronic cryptosporidiosis

Contact Info

Product

Resources

About