Due to the severe side effects revealed by most of the currently used antidiabetic medicines, search for finding new and safe drugs to manage diabetes is continued. Naphthoquinones possessing strong antioxidant properties have been employed as candidates for diabetes therapy. Present study is aimed at finding the antioxidant and hypoglycaemic potential of some novel derivatives of 2-phenylamino-1,4-naphthoquinones (PAN) including chloro, nitro, methyl and bromo (5a-d) derivatives synthesized by single pot experiment. Product crystals were purified by TLC and characterized by FT-IR. The antioxidant potential of the compounds was assayed through DPPH radical scavenging and reducing power activities noted as UV-vis. absorbance. The DPPH assay has showed the powerful antioxidant activity of nitro and bromo derivatives, while the nitro derivative showed the significant reduction potential towards FRAP assay. Hypoglycaemic potential of the compounds was studied in rat animal model. All synthesized compounds revealed better hypoglycaemic activity; however, the chloro-derivative exhibited the more potent hypoglycaemic activity showing about 43% reduction in the mean blood glucose levels of the treated animals. As the bioreduction of naphthoquinones may be influenced by changing its redox properties, it has been noticed that the e-donating resonance effect (+R) of ‘chloro’ group has shown the significant effects on biological activity through stabalization of its imine form which limits the potential of generation of free radicals during bioreduction of quinones and thus has been proposed as the reason of its hypoglycaemic activity. Future studies employing the properties of e-donating groups of PAN may optimize the drug-receptor interaction for better drug designing and drug development strategies against diabetes and also for the clinical trials.

SCREENING OF PHYTOCHEMICALS AND IN VITRO ANTIDIABETIC POTENTIAL OF RAPHANUS SATIVUS LEAVES EXTRACT

Introduction: Tuberculosis (TB) remains a major global health challenge, further complicated by drug resistance and comorbidities. This study investigates curcumin analogues, dibenzylidene-cyclohexanones, as potential multitarget anti-TB agents. Methods: Nine benzylidene cyclohexanone derivatives were synthesized using microwave-assisted techniques (yields: 23–81%). Their potential activities were evaluated through molecular docking against key Mycobacterium tuberculosis (Mtb) enzymes and supported by network pharmacology analysis focused on TB-related pathologies. Results: The benzylidene cyclohexanone analogs A-135 (81%), A-144 (58%), and A-154 (30%), synthesized efficiently via microwave-assisted green chemistry, exhibited superior multitarget binding affinities against key Mtb enzymes—A-135 (MtFabH, pantothenate synthetase), A-144 (MurE, DprE1, PTPs), and A-154 (Ddn, GlmU, Pks13)—with halogen substituents enhancing interactions through halogen bonds and lipophilicity; network pharmacology further revealed 294 overlapping TB-related targets and identified NF-κB1, STAT3, STAT1, and PTGS2 as key hubs mediating their multitarget therapeutic potential modulating TB clinical manifestation in human body. Discussion: They exhibited superior multitarget binding affinities against key Mtb enzymes, A-135 (MtFabH, pantothenate synthetase), A-144 (MurE, DprE1, PTPs), and A-154 (Ddn, GlmU, Pks13)—with halogen substituents enhancing interactions through halogen bonds and lipophilicity; network pharmacology further revealed 294 overlapping TB-related targets and identified NF-κB1, STAT3, STAT1, and PTGS2 as key hubs mediating their multitarget therapeutic potential, modulating TB clinical manifestation in the human body. Conclusion: A-135, A-144, and A-154 demonstrate promising multitarget anti-TB activity and potential as adjuvant therapies to complement existing treatments, especially for managing drug resistance and related comorbidities.