Design, Synthesis and Biological Evaluation of Novel Furan & Thiophene Containing Pyrazolyl Pyrazolines as Antimalarial Agents

Aryl glyoxal: a prime synthetic equivalent for multicomponent reactions in the designing of oxygen heterocycles

“…17 Likewise, the pyrazoline derivative containing a furan moiety shows anti-malarial activity against Plasmodium falciparum . 18 Isoxazoles, as oxygen-nitrogen heterocycles, add to the synthetic utility of oxygen heterocycles as they offer anti-tubercular, 19 anti-inflammatory, 20 and COX-2 inhibitor properties, 21 and are thus a constituent of many therapeutic drugs. The newly synthesized 2 H -chromene-2-one derivative was tested and found to show the potential anti-convulsant 22 activity.…”

Thiophene‐containing compounds with antimicrobial activity

“…Claisen-Schmidt condensation of three 1-aryl-3-(thiophen-2-yl) pyrazole-4-carboxaldehydes with 3-acetyl-2,5-dimethylfuran afforded chalcone analogs 29 (Figure 4), which were further converted into pyrazolines 30 through ring closure with hydrazine. [43] Chalcone analog 29 (R = Br, R 1 = H) was the most potent compound in the series against E. coli (MIC = 62.5 μg/ml) compared to chloramphenicol (MIC = 50 μg/ml) and had a moderate activity against S. aureus (MIC = 125 μg/ml). The corresponding pyrazoline 30 (R = Br, R 1 = H) was also moderately potent (MIC = 125 μg/ml) against E. coli and P. aeruginosa, while its analog 30 (R = R 1 = H) had a similar activity against S. aureus and P. aeruginosa.…”

Synthesis of some new antipyrine-thiophene hybrids and their evaluations as antioxidant and antibacterial agents

“…They occupy a unique position because advances in their synthesis, availability, stability, and structural simplicity make them useful scaffolds in pharmaceuticals and other therapeutics, like the best-selling drugs Olanzepine and Tinoridine [1][2][3] (Figure 1). Furthermore, thiophene derived molecules displayed a variety of pharmacological properties, including anti-inflammatory [4], antimicrobial [5], antihypertensive [6], anti-atherosclerotic properties [7], cytotoxicity in several cancer cell lines [8,9], tubulin polymerization [10,11], antioxidant [12], inhibitor for acetyl-CoA carboxylase [13], STAT3 inhibitors [14], antidepressant [15], antidepressant, anti-diabetic [16], anti-tubercular [17], antifungal [18], enzyme inhibitor [19], anti-malarial drugs [20] and are used in the treatment of asthma [21]. On the other hand, thiophene derivatives are the largest class of industrial chemistry, thermal, optoelectronic properties and material science because of their wide utilized applications, such as materials for electroluminescence devices [22,23], corrosion inhibitors [24], organic semiconductors [25], organic field-effect transistors (OFETs), and in the fabrication of organic light-emitting diodes (OLEDs) [26], synthesis of fluorescent chemo sensors [27].…”