Novel azole-sulfonamide conjugates as potential antimicrobial candidates: synthesis and biological assessment.

Background: Azole and sulfonamide molecular frameworks are endowed with potent antimicrobial activity. Materials & methods: A series of azole-sulfonamide conjugates were synthesized using click reaction of N-propargylated imidazole with azide of sulfonamide and its antimicrobial efficacy was evaluated. Results: The compounds 7c, 7i and 7r displayed promising antibacterial activities, better than the standards sulfonamide and norfloxacin. All molecules exhibited promising antifungal activity, more potent than fluconazole. Docking studies of the active conjugates signified the importance of hydrophobic interactions in hosting the molecules in the active site of dihydrofolate reductase. Conclusion: Azole-sulfonamide conjugates are more active than single sulfonamide moieties and 7c, 7i and 7r may prove valuable leads for further optimization as novel antimicrobial agents.

An Introductory Overview on Applications of Pyrazoles as Transition Metal Chemosensors.

Utility of pyrazoles and their derivatives in constructing ordered porous materials with physicochemical characteristics such as chemosensors has undoubtedly created much interest in developing newer frameworks. A variety of pyrazole based chemosensors are known for their remarkable photophysical, pH sensitivity, solvatochromic, ion detection, high quantum yields and nonlinear optical behavior. Many of the transition metals have shown beneficial biological effects in biological systems. There is always a need of continuous monitoring to maintain an adequate range of all and specifically for the toxic ones like mercury. Pyrazoline nanoparticle probes have been reported for sensing/detection of Hg2+ions. Pyridinyl pyrazoline and benzimidazolyl pyrazole derived sensors are more selective and sensitive towards Zn2+and Fe3+ ions respectively. Pyrazole derived metal organic frameworks (MOF's) have been reported for environmental monitoring and biological imaging. Keeping in view of the enormous synthetic and biological importance of pyrazoles, herein, we are presenting an overview on applications of pyrazoles in transition metal chemosensors.