Background:
Benzothiazoles possess a vast sphere of biological activities including anti-inflammatory, antibacterial activities whereas triazoles display various pharmacological properties including antimicrobial and antitubercular activities. Hence we focused on triazole conjugated benzothiazole side chain anticipating their interesting biological properties.
Objective:
The objective of the current work is synthesis and biological evaluation of a new series of benzothiazole appended triazole derivatives.
Methods:
The target compounds were prepared via a multi-step method involving treatment of 2-amino benzothiazole with hydrazine followed by cyclization with carbon disulfide to give the corresponding triazol-2-thiol derivatives and then alkylation of these derivatives. All the synthesized compounds were characterized by FT-IR, Mass, 1H and 13C NMR spectra and were screened for their antibacterial, antioxidant, anti-inflammatory and anti-tubercular (anti-TB) activities in vitro. These molecules were also docked into the enoyl acyl carrier reductase (Inha, PDB ID-1ZID) in-silico.
Results:
While all the synthesized compounds were active against M. tuberculosis at 50 μg/ml the pyrrolidine and piperidine appended benzothiazolyltriazoles showed the superior activity (MIC values 12.5 to 1.6 μg/ml). Compound 5a (5-CH3 with piperidine), 5b (7-CH3 with piperidine) and 7b (7-CH3 with pyrrolidine) showed good antibacterial activity against Staphylococcus aureus with MIC value 31.25μg/ml, while compounds 7a (5-CH3 with pyrrolidine), 6b (7-CH3 with morpholine) and 8c (7-Br with pyridine) exhibited good antibacterial activity against E-coli with MIC value 62.5μg/ml. Compounds 7b (7-CH3 with pyrrolidine) and 5c (7-Br with piperidine) showed good anti-oxidant activities with IC50 values 93.25 and 82.25 respectively. Notably, these compounds were non-toxic to the normal cells even at high concentration with IC50 value 238μg/ml.
Conclusion:
The compound 7b, a benzothiazolyltriazole having a pyrrolidine group (five membered ring) attached to two CH2 groups and methyl substituent at 7th position of the benzothiazole ring emerged as a novel and promising hit molecule that showed anti-TB, antimicrobial and anti-inflammatory activities in vitro.
India will be producing 80-85 MT of Solid waste by 2030. Given the alarming quantity it is imperative to bring in methods which will alleviate the problem especially the plastic waste. One of the products which helps in effective disposal of plastics is the Reverse Vending Machine (RVM). An RVM is a device which accepts bar coded plastic bottles and returns digital cash or redeemable coupons. The field study and literature show that reverse vending machine is not used extensively. This study attempts to explore the challenges for adoption of eco-friendly products like RVM. A conceptual model was built using the variables identified through literature review. The variables identified included awareness, willingness, incentives, convenience and involvement. A survey was designed and data was collected from 246 citizens to understand their views. Structural Equation Modelling was used to test conceptual model. The results emphatically show that willingness to adopt RVM was influenced by factors of involvement, convenience, awareness and incentives in that order. It is also intuitive that when involvement is high then there is an attempt to become aware and adopt eco-friendly methods which is reiterated by the results. Hence citizens have to get involved either by their own interest or by enforcing through legislation and policies to use RVM. The study concludes by recommending more policies and strategies like "bottle bill", "European Union Plastic Strategy" and Recycle Refund Systems to be mandated across the world to encourage citizens to use methods which will keep our environment plastic free.
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