Nikhil Rautela

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The widespread emergence of Plasmodium falciparum (Pf) strains resistant to frontline agents has fuelled the search for fast-acting agents with novel mechanism of action. Here, we report the discovery and optimization of novel antimalarial compounds, the triaminopyrimidines (TAPs), which emerged from a phenotypic screen against the blood stages of Pf. The(More)
OBJECTIVE The objective of this study was to assess the prevalence of risk factors for coronary artery disease (CAD) in government employees across India. METHODS The study population consisted of government employees in different parts of India ({n=10,642 men and n=1966 women; age 20-60 years}) and comprised various ethnic groups living in different(More)
Whole-cell high-throughput screening of the AstraZeneca compound library against the asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino imidazoles, a robust starting point for initiating a hit-to-lead medicinal chemistry effort. Structure-activity relationship studies followed by pharmacokinetics optimization resulted in(More)
Repositioning of existing drugs has been suggested as a fast track for developing new anti-malarial agents. The compound libraries of GlaxoSmithKline (GSK), Pfizer and AstraZeneca (AZ) comprising drugs that have undergone clinical studies in other therapeutic areas, but not achieved approval, and a set of US Food and Drug Administration (FDA)-approved drugs(More)
The thyroid follicles represent a biological continuum. Each follicle is closely related to the follicle that is next to it. The important feature of a follicular carcinoma is a microfollicular pattern. We report a case of follicular carcinoma in a 48-year-old female that demonstrates microfollicles which are larger in size and contain more number of(More)
The pace of anti-malarial drug discovery is often impeded due to the lack of tools to determine the cidality of compounds in vitro. An anti-malarial compound must have a cidal mode of action, i.e. kill parasites, in order to quickly reduce parasite load. A static compound that merely inhibits growth must be identified early on in the discovery cascade. In(More)
From the phenotypic screening of the AstraZeneca corporate compound collection, N-aryl-2-aminobenzimidazoles have emerged as novel hits against the asexual blood stage of Plasmodium falciparum (Pf). Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the identification of 12 as a lead molecule. Compound 12 was(More)
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