Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents

Thienopyrimidines are widely represented in the literature, mainly due to their structural relationship with purine base such as adenine and guanine. This current review presents three isomers—thieno[2,3-d]pyrimidines, thieno[3,2-d]pyrimidines and thieno[3,4-d]pyrimidines—and their anti-infective properties. Broad-spectrum thienopyrimidines with biological properties such as antibacterial, antifungal, antiparasitic and antiviral inspired us to analyze and compile their structure–activity relationship (SAR) and classify their synthetic pathways. This review explains the main access route to synthesize thienopyrimidines from thiophene derivatives or from pyrimidine analogs. In addition, SAR study and promising anti-infective activity of these scaffolds are summarized in figures and explanatory diagrams. Ligand–receptor interactions were modeled when the biological target was identified and the crystal structure was solved.

A Systematic Review on Synthetic and Antimicrobial Bioactivity of the Multifaceted Hydrazide Derivatives

: To overcome the upsurge of antimicrobial resistance that has emerged in recent years, there is a need for the development of newer hits having gratifying anti-infective activity. Hydrazides incorporated with an azomethine hydrogen account for a cardinal class of molecules for the development of newer derivatives. Hydrazide derivatives have gainedconsiderable interest of medicinal chemists owing to their diverse bioactivity. In the present review, we have attempted to compile the recent trends in the synthesis of hydrazides and their substituted derivatives. The structural features that lead to the desired antimicrobial activity are highlighted, which will lead the way for synthetic and medicinal chemists to focus on newer designs in this arena.

Anti-infective Potential of Manzamine Alkaloids – A Review

Background: From time immemorial, natural products have been used for the treatment of various diseases. Various natural products, their semisynthetic derivatives, and synthetic analogs have been explored for their anti-infective properties. One such group of natural compounds that have been widely explored is manzamine alkaloids. Manzamine alkaloids are complex natural compounds consisting of a β-carboline nucleus attached to a pentacyclic ring system that was first isolated from a marine sponge during the 1980s. Objective: The review aims to provide a critical overview of the anti-infective potential of manzamine alkaloids. Method: A comprehensive and exhaustive review of the literature on manzamine alkaloids consisting of their isolation, anti-infective properties, and mechanism of action is presented. Results: Various manzamine alkaloids have been isolated and found to exhibit potent anti-infective activities like antibacterial, antimalarial, antiviral, antifungal, antileishmanial, among others. These manzamine alkaloids exhibit their anti-infective activity by inhibiting targets like GSK-3β and MtSK. Conclusion: This present review with structure-activity relationship study of manzamine alkaloids for their anti-infective activity will be useful for further development of semisynthetic manzamine analogs as potent anti-infective agents with better therapeutic potential and reduced toxicity.

Clinical and metabolic effects of the original iodine metabolic composition in the experiment on calves

The article provides a theoretical justification for the development of a complex iodine metabolic composition based on an iodinepolymer complex (iodinol) and succinic acid. The research on the effectiveness of the proposed composition for the correction of energymetabolic disorders in calves with severe iodine deficiency was carried out. The objects of research were calves with clinical signs of iodine deficiency and pronounced energy metabolic disorders. During the experiment, it was found that the test calves showed a marked improvement in the clinical condition. The thyroid status normalized, the total protein and glucose indicators approached the physiological norm, and the reserve alkalinity of the blood increased. The energetic metabolic effect was due to the combined action of iodinol and succinic acid. The obtained results indicate the opening prospect of an injection method for the use of an iodine polymer complex based on iodine-iodide with polyvinyl alcohol (iodinol) in combination with sodium succinate, not only as an effective approach to cupping and eliminating the iodine deficiency symptoms, but also as an active energy-metabolic drug with a potentially high anti-infective activity.