62946-50-3

Upstream product

• 140-53-4 p-chlorobenzyl cyanide 
• 10200-59-6 Thiazole-2-carbaldehyde 
• 873-77-8 (4-chlorphenyl)magnesium bromide 

Downstream Products

• 62946-51-4 (4-chloro-3-nitro-phenyl)-thiazol-2-yl-methanone 
• 949934-48-9 (4-chlorophenyl)[4-(pyrrolidin-1-ylmethyl)phenyl](thiazol-2-yl)methanol 

Relevant academic research and scientific papers

DDQ-induced dehydrogenation of heterocycles for c-c double bond formation: Synthesis of 2-thiazoles and 2-oxazoles

Strong as an Ox: 2-Thiazoles and 2-oxazoles are formed by oxidation of 2-thiazolines and 2-oxazolines without requiring substituents at the C4 and C5 positions. DDQ plays an important role as the oxidant in this transformation and metal is unnecessary. This general procedure shows good functional group tolerance and provides a wide variety of 2-thiazoles and 2-oxazoles in moderate to excellent yields.

Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: Design, synthesis, and biological and structure-activity relationship studies

We describe herein the design, synthesis, biological evaluation, and structure-activity relationship (SAR) studies of an innovative class of antimalarial agents based on a polyaromatic pharmacophore structurally related to clotrimazole and easy to synthesize by low-cost synthetic procedures. SAR studies delineated a number of structural features able to modulate the in vitro and in vivo antimalarial activity. A selected set of antimalarials was further biologically investigated and displayed low in vitro toxicity on a panel of human and murine cell lines. In vitro, the novel compounds proved to be selective for free heme, as demonstrated in the β-hematin inhibitory activity assay, and did not show inhibitory activity against 14-α-lanosterol demethylase (a fungal P450 cytochrome). Compounds 2, 4e, and 4n exhibited in vivo activity against P. chabaudi after oral administration and thus represent promising antimalarial agents for further preclinical development.

ANTIMALARIAL AGENTS HAVING POLYAROMATIC STRUCTURE

Antimalarial agents having a novel pharmacophore of formula (I) are herein described. These polycyclic compounds are able to inhibit chloroquine-sensitive and chloroquine-resistant strains ofPlasmodium falciparum (Pf). Furthermore, the synthesis of these compounds involves few steps from commercial products with low cost of production.Λa présente invention concerne des agents antimalariaux comportant un nouveau pharmacophore de formule (I). Ces composés polycycliques sont susceptibles d''inhiber les souches sensibles à la chloroquine et résistantes à la chloroquine de Plasmodium falciparum (Pf). En outre, la synthèse de ces composés est peu onéreuse et implique peu d''étapes à partir des produits commerciaux.

Anthelmintic pyridine and thiazole substituted benzimidazole carbamates

Compounds represented by the formula STR1 wherein R is STR2 R1 is 2-pyridyl, 3-pyridyl, 4-pyridyl or 2-thiazyl, R2 is lower alkyl and n is 1 or 2, And acid addition salts of the compounds wherein R1 is 2-pyridyl, 3-pyridyl or 4-pyridyl are disclosed as useful as anthelmintics against a broad spectrum of helminths. Processes for making the active compounds and novel intermediates useful therein are also disclosed.