A5105406127- Tuberculosis Research and Epidemiology
- Mycobacterium research and diagnosis
- Pneumocystis jirovecii pneumonia detection and treatment
- Synthesis and biological activity
- Gastrointestinal disorders and treatments
- Synthesis and Characterization of Heterocyclic Compounds
- Cancer therapeutics and mechanisms
- Quinazolinone synthesis and applications
- Esophageal and GI Pathology
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Intestinal Malrotation and Obstruction Disorders
- Congenital gastrointestinal and neural anomalies
- Congenital Diaphragmatic Hernia Studies
- Tracheal and airway disorders
- Leprosy Research and Treatment
- Congenital Anomalies and Fetal Surgery
- Tumors and Oncological Cases
- Urological Disorders and Treatments
- Click Chemistry and Applications
- Chemical Synthesis and Analysis
- Bioactive Compounds and Antitumor Agents
- Pharmacological Effects of Natural Compounds
- Biochemical and Molecular Research
Sawai ManSingh Medical College and Hospital
2013-2024
Central Drug Research Institute
2013-2023
Creative Commons
2019
University of Lucknow
2015
Academy of Scientific and Innovative Research
2013
National JALMA Institute for Leprosy & Other Mycobacterial Diseases
1990-1995
New and better drugs are needed for tuberculosis (TB), particularly the multi-drug resistant (MDR) disease. However, highly infectious nature of MDR Mycobacterium restricts its use large scale screening probable drug candidates. We have evaluated potential a screen based on 'fast grower' mycobacterium to shortlist compounds which could be active against M. tuberculosis. Sensitivity profiles smegmatis, phlei fortuitum as well clinical isolates were determined anti-TB isoniazid rifampicin....
An efficient, green strategy for synthesis of 1,4-disubstituted-1,2,3-triazole has been developed using 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) acetate ionic liquid (200 μL) under a solvent- and external base-free condition. This protocol is further applied the novel amino acid containing 1,2,3-triazole molecules, which were then evaluated potential antitubercular antibacterial activities. Cytotoxicity assay compounds was also performed. In silico analysis promising selected through...
The study was aimed at identification by proteomics and validation enzyme-linked immunosorbent assay (ELISA) of potential urinary biomarkers for lupus nephritis. Study subjects comprised 88 systemic erythematosus (SLE) patients 60 controls (rheumatoid arthritis, diabetes mellitus healthy individuals). Based on the SLE disease activity index (SLEDAI), were classified as active renal (AR), non-renal (ANR) or inactive (ID). Urinary proteins from a group with AR ID resolved two-dimensional gel...
A series of C-3 alkyl and arylalkyl 2,3-dideoxy hex-2-enopyranoside derivatives were synthesized by Morita−Baylis−Hillman reaction using enulosides 4, 5, 6 various aliphatic aromatic aldehydes. The compounds evaluated in vitro for the complete inhibition growth Mycobacterium tuberculosis H37Rv. They exhibited moderate to good activity range 25−1.56 μg/mL. Among these, 4d, 4h, 5c, 4hr showed at minimum inhibitory concentrations, 3.12, 6.25, 1.56, 1.56 μg/mL, respectively. These safe against...
New, highly stable tricyclic antitubercular ozonides 9 and 10 derived from artemisinin are reported in 39 9% yields, respectively. The ozonide groups of were found to be under strong basic acidic conditions. absolute configuration was confirmed by X-ray crystallography. Ozonide shows promising activity against M. tuberculosis H37Ra H37Rv with MIC values 0.39 3.12 μg/mL,
A straightforward and convenient methodology has been developed for the reaction of 2-aminobenzamide carbonyls affording 2,3-dihydroquinazolin-4(1H)-ones using aqueous solution [C12Py][FeCl3Br]. The was applied synthesis 25 quinazolinone-triazole hybrids followed by evaluation their in vitro anti-tubercular (TB) activity. results revealed that 8 displayed promising activity having MIC values 0.78–12.5 μg/mL. compound 3if with 0.78 μg/mL found to be lead nominee among series, better than...
Despite intense research, PE_PGRS proteins still represent an intriguing aspect of mycobacterial pathogenesis. These cell surface influence virulence in several pathogenic species, but their diverse and exact functions remain unclear. Herein, we focussed on a member from Mycobacterium marinum, MMAR_0242, characterized by extended unique C-terminal domain. We demonstrate that M. marinum mutant carrying transposon insertion MMAR_0242 is highly impaired its ability to replicate macrophages...
In view of the worldwide spread multidrug resistance Mycobacterium tuberculosis, there is an urgent need to discover antitubercular agents with novel structures. Thymidine monophosphate kinase from M. tuberculosis (TMPKmt) attractive target for chemotherapy. We report here identification potent compounds targeting TMPKmt using virtual screening methods. For this purpose we have developed a pharmacophore hypothesis based on substrate and known inhibitors employed it screen Maybridge small...
A series of 1-[(4-benzyloxyphenyl)-but-3-enyl]-1H-azoles has been identified as potent antitubercular agents against Mycobacterium tuberculosis. Synthesis compounds involved acid catalyzed ring-opening cyclopropyl ring phenyl methanols followed by nucleophilic attack the azoles on carbocation intermediates. Several 26, 34, and 36 exhibited significant activities with MIC value low 1.56, 0.61 μg/mL, respectively, comparable to many standard drugs. These were also screened other strains...
We earlier reported thiophene-containing trisubstituted methanes (TRSMs) as novel cores carrying anti-tubercular activity, and identified S006-830 the phenotypic lead with potent bactericidal activity against single- multi-drug resistant clinical isolates of Mycobacterium tuberculosis (M. tb). In this work, we carried out additional synthesis several TRSMs. The reaction scheme essentially followed Grignard Friedel-Crafts alkylation, by insertion a dialkylaminoethyl chain. also performed...
Conformationally-constrained and bisquinoline analogs of TMC207 as antitubercular agents.