A5005111628- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and biological activity
- Parasitic Diseases Research and Treatment
- Toxin Mechanisms and Immunotoxins
- Parasites and Host Interactions
- Cancer-related molecular mechanisms research
- Quinazolinone synthesis and applications
- Phenothiazines and Benzothiazines Synthesis and Activities
- Parasite Biology and Host Interactions
- Phytochemistry and Bioactivity Studies
- NF-κB Signaling Pathways
- Graphene and Nanomaterials Applications
- Lysosomal Storage Disorders Research
- Transgenic Plants and Applications
- Plant-derived Lignans Synthesis and Bioactivity
- Supramolecular Self-Assembly in Materials
- Anesthesia and Neurotoxicity Research
- Carbohydrate Chemistry and Synthesis
- Mosquito-borne diseases and control
- Malaria Research and Control
- Signaling Pathways in Disease
- Lung Cancer Treatments and Mutations
The Ohio State University
2024
The Ohio State University Wexner Medical Center
2023
Central Drug Research Institute
2011-2022
University of Lucknow
2014-2017
King George's Medical University
2015-2016
The high potential of quinazolinone containing natural products and their derivatives in medicinal chemistry led us to discover four novel series 53 compounds based on the concept molecular hybridization. Most synthesized analogues exhibited potent leishmanicidal activity against intracellular amastigotes (IC50 from 0.65 ± 0.2 7.76 2.1 μM) as compared miltefosine = 8.4 nontoxic toward J-774A.1 cell line Vero cells. Moreover, activation Th1 type suppression Th2 immune responses induction...
The objective of this study was to identify a nitroimidazo-oxazole lead molecule for the treatment visceral leishmaniasis (VL). A library 72 nitroimidazo-oxazoles evaluated in vitro their antileishmanial activity against luciferase-transfected DD8 amastigotes Leishmania donovani. On basis potency and pharmacokinetic properties, promising compounds were tested acute BALB/c mouse chronic hamster models VL via oral administration efficacy by microscopic counting after Giemsa staining. best...
Immuno-modulators in combination with antileishmanial drug miltefosine is a better therapeutic approach for treatment of Visceral Leishmaniasis (VL) as it not only reduces the dose but also shortens regimen. However, immunological mechanisms behind perceived benefits this therapy have been investigated detail. In present study, we hypothesized that potential use drugs target host addition to parasite might represent an alternative strategy therapy. We immune responses generated Leishmania...
Novel β-carboline–quinazolinone hybrids are able to inhibit <italic>Leishmania donovani</italic> TR (LdTR). Molecular docking studies investigate possible binding sites were performed.
Antileishmanial activities of a library synthetic chalcone analogues have been examined. Among them, five compounds (11, 14, 16, 17, 22, and 24) exhibited better activity than the marketed drug miltefosine in vitro studies against intracellular amastigotes form Leishmania donovani. Three promising compounds, were tested L. donovani/hamster model. Oral administration at concentration 100 mg/kg body weight per day for 5 consecutive days, resulted >84% parasite inhibition 7 post-treatment it...
The World Health Organization has classified the leishmaniasis as a major tropical disease. discovery of new compounds for is therefore pressing concern anti-infective research program. We have synthesized 19 triazine dimers novel antileishmanial agents. Most derivatives exhibited better activity against intracellular amastigotes (IC50 ranging from 0.77 to 10.32 μM) than control, pentamidine = 13.68 μM), and are not toxic Vero cells. Compounds 14 15 showed significant in vivo inhibition...
The first protocol for the synthesis of perspicamide A and related diverse analogues has been developed from economical readily available starting materials. Furthermore, a few synthesized analogues, 24a, 24b, 24c, 24d, 24l, exhibited potent activity against Leishmania donovani with IC(50) values ranging 3.75 to 10.37 μM selectivity index (SI) 9.58 53.12, which is improved compared standard drug Miltefosine (IC(50) 12.4 SI 4.1).
Rejuvenation of deteriorated host immune functions is imperative for successful annihilation Leishmania parasites. The use immunomodulatory agents may have several advantages as they conquer immunosuppression and, when given in combination, improve current therapeutic regimens. We herein investigated the immunostimulatory potency a β-glucan, lentinan either alone or combination with short dose standard drug, miltefosine on Leishmania-infected J-774A.1 macrophages. Our study shows that...
Leishmaniasis, caused by the protozoan parasites of genus Leishmania, is one most neglected diseases endemic in many continents posing enormous global health threats and therefore discovery new antileishmanial compounds utmost urgency. The activities a library sugar amino acid-based linear lipopeptide analogues were examined with aim to identify potential drug candidates treat visceral leishmaniasis. It was found that among synthesized analogues, permethylated exhibited more activity vitro...
In the era of drug repurposing, speedy discovery new therapeutic options for drug-resistant malaria is best available tactic to reduce financial load and time in process. Six anticancer drugs, three immunomodulators four antibiotics were selected repositioning against experimental owing their mode action published literature. The efficacy existing therapeutics was evaluated chloroquine-resistant vitro vivo strains Plasmodium falciparum P. yoelii, respectively. All pre-existing FDA-approved...
Human infection with the protozoan parasite Trypanosoma cruzi causes Chagas disease for which there are no prophylactic vaccines. Cyclophilin 19 is a secreted cis-trans peptidyl isomerase expressed in all life stages of cruzi. This protein insect stage leads to inactivation anti-parasitic peptides and transformation whereas intracellular amastigotes it participates generating ROS promoting growth parasites. We have generated mutant depleted expression Cyp19 by removal 2 3 genes encoding this...