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Comparison of the Pharmacokinetics of Albendazole and its Major Metabolites after Oral Administration of Albendazole as a Suspension and as a Paste Formulation to Sheep

Comparison of the Pharmacokinetics of Albendazole and its Major Metabolites after Oral Administration of Albendazole as a Suspension and as a Paste Formulation to Sheep

Albendazole is a member of the benzimidazole group of anthelmintics with broad-spectrum activity against gastro-intestinal roundworms including inhibited larval stages, tapeworms, liver flukes and lungworms in many species. In the […]

Discovery and optimisation of 1-acyl-2-benzylpyrrolidines as potent dual orexin receptor antagonists

Discovery and optimisation of 1-acyl-2-benzylpyrrolidines as potent dual orexin receptor antagonists

The vertebrate orexin neuropeptide–receptor system plays a pivotal role in the regulation of sleep and wake states as well as emotional states related to stress or reward. The neuropeptides orexin […]

Small-molecule modulators of the Sonic Hedgehog signaling pathway

Small-molecule modulators of the Sonic Hedgehog signaling pathway

Small-molecule modulators of the Sonic Hedgehog signaling pathway Shh pathway inhibition with non-naturally occurring small molecules Cell-based assays with reporter gene constructs have been widely used for discovering non-naturally occurring […]

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

Design and discovery of 3-aryl-5-substituted-isoquinolin-1-ones as potent tankyrase inhibitors

The ADP-ribosyltranferase diphtheria toxin-like (ARTD) or poly-ADP-ribose polymerase (PARP) protein superfamily comprises 17 proteins that contain a common catalytic domain. Those that are catalytically active use β-NAD+ as an essential […]

HPLC-DAD-MSn analysis and HPLC quantitation of chemical constituents in the traditional Chinese medicine formula Ya-tong-yi-li-wan

HPLC-DAD-MSn analysis and HPLC quantitation of chemical constituents in the traditional Chinese medicine formula Ya-tong-yi-li-wan

Ya-tong-yi-li-wan (YTYLW) is a well-known traditional Chinese medicine (TCM) formula composed of ChanSu (toad venom), licorice root, realgar, and cinnabaris in the ratio of 24 : 24 : 6 : […]

Recent advances in the synthesis of new glycopeptide antibiotics

Recent advances in the synthesis of new glycopeptide antibiotics

  Semi-synthetic glycopeptide antibiotics   Oritavancin, telavancin and dalbavancin   Early studies by Nagarajan et al. into the development of semi-synthetic glycopeptide antibiotics focused on utilizing vancomycin as a structural […]

Design and Synthesisof Gramicidin S Analogs with High Antibiotic Activity

Design and Synthesisof Gramicidin S Analogs with High Antibiotic Activity

N-(2,4-Dinitrophenyl)tetrapeptide p-nitroanilides (Dnp-tetra-peptide-pNA) exhibit characteristic CD spectra when they take on β-turn conformation. Exciton coupling of electric transition dipoles of the two chromophores is thought to be the origin of […]

Preclinical Studies on the Pharmacokinetics, Safety, and Toxicology of Oxfendazole: Toward First in Human Studies

Preclinical Studies on the Pharmacokinetics, Safety, and Toxicology of Oxfendazole: Toward First in Human Studies

A number of BZ anthelmintics used in veterinary medicine have been considered for transition to human use, including oxibendazole and oxfendazole (OXF). In addition, flubendazole, already approved for use as […]

First report of fluazuron resistance in Rhipicephalus microplus: A field tick population resistant to six classes of acaricides

First report of fluazuron resistance in Rhipicephalus microplus: A field tick population resistant to six classes of acaricides

João Ricardo de Souza Martins and co-workers described the first report of fluazuron resistance in R. microplus, and also report the first tick strain that was multi-resistant to six classes […]

Development of albendazole sulfoxide-loaded Eudragit microparticles: A potential strategy to improve the drug bioavailability

Development of albendazole sulfoxide-loaded Eudragit microparticles: A potential strategy to improve the drug bioavailability

Benzimidazole compounds are especially effective against nematodes found in the gastrointestinal tube in combating adult worms besides their larvae and eggs. They are also highly effective against lung worms. Their […]