The ever increasing cases of microbial resistance pose a major threat to the scientific community and therefore the need for discovery and development of newer antimicrobial agents with novel mode of action is becoming critical. One of the ways to tackle this herculean problem is to generate hybrid molecules by combining two or more bioactive heterocyclic moieties in a single molecular platform. The review here describes published results of our research group's endeavors towards development of potential new and safe antimicrobial agents with better effectiveness by using the hybrid approach. In the present review article the landscaping of heterocycles like 4-thiazolidinones, benzimidazole and quinoline are described. Compounds displaying two of more fold antimicrobial activity are included in the review.

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Microwave-assisted organic reaction enhancement (MORE) has become more important in synthetic organic chemistry for efficient resource utilization. In this study, we synthesized bioactive compounds using both traditional and microwave methods. Microwave-assisted synthesis takes less time and produces higher yields and quality than conventional approaches. We reported the synthesis of N′-(1-(2-(3-(4chlorophenyl)-1-phenyl-1H-pyrazol-4-yl)-5-phenyl-1,3,4-oxadiazol-3(2H)yl)ethylidene) substituted hydrazides (4a−t). We also tested them against two strains: M. tuberculosis H 37 Ra and M. bovis BCG. Against M. tuberculosis H 37 Ra, the compounds 4e, 4h, 4k, 4p, and 4s were the most effective. Compounds 4f, 4g, and 4s showed significant activity against M. bovis BCG. The structures of newly synthesized molecules were determined using spectral methods. Furthermore, molecular docking investigations into the active site of mycobacterial InhA yielded well-clustered solutions for these compounds' binding modalities producing a binding affinity in the range of −10.366 to −8.037. Theoretical results were in good accord with the observed experimental values. The docking score of compound 4e was −10.366, and the Glide energy was −66.459 kcal/mol.

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In this green synthesis, zeolite (Y‐H) appears to be an intriguing choice for obtaining a high yield with a shorter reaction time. In addition, we have synthesized N‐aryl‐(4‐benzylidene‐5‐oxo‐2‐phenyl‐4,5‐dihydro‐1H‐imidazol‐1‐yl)‐3‐phenoxybenzamides (4a‐i), which will be proved to be potent antimicrobial agents. The title compounds were tested against Gram‐positive, Gram‐negative, and fungal strains using the Mueller–Hinton Broth technique. N‐(4‐benzylidene‐5‐oxo‐2‐phenyl‐4,5‐dihydro‐1H‐imidazol‐1‐yl)‐3‐phenoxybenzamide (4a) (minimum inhibitory concentration [MIC] = 25 μg/mL, S. pyogenes) and N‐(4‐[4‐fluorobenzylidene]‐5‐oxo‐2‐phenyl‐4,5‐dihydro‐1H‐imidazol‐1‐yl)‐3‐phenoxybenzamide (4f) (MIC = 100 μg/mL, C. albicans, A. niger, A. clavatus) were the most effective against Gram‐positive and Gram‐negative bacteria as well as fungal strains. To understand the mechanism of action of synthesized compounds, molecular docking experiments were performed against S. aureus tyrosyl‐tRNA synthetase and C. albicans sterol 14‐α demethylase.

Diabetes management is very important as the number of diabetic patients increased and therefore the present research article will be very much useful for the development of new molecules.

Antibiotic resistance in bacteria exacerbates the issue of antimicrobial resistance. Bacteria that cause common or serious infections have evolved resistance to every new antibiotic that has been introduced into the market, to varying degrees, over several decades. Faced with this reality, one of society's most urgent needs is for new antimicrobial drugs with novel mechanisms of action. With this objective, we describe here the development of a novel set of compounds including piperazine‐ and thiophene‐based thiazolidinones (5a–i) and thiophene‐thiazolidinones (6a–i). Compounds (5a–i) and (6a–i) were developed, synthesized, and tested for their antimicrobial activity, and their structures were elucidated with the help of various analytical techniques. Compounds 5a and 5d showed excellent antibacterial efficacy against Pseudomonas aeruginosa, with MICs of 50 μg/ml, whereas compounds 6c and 6e showed similar potency against Staphylococcus aureus and Escherichia coli, respectively. The antifungal efficacy of compounds 5e and 6i against Candida albicans was outstanding (MIC = 50 μg/ml). The only compound that had excellent antifungal efficacy against Aspergillus niger was compound 5e (MIC = 50 μg/ml). The chemico‐in silico‐biology approach could provide valuable insights into the potential of this novel hybridized scaffold for the development of promising antimicrobial agents.

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