title: Preparation and evaluation of a new erythromycin derivative -- erythromycin taurate.
abstract: Erythromycin taurate, a new derivative of erythromycin, was prepared by reacting erythromycin base with tauric acid and its physico-chemical and biological properties were evaluated. The derivative has reasonably good solubility in organic solvents. The partition coefficient values in chloroform/water 1.17 and octanol/water 1.16 systems indicate its good distribution in various tissues in vivo. The in vitro antimicrobial potency of the derivative (833.33 microg mg(-1)) is higher than that of the existing derivatives such as erythromycin estolate, erythromycin stearate, erythromycin ethyl succinate, erythromycin gluceptate, erythromycin lactobionate. The antimicrobial spectrum is comparable to that of the parent compound. Our results indicate that erythromycin taurate has a high potential for possible clinical application and is more efficient against Escherichia coli and Klebsiella pneumoniae than the parent base.
authors.affiliation: Department of Pharmacy, Annamalai University, Annamalai Nagar, 608002 Tamil Nadu, India. pkmanna@rediffmail.com
authors.forename: Prabal Kumar
authors.initials: PK
authors.lastname: Manna
authors.forename: Venugopal
authors.initials: V
authors.lastname: Kumaran
authors.forename: Guru Prasad
authors.initials: GP
authors.lastname: Mohanta
authors.forename: Rajappan
authors.initials: R
authors.lastname: Manavalan
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004917:Erythromycin / Q000138:chemical synthesis / Q000494:pharmacology*; D007194:India; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests / Q000379:methods; D011817:Rabbits; D012995:Solubility / Q000187:drug effects; D023382:Toxicity Tests, Acute / Q000379:methods
chemical_list: D004917:Erythromycin