Alkaloids with Anti-Onchocercal Activity from Stapf (Apocynaceae): Identification and Molecular Modeling.

A new iboga-vobasine-type isomeric bisindole alkaloid named voacamine A (), along with eight known compounds-voacangine (), voacristine (), coronaridine (), tabernanthine (), iboxygaine (), voacamine (), voacorine () and conoduramine ()-were isolated from the stem bark of . The structures of the compounds were determined by comprehensive spectroscopic analyses. Compounds , , , , , and were found to inhibit the motility of both the microfilariae (Mf) and adult male worms of , in a dose-dependent manner, but were only moderately active on the adult female worms upon biochemical assessment at 30 μM drug concentrations.

Sub-Standard Pharmaceutical Services in Private Healthcare Facilities Serving Low-Income Settlements in Nairobi County, Kenya.

Quality pharmaceutical services are an integral part of primary healthcare and a key determinant of patient outcomes. The study focuses on pharmaceutical service delivery among private healthcare facilities serving informal settlements within Nairobi County, Kenya and aims at understanding the drug procurement practices, task-shifting and ethical issues associated with drug brand preference, competition and disposal of expired drugs. Forty-five private facilities comprising of hospitals, nursing homes, health centres, medical centres, clinics and pharmacies were recruited through purposive sampling.

Medicine Prices, Availability, and Affordability in Private Health Facilities in Low-Income Settlements in Nairobi County, Kenya.

Medicine prices are a major determinant of access to healthcare. Owing to low availability of medicines in the public health facilities and poor accessibility to these facilities, most low-income residents pay out-of-pocket for health services and transport to the private health facilities. In low-income settlements, high retail prices are likely to push the population further into poverty and ill health.

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.

A novel class of benzoheterocyclic analogues of amodiaquine designed to avoid toxic reactive metabolite formation was synthesized and evaluated for antiplasmodial activity against K1 (multidrug resistant) and NF54 (sensitive) strains of the malaria parasite Plasmodium falciparum. Structure-activity relationship studies led to the identification of highly promising analogues, the most potent of which had IC50s in the nanomolar range against both strains. The compounds further demonstrated good in vitro microsomal metabolic stability while those subjected to in vivo pharmacokinetic studies had desirable pharmacokinetic profiles.

Artemisinin derivatives: a patent review (2006 - present).

Introduction: The isolation of artemisinin from an ancient Chinese remedy in the early 1970s heralded the beginning of a new era in antimalarial drug therapy culminating in artemisinin-based combination therapies currently being the mainstay of malaria treatment worldwide. Ongoing research on this compound and its derivatives has revealed its potential use in treating other infectious and noninfectious diseases.

Areas Covered: This review provides a summary of patents published globally from January 2006 to June 2012 covering promising artemisinin derivatives and artemisinin-based drug combinations developed for use in various therapeutic areas.

Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluation.

The synthesis and evaluation of antiplasmodial activity of benzothiazole, benzimidazole, benzoxazole and pyridine analogues of amodiaquine is hereby reported. Benzothiazole and benzoxazole analogues with a protonatable tertiary nitrogen atom possessed excellent activity against the W2 and K1 chloroquine resistant strains of Plasmodium falciparum, with IC(50)s ranging from 7 to 22 nM.