What's new for 'Trypanosomatids' in PubMed

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Sent on Sunday, 2010 Jun 06
Search kinetoplastids OR kinetoplastid OR Kinetoplastida OR "trypanosoma brucei" OR leishmania OR brucei OR leishmaniasis OR "African trypanosomiasis"
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PubMed Results

Items 1 - 2 of 2

1.	Indian J Pharmacol. 2009 Aug;41(4):176-81. Determination of drug-like properties of a novel antileishmanial compound: In vitro absorption, distribution, metabolism, and excretion studies. Mondal SK, Mondal NB, Banerjee S, Mazumder UK. Department of Pharmaceutical Technology, Jadavpur University, India. Abstract In drug discovery research, the compounds should not only to be potent and selective but also must possess acceptable pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) to increase success rate in clinical studies. OBJECTIVE: Exploration of drug-like properties of 2-(2-methylquinolin-4-ylamino)-N-phenyl acetamide, a potent antileishmanial compound by performing some in vitro ADME experiments along with validation of such studies. MATERIALS AND METHODS: Experimental protocols were established and validated for stability (in PBS pH7.4, simulated gastric and intestinal fluid), solubility, permeability, distribution coefficient (Log D), plasma protein binding and metabolism by rat liver microsomes by using spectrophotometer or HPLC. Methods were considered valid if the results of the standard compounds matched with reported results or within acceptable range or with proper ranking (high-medium-low). RESULTS: The compound was found to be stable (>95% remaining) in all stability studies and aqueous solubility was 299.7 +/- 6.42 muM. The parallel artificial membrane permeability assay (PAMPA) indicated its medium permeability (Log Pe = -5.53 +/- 0.01). The distribution coefficients (Log D) in octanol/PBS and cyclohexane/PBS systems were found to be 0.54 and -1.33, respectively. The plasma protein binding study by the equilibrium dialysis method was observed to be 78.82 +/- 0.13% while metabolism by Phase-I enzymes for 1 hour at 37 degrees C revealed that 36.07 +/- 4.15% of the compound remained after metabolism. CONCLUSION: The methods were found to be very useful for day-to-day ADME studies. All the studies with the antileishmanial compound ascertained that the compound bears optimum pharmacokinetic properties to be used orally as a potential drug for the treatment of leishmaniasis.
	PMID: 20523869 [PubMed - in process]
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2.	Ann Trop Paediatr. 2010;30(2):161-4. Congenital visceral leishmaniasis in Ukraine: case report. Zinchuk A, Nadraga A. Department of Infectious Diseases, Lviv National Medical University, Lviv, Ukraine. Abstract An 8-month-old boy was diagnosed with visceral leishmaniasis in the Ukraine, a non-endemic area. His mother had been treated for visceral leishmaniasis at 28-32 weeks gestation whilst working in Alicante, Spain and delivered her infant at 38 weeks gestation by elective caesarean section in Ukraine. It is presumed that the infant's infection was as a result of vertical transmission.
	PMID: 20522305 [PubMed - in process]
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