A5028352281- Phytochemistry and Biological Activities
- Natural Antidiabetic Agents Studies
- Tuberculosis Research and Epidemiology
- Diabetes, Cardiovascular Risks, and Lipoproteins
- Inflammatory Biomarkers in Disease Prognosis
- Drug Transport and Resistance Mechanisms
- Essential Oils and Antimicrobial Activity
- Viral Infections and Vectors
- Synthesis and biological activity
- Phytochemistry and biological activities of Ficus species
- Diabetes Management and Education
- Cardiovascular Disease and Adiposity
- Cardiovascular Health and Disease Prevention
- Ethnobotanical and Medicinal Plants Studies
- Effects of Radiation Exposure
- HIV/AIDS drug development and treatment
- Computational Drug Discovery Methods
- Leptospirosis research and findings
- Adipokines, Inflammation, and Metabolic Diseases
- Cardiovascular Function and Risk Factors
- Magnesium in Health and Disease
- Metabolism and Genetic Disorders
- Malaria Research and Control
- Cancer therapeutics and mechanisms
- Synthesis and Biological Evaluation
Chaitanya Bharathi Institute of Technology
2024
Sri Devaraj Urs Academy of Higher Education and Research
2012-2023
Sri Devaraj Urs Medical College
2012-2023
Syngene International (India)
2016-2021
Biocon (India)
2016-2021
Bristol-Myers Squibb (India)
2016-2021
General Department of Preventive Medicine
2021
Bristol-Myers Squibb (United States)
2016-2018
AstraZeneca (India)
2014-2017
Manipal Academy of Higher Education
2002-2013
In the present study, an open-label, three-treatment, three-period clinical study of rosuvastatin (RSV) and rifampicin (RIF) when administered alone in combination was conducted 12 male healthy subjects to determine if coproporphyrin I (CP-I) III (CP-III) could serve as biomarkers for organic anion transporting polypeptide 1B1 (OATP1B1) 1B3 that belong solute carrier gene subfamily. Genotyping human OATP1B1 performed all confirmed absence OATP1B1*5 OATP1B1*15 mutations. Average plasma...
The approval of bedaquiline to treat tuberculosis has validated adenosine triphosphate (ATP) synthase as an attractive target kill Mycobacterium (Mtb). Herein, we report the discovery two diverse lead series imidazo[1,2-a]pyridine ethers (IPE) and squaramides (SQA) inhibitors mycobacterial ATP synthesis. Through medicinal chemistry exploration, established a robust structure-activity relationship these scaffolds, resulting in nanomolar potencies synthesis inhibition assay. A biochemical...
Ethanol extract (FRE) and water (FRW) of Ficus racemosa (family: Moraceae) were subjected to free radical scavenging both by steady state time resolved methods such as nanosecond pulse radiolysis stopped-flow spectrophotometric analyses. FRE exhibited significantly higher antioxidant activity than FRW. concentration dependent DPPH, ABTS(*-), hydroxyl superoxide inhibition lipid peroxidation with IC(50) comparable tested standard compounds. In vitro radioprotective potential was studied using...
In a previous report, we described the discovery of 1,4-azaindoles, chemical series with excellent in vitro and vivo antimycobacterial potency through noncovalent inhibition decaprenylphosphoryl-β-d-ribose-2′-epimerase (DprE1). Nevertheless, high mouse metabolic turnover phosphodiesterase 6 (PDE6) off-target activity limited its advancement. Herein, report lead optimization this series, culminating potent, metabolically stable compounds that have robust pharmacokinetic profile without any...
Abstract The widespread emergence of Plasmodium falciparum ( Pf ) strains resistant to frontline agents has fuelled the search for fast-acting with novel mechanism action. Here, we report discovery and optimization antimalarial compounds, triaminopyrimidines (TAPs), which emerged from a phenotypic screen against blood stages . clinical candidate (compound 12 is efficacious in mouse model malaria an ED 99 <30 mg kg −1 displays good vivo safety margins guinea pigs rats. With predicted...
Plasma pyridoxic acid (PDA) and homovanillic (HVA) were recently identified as novel endogenous biomarkers of organic anion transporter (OAT) 1/3 function in monkeys. Consequently, this clinical study assessed the dynamic changes utility plasma PDA HVA an initial evaluation OAT1/3 inhibition early-phase drug development. The was designed a single-dose randomized, three-phase, crossover study; 14 Indian healthy volunteers received probenecid (PROB) (1000 mg orally) alone, furosemide (FSM) (40...
High fat diet (HFD) and low-dose streptozotocin (STZ) is an ideal model for type 2 diabetes mellitus (T2DM) that would closely reflect the natural history metabolic characteristics of human T2DM also suitable pharmacological screening.The present study was designed to investigate effect water extract (DVW) polar fraction ethanol (DVE-4) Dodonaea viscosa (L). Jacq. (Sapindaceae) on biochemical parameters in induced by a standardized HFD low dose (25 mg/kg) rats. Further, elucidate mode action...
From the phenotypic screening of AstraZeneca corporate compound collection, N-aryl-2-aminobenzimidazoles have emerged as novel hits against asexual blood stage Plasmodium falciparum (Pf). Medicinal chemistry optimization potency Pf and ADME properties resulted in identification 12 a lead molecule. Compound was efficacious P. berghei (Pb) model malaria. This displayed an excellent pharmacokinetic profile with long half-life (19 h) rat blood. led to extended survival animals for over 30 days...
Purpose: To evaluate and optimize the radioprotective ability of most potent fraction an aqueous extract Coronopus didymus in whole body γ-irradiated Swiss albino mice to antioxidant status lipid peroxidation livers surviving mice. correlate free radical scavenging studies with vivo radioprotection ability.Materials methods: were treated either vehicle or different doses extract/fraction suspension by i.p. route, 30 min before exposure 10 Gy γ-irradiation animals monitored twice daily for...
Seventy five patients with oral lesions attending the different departments of Rajah Muthiah Medical College and Hospital, Annamalai University were screened for Candida. Forty six (61.3%) Candida strains isolated from lesions. Of 46 strains, albicans accounted 35 (76.08%), glabrata 5 (10.86%), tropicalis krusei 2 (4.34%) each parapsilosis guilliermondii one (2.17%) each. Antifungal activity ethanol extracts plant species that included Syzygium jambolanum, Cassia siamea, Odina wodier,...
The in vitro metabolism and vivo pharmacokinetic (PK) properties of DNDI-VL-2098, a potential oral agent for Visceral Leishmaniasis (VL) were studied used to predict its human pharmacokinetics. DNDI-VL-2098 showed low solubility (10 μM) was highly permeable (>200 nm/s) the Caco-2 model. It stable liver microsomes hepatocytes no metabolite detectable circulating plasma from dosed animals suggesting very slow, if any, compound. moderate bound proteins across species tested (94–98%)....
2,4-Diaminoquinazolines, 2,4-diaminoquinolines and aminopyrazolopyrimidines, inhibitors of mycobacterial ATP synthesis, are novel lead molecules towards discovery development new anti-tubercular agents.
Whole-cell high-throughput screening of the AstraZeneca compound library against asexual blood stage Plasmodium falciparum (Pf) led to identification amino imidazoles, a robust starting point for initiating hit-to-lead medicinal chemistry effort. Structure–activity relationship studies followed by pharmacokinetics optimization resulted in 23 as an attractive lead with good oral bioavailability. Compound was found be efficacious (ED90 28.6 mg·kg–1) humanized P. mouse model malaria (Pf/SCID...
In this study, we report an effective electrochemical sensor of single-walled carbon nanotubes (SWCNTs)/Nafion glassy electrode (SWCNTs/Nafion/GCE) for determination dicapthon in water and agricultural food samples. The electroanalytical performance SWCNTs/Nafion/GCE toward the reduction was analyzed via cyclic differential pulse voltammetry. optimum parameters like effect pH, concentration solution, scan rate, accumulation potential time were thoroughly optimized. At conditions,...
The effect of mononuclear copper (II) complex curcumin in 1:1 stoichiometry (hereafter referred to as complex) administered 30 min before gamma-irradiation (4.5 Gy) on alterations antioxidant and Thiobarbituric acid reactive substances (TBARS) levels livers was studied comparison at a dose 50 mg/kg. different antioxidants like GSH, GST, catalase, SOD, TBARS total thiols were estimated the liver homogenates excised time intervals (1, 2 4 h) post irradiation using colorimetric methods. There...