UNVEILING STRATEGIES FOR SHORTENING TUBERCULOSIS TREATMENT: TARGETING MYCOBACTERIUM TUBERCULOSIS STRINGENT RESPONSE AND REVIEWING POLYPHOSPHATE KINASE 2 (PPK2) ENZYMES SINGIRISETTY TRIVENI, KURUBA VIJAYA BHASKAR, CHILAMAKURU NARESH BABU, MALLELA VIJAYA JYOTHI Asian Journal of Pharmaceutical and Clinical Research, 2025 Tuberculosis (TB) is one of the oldest infectious diseases known to humankind, with traces of its presence found in remains that are around 17,000 years old. TB is mostly caused by the tiny aerobic non-motile bacillus Mycobacterium TB (MTB). The unique shape and chemical content of the mycobacterial cell wall make an efficient TB therapy method challenging. A strict bacterial survival strategy for establishing drug tolerance in the stringent response (SR), MTB is a sophisticated remodeling of metabolism that slows down growth and energy requirements during famine. Recent studies emphasize the need to focus on the SR in MTB as a means of reducing the treatment duration. The MTB genome codes two polyphosphate kinases (PPK-1 and PPK-2), for maintenance of intracellular Inorganic Polyphosphate (Poly P) levels. The identification of a virulence factor of TB growth as well as persistence in host tissues may be helped in MTB using PPK2, which is required to modulate intracellular levels of regulating molecules and to sustain sensitivity to the first-line anti-drug isoniazid. Synthesized and under control by PPK2 enzymes, inorganic polyP is essential in this process since it controls stress reactions. This research, therefore, investigates the significance of PPK2 in the MTB, the chemicals suppressing a bacterial SR in MTB, and the list of PPK2 inhibitors for shortening TB.
Schiff Base Mediated Synthesis of Novel Imidazolidine-4-One Derivatives for Potential Antimicrobial and Anthelmintic Activities Naresh Babu Chilamakuru, Triveni Singirisetty, Anoop Bodapati, Sudha Divya Madhuri Kallam, Vinod Kumar Nelson, Punna Rao Suryadevara, Selvankumar Thangaswamy Luminescence, 2024 This study focuses on developing novel antimicrobials to combat drug‐resistant pathogens, addressing compounds failing clinical trials due to inadequate physicochemical properties. Sixteen imidazolidine‐4‐one derivatives were synthesized by extensive evaluation using molecular docking, absorption, distribution, metabolism, excretion (ADME) predictions, and antimicrobial testing. Molecular docking studies conducted with Schrödinger's Glide revealed that compounds S4 and G8 exhibited superior docking scores of −7.839 and −7.776, respectively. The G series outperformed the S series in scores. ADME analysis confirmed all compounds adhered to Lipinski's rule of five. In addition, IR and NMR provided details about the structure of the compounds. Antimicrobial activity was assessed against Escherichia coli, Staphylococcus aureus, and Candida albicans, with compounds G2 and S2 showing exceptional minimum inhibitory concentration (MIC) values of 6.25 μg/mL against E. coli. S2 also demonstrated impressive activity against S. aureus (MIC 3.12 μg/mL), and S4 exhibited potent activity against C. albicans (MIC 0.8 μg/mL) than fluconazole (1.6 μg/mL). Additionally, antihelmintic activity was evaluated, with G1, G3, G8, S2, S4, S7, and S8 showing effective paralysis and death time 20 min and below at 50 mg/mL concentration. These results underscore the potential of new imidazolidine‐4‐one derivatives as suitable sources to develop a drug candidate to treat resistant infections.
Development of Imidazoline-2-one Derivatives as Potential Antifungal and Anthelminthic Agents: in silico and in vitro Evaluation Indian Journal of Heterocyclic Chemistry, 2021
in silico design, ADME prediction, molecular docking, synthesis of novel triazoles, indazoles & aminopyridines and in vitro evaluation of antitubercular activity S. Triveni, C. Naresh Babu, E. Bhargav, M. Vijaya Jyothi Asian Journal of Chemistry, 2020 To design and synthesize novel triazoles, indazoles and aminopyridines from various (thiophene-2-yl)prop-2-en-1-one derivatives as antitubercular leads by in silico and in vitro methods. in silco Drug design, ADME prediction and molecular docking studies were performed to assess drug likeliness and antitubercular potential of all 30 novel triazoles, indazoles and aminopyridines. in silico Drug design studies revealed that the synthetic routes applied were appropriate according to the calculations of Swiss-ADME that measure synthetic accessibility. Most of the synthesized compounds found to have considerable binding score with enoyl ACP reductase enzyme of Mycobacterium tuberculosis. All the synthesized compounds were evaluated for antitubercular potential against Drug Resistant Mycobacterium tuberculosis H37Rv strain by Luciferase reporter assay method. Most of the synthesized compounds exhibited remarkable antitubercular potential against resistant strain.
Design, synthesis and antimicrobial evaluation of novel 2-thiobenzimidazole derivatives: In silico and in vitro approach C. Naresh Babu, S. Triveni, M. Vijaya Jyothi, B. Yamuna, A. Yamini Asian Journal of Chemistry, 2020 The development of potent antimicrobial agents is more essential due to resistance developed in microorganisms towards the existing drugs. The diversity in the biological retort profile of benzimidazole more attracted the attention to develop novel compounds to its various potential against microorganisms. In present work, designed molecular structures docked against DNA gyrase subunit B and lanosterol 14α-demethylase (LAD) proteins. Interestingly, most of the compounds revealed excellent docking scores and interactions compared with the co-crystal ligands KKK, 1YN of LAD proteins 3LD6, 5V5Z than DNA gyrase subunit B proteins 5L3J and 4P8O. Then, the molecular properties were predicted by the Swiss ADME tool, the compounds showed no violation in Lipinski’s rule and good synthetic accessibility. These compounds synthesized by stirring of 2-mercapto benzimidazole (1), epichlorohydrin (2) in the presence of sodium hydroxide gives 1-(1H-benzo[d]imidazole-2-ylthio)-3- chloropropan-2-ol (3), which upon refluxing with different substituted aliphatic and aromatic amines in methanol produces novel benzimidazole derivatives (4a-l). These compounds were characterized by their melting point, FT-IR, 1H NMR and Mass spectral data. The synthesized molecules screened for antibacterial and antifungal activity. The compound 4l exhibited excellent activity at MIC 0.4 μg/mL against C. albicans. Compounds 4c and 4e showed MIC at 3.12 μg/mL against E. coli and the compounds 4l and 4J exhibited MIC at 3.12 μg/mL against S. aureus. Docking studies and activity result reveals the novel benzimidazole compound 4l has excellent antifungal and antibacterial effect.
Design and Synthesis of 5-Oxoimidazolidine Derivatives in Search of Potent Antitubercular and Antifungal agents Indian Journal of Heterocyclic Chemistry, 2020
A green approach for quantification of naproxen in bulk and oral dosage form by FT-IR method Ahmed Khayoon Abed Al- Abboodi, Ghaidaa Husain Al- Rubiaee, Neihaya Heikmet Zaki International Journal of Research in Pharmaceutical Sciences, 2018 The current study aims at the in-vitro use of 2 types of extracts of Chlorella Vulgaris, one of the most widely known green algae species in the world, to evaluate their effects on biofilm-producing bacteria. In this study, 7 species of algae were isolated from different environments and then diagnosed according to the sources of green algae and greenish algae. Some of these isolates were proliferated under constant laboratory conditions at 25±2 ̊C, 200μm/m2/sec, and 8:16 hours of light: dark using fixed farms. Then, these species were subjected to 2 types of polycarbonate-based solvents (hexane and chloroform). These extracts were tested on E.Coli, Klebsiella, Acinetobacter, Serratia mesccens, St epidermis, S. aureus, Candida albicans, and Aspergills niger. Using different methods of measuring turbidity of the red agar, micrometer plate, spreading Balacar, the effects of these extracts were examined on these microorganisms. Then, the algae were subjected to vertical chromatography to separate active substances. The hexane-based extract was more effective against E. coli, Acinetobacter, St. aureus. On the other hand, the chloroform-based extract showed slight effects on Acinetobacter and C. albicans. The best inhibitory activities were 30mm for Staphylococcus aureus and Serratia and 25mm for E. coli. The lowest inhibition activity was 15mm for Klebsiella and C. albicans. For the chloroform-based extract, the highest rate of inhibition was 20mm for Klebsiella and S. aureus. The lowest inhibition was 10mm for Acinetobacter and C. albicans. Separation method targeted the hexane-based extraction yielded hxan, gasoline group III ethyl estate, gasoline, group IV ethyl ester, methanol group, and methanol. The hexane + 25 ml of benzene and the fourth group of ethyl ester 25 + methanol showed higher inhibition activities against microbes than that using the other three groups. The hexane-based extracts and the related hexane + 25 ml of benzene and the fourth group of ethyl ester 25 + methanol of C. vulgaris were better than the chloroform-based extracts in their effectiveness against the studied microbes using the turbidity measurement method.
 Keywords: Biofilm; Chlorella Vulgaris; Extract effects; Microorganisms
Preclinical evaluation of nephroprotective potential of a probiotic formulation LOBUN on cyclosporine-a induced renal dysfunction in wistar rats Kambham Venkateswarlu, Thakur Heerasingh, Chilamakuru Naresh Babu, Singirisetty Triveni, Suroju Manasa, Thumati Nagendra Bhaskar Babu Brazilian Journal of Pharmaceutical Sciences, 2017 The aim of present study was to evaluate the nephroprotective effect of probiotic formulation LOBUN on Cyclosporine A (CsA) induced renal dysfunction in Wistar rats. CsA (20 mg/kg body weight s.c) was administered for 15 days to cause renal dysfunction in Wistar rats. The probiotic formulation LOBUN was administered with the dose of 500 mg/kg body weight (p.o) for twice (TGI) and thrice a day (TGII). The samples were analyzed for the parameters like blood urine nitrogen (BUN), serum creatinine, serum uric acid, total serum protein and urine proteins, urine potassium, urine sodium. The renal functional and histopathological studies revealed that the oral administration of probiotic formulation LOBUN has provided appreciable renoprotection and possibly alleviated the symptoms of Chronic Kidney Disease (CKD) at the dose of 500 mg/kg body weight administered thrice a day and also the results were supported by histopathological findings.
Synthesis, characterisation and anti-tubercular activity of some new 3,5-disubstituted-2,4-thiazolidinediones Asian Journal of Pharmaceutical and Clinical Research, 2013
