Identification of potential drug candidates to treat gastritis and associated oxidative stress based on some novel 2-aryl-1H-naphtho[2,3-d]imidazole: synthesis, in vitro and in silico analysis.

To identify potential scaffolds to treat gastritis and oxidative stress, 2-aryl-1H-naphtho[2,3-d]imidazole derivatives (1-15) were synthesized. The synthesis was conveniently carried out by condensing 2,3-diaminonaphthalene with variously substituted aldehydes to yield 15 new 2-aryl-1H-naphtho[2,3-d]imidazole derivatives. Structures of all synthesized compounds were elucidated using MS and NMR spectroscopic techniques. Compounds containing an imidazole moiety have continued to spark interest in the field of medicinal chemistry due to their unique properties. In continuation of this statement, to further explore the biological potential of these types of compounds, newly synthesized imidazole derivatives were evaluated for their inhibitory potential against urease and antioxidant activities. Compounds 4 and 11 were identified as the most potent urease inhibitors in the series, with IC50 values of 34.2 ± 0.72 and 42.43 ± 0.65 µM, respectively. Compounds 1, 3, 6, 11, and 15, with EC50 values in the range of 37-75 µg ml-1, showed significant antioxidant activity. Molecular docking studies of the selected synthesized compounds 3, 4, 9, and 11 were also performed to determine their binding interaction with the jack bean urease. Through docking studies, it was revealed that all the compounds that showed good inhibitory potential against urease fit well within the protein's binding pocket. Furthermore, ADME analysis was carried out to explore the drug-likeness properties of the compounds. The findings of the present work revealed that compounds 4 and 11 could be better options to treat gastritis and associated oxidative stress.

Development and evaluation of herbal formulation AKIGTU01 and AKIGCL03 against acne producing microbes.

Acne vulgaris is a common global skin disease affecting teenagers and adults and exerting serious psychological impacts which includes everlasting scarring, reduced self-image, depression and anxiety. One of the suspected causative agent of acne is Propionibacterium acnes; a Gram positive anaerobic organism which lives in skin hair follicle and openings. Treatments currently available for acne include use of oral antibiotics, hormones, isotretinoin and also physical treatments like lesion removal and photo-therapy. All these are associated with risks and none is completely satisfactory.Therefore, natural alternatives are gaining greater research support but lacks sufficient studies. In our study we have isolated Propionibacterium acnes from infected individuals and tested the effect of certain chemicals and herbs/ vegetable extracts against it. There anti-acne property was studied and compared with commercially used antibiotics including Clinagel (Clindamycin phosphate), Vibramycin (Doxycycline), Erythromycin, Novidat (Ciprofloxacin) and Amoxil (Amoxicillin). Results indicate that some of the selected herbs and chemicals showed good activity against Propionibacterium acnes synergistic to the antibiotics when used alone or in combination. Findings of this research can play an important role in natural product based drug discovery for the treatment of Acne vulgaris.