Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review

In order to optimize a lead molecule for further development, bioisosteric replacements are generally adopted as one of the strategies. Silicon appears to be the right choice as a carbon isostere because of the similarity in chemical properties. Silicon can be strategically introduced in a molecule to modulate its druglike properties, providing medicinal chemists with an unconventional strategy for replacing a carbon atom. Silicon can also be introduced to replace other heteroatoms and can act as a surrogate of functional groups such as olefin and amide as well. The present Perspective focuses on the opportunities that silicon incorporation offers in drug discovery, with an emphasis on case studies where introduction of silicon has created a benefit over its analog. We have tried to highlight all the recent developments in the field and briefly discuss the challenges associated with them.

Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds

Recent advances of pyrazole-containing derivatives as anti-tubercular agents.

Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target.

Chemical matter is needed to target the divergent biology associated with the different life cycle stages of Plasmodium. Here, we report the parallel de novo screening of the Medicines for Malaria Venture (MMV) Pandemic Response Box against Plasmodium asexual and liver stage parasites, stage IV/V gametocytes, gametes, oocysts and as endectocides. Unique chemotypes were identified with both multistage activity or stage-specific activity, including structurally diverse gametocyte-targeted compounds with potent transmission-blocking activity, such as the JmjC inhibitor ML324 and the antitubercular clinical candidate SQ109. Mechanistic investigations prove that ML324 prevents histone demethylation, resulting in aberrant gene expression and death in gametocytes. Moreover, the selection of parasites resistant to SQ109 implicates the druggable V-type H+-ATPase for the reduced sensitivity. Our data therefore provides an expansive dataset of compounds that could be redirected for antimalarial development and also point towards proteins that can be targeted in multiple parasite life cycle stages. Here, Reader et al. screen the Medicines for Malaria Venture Pandemic Response Box in parallel against Plasmodiumasexual and liver stage parasites, stage IV/V gametocytes, gametes, oocysts and as endectocides. They identify two potent transmission-blocking drugs: a histone demethylase inhibitor ML324 and the antitubercular SQ109.

/pdf/multistage-and-transmission-blocking-targeted-antimalarials-12q1q1t0fr.pdf

Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box

Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.

A General Approach to N‐Heterocyclic Carbenes with a Fused Tetracyclic Core: Ligands for Suzuki–Miyaura Cross‐Coupling Reaction

The present invention relates to novel N-heterocyclic carbenes compounds and process of the preparation thereof. The present invention further relates to the use of use of these novel N-heterocyclic carbenes as ligand in the Suzuki-Miyaura cross coupling reactions.

Novel n-heterocyclic carbene compounds, their preparation and use

The synthesis of a novel N-heterocyclic carbene complex composed of a tetracyclic scaffold is disclosed and its usability as a ligand in Pd-catalyzed Suzuki—Miyaura cross-coupling reactions is demonstrated.

A General Approach to N-Heterocyclic Carbenes with a Fused Tetracyclic Core: Ligands for Suzuki—Miyaura Cross-Coupling Reaction.

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Papers

Repurposing of a drug scaffold: Identification of novel sila analogues of rimonabant as potent antitubercular agents.

A General Approach to N‐Heterocyclic Carbenes with a Fused Tetracyclic Core: Ligands for Suzuki–Miyaura Cross‐Coupling Reaction

Novel n-heterocyclic carbene compounds, their preparation and use

A General Approach to N-Heterocyclic Carbenes with a Fused Tetracyclic Core: Ligands for Suzuki—Miyaura Cross-Coupling Reaction.