Mini-Review of the Importance of Hydrazides and Their Derivatives—Synthesis and Biological Activity

Organic acid hydrazides include a vast group of organic derivatives of hydrazines containing the active functional group (-C(=O)NHNH2). Acid hydrazones were important bidentate ligands and show keto-enol (amido-iminol) tautomerism. They usually exist in keto form in the solid-state while in equilibrium between keto and enol forms in solution state. Such hydrazones were synthesized in the laboratory by heating substituted hydrazides or hydrazines with corresponding aldehydes or ketones in different organic solvents such as ethanol, methanol, butanol, tetrahydrofuran, etc., and some cases with the ethanol-glacial acetic acid or acetic acid alone. Hydrozones are very important intermediates for the synthesis of heterocyclic compounds and also have different biological activities. The organic chemist would have more interest in the synthesis of acid hydrazides and their derivatives because of their properties. These derivatives having wide applications as chemical preservers for plants, drugs, for manufacturing polymers, glues, etc., in industry and many other purposes. These acid hydrazides and their derivatives were found to be useful synthons for various heterocyclic five, six or seven-membered rings with one or more heteroatoms that were exhibited great biological, pharmacological and industrial applications. This paper will present a review of the chemistry and pharmacological potentials of hydrazide-hydrazones. The various synthetic routes for hydrazone, as well as antibacterial, antifungal and antiviral potentials, have been elaborated in brief

Greener Synthesis, In-Silico and Theoretical Analysis of Hydrazides as Potential Antituberculosis Agents (Part 1)

Since several decades, our healthcare burden has been increased due to tremendous cases of multidrug-resistant (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) infections, especially in tropical countries. In the present study, we have synthesized ten hydrazides with the use of the greener Chitosan-derived catalyst. This catalyst accomplished the said condensation reaction within 15–30 min at room temperature conditions. All our synthesized compounds showed stronger affinities against Mycobacterium tb and bacterial targets, especially towards 1d7u, than the standard drug ciprofloxacin. One of our compounds retained a lower toxicity (electrophilicity index (ω) 3.1304), low chemical hardness (η: 2.1740), and high softness (S: 0.4600). In the realm of the development of more potent, effective, and safe antituberculosis agents with an effective greener synthesis, our current study would provide more insights on potent analogues containing hydrazine motifs in them

SYNTHESIS OF DIAZO COMPOUNDS FROM AMINO BENZOPYRANO THIAZOLES

ABSTRACT 8-Amino-6-chlorocoumarine (5) has been synthesized by multistep synthesis (by known literature methods) which involves the successive chlorination and nitration salicylaldehyde (1) to 5-chloro-3-nitrosalicyladehyde (3). The coumarin was synthesized by using Perkin reaction of 5-chloro-3-nitrosalicyladehyde. The nitro coumarin (4) obtained was reduced to 8-amino-6-chloro coumarin (5) which was then treated with bromine and potassium thiocyanate followed by the treatment of ammonia gives 2-amino-4-chloro-8H-chromeno-[8,7-d]-1,3-thiazol-8-one (6). The final 2-aminobenzo-1,3-thiazole derivative was diazotized and coupled with different phenols and anilines to yield diazo compounds. These compounds are then subjected to biological characterization