Versatility of chalcone derivative of 2-(4-acetyl)-phenoxyl-5-carboxamido-1,4-benzodiazepin-5-(4-methylpiperazinyl)-carboxamide (6) was explored to provide an easy one-pot access to its 2-(isoxazolo, pyrazolo and pyrimido) substituted analogues 9,

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Inclusion of metabolic considerations in the drug design process leads to significant development in the field of chemical drug targeting and the design of safer drugs during past few years which is a part of an approach now designated as Retro metabolic drug design (RMDD). This approach represents systematic methodologies that integrate structure-activity and structure-metabolism relationships and are aimed to design safe, locally active compounds with an improved therapeutic index. It embraces two distinct methods, chemical delivery systems and a soft drug approach. Present review recapitulates an impression of RMDD giving reflections on the chemical delivery system and the soft drug approach and provides a variety of examples to embody its concepts. Successful application of such design principles has already been applied to a number of marketed drugs like esmolol; loteprednol etc., and many other candidates like beta blockers, ACE inhibitors, alkylating agents, antimicrobials etc., are also under investigation.

A study directed towards exploring the temperature-dependent reactivity of the chlorine atoms of 2,4,6-trichloro-s-triazine (TCT) in the nucleophilic displacement reaction, allowed a facile replacement of its chlorine atoms in succession with (i) N-amino methyl substituted isatin-3-hydrazones, (ii) N1-substituted-4-amino benzene sulphonamides, and (iii) 8-amino-4-oxo-N-benzyl-azacarbazole to produce the corresponding 2,4,6-trisubstituted-s-triazine, namely; 2-(N-amino methyl substituted isatin-3-hydrazinyl)-4-(N1-substituted-4′-amino benzenesulfonamidyl)-6-(8′-amino-4′-oxo-N-benzylazacarbazolyl)-1,3,5-triazine derivatives in acceptable yields. The compounds prepared were further evaluated for their antibacterial activity againstE. coliandB. subtilisand antifungal activities againstA. nigerandA. flavus, and some of them showed promising activity profile.

One-pot heterocyclic synthesis is an exciting research area as it can open routes for the development of otherwise complex transformations in organic synthesis. Heterocyclic compounds show wide spectrum of applications in medicinal chemistry, chemical biology, and materials science. These heterocycles can be generated very efficiently through highly economical and viable routes using one-pot synthesis. In particular, the metal-free one-pot synthetic protocols are highly fascinating due to several advantages for the industrial production of heterocyclic frameworks. This comprehensive review is devoted to the transition metal-free one-pot synthesis of nitrogen-containing heterocycles from the period 2010-2013.