Pyrazole Linked-1,2,4-Oxadiazole Derivatives as Potential Pharmacological Agent: Design, Synthesis and Antimicrobial Study was written by Kulkarni, Pravin S.;Sarda, Swapnil R.;Khandebharad, Amol U.;Farooqui, Mazahar;Agrawal, Brijmohan R.. And the article was included in Polycyclic Aromatic Compounds.Safety of Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate The following contents are mentioned in the article:
A new series of 3-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-5-aryl-1,2,4-oxadiazole I (R = H, 4-Cl, 4-OMe, 3,4-(OMe)2; R1 = H, 2-Cl, 4-Cl, 4-Me, 4-OMe, 2,3-(OMe)2) have been synthesized by a reaction of 5-aryl-N′-hydroxy-1-phenyl-1H-pyrazole-3-carboximidamide with substituted Me benzoate. The newly synthesized compounds I were characterized by spectroscopic techniques and screened for in vitro antibacterial activity against Gram-pos. bacterial strains Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178). Gram-neg. bacterial strains Escherichia coli (NCIM 2574), it was noticed that compounds I (R = 4-Cl; R1 = 2-Cl, 4-Cl, 4-Me) showed good activity against B. subtilis with MIC 31.25 μg/mL against standard S. albus having MIC 7.81 μg/mL. Proteus mirabilis (NCIM 2388) and in vitro antifungal activity against Aspergillus niger (ATCC 504) Candida albicans (NCIM 3100). Compounds I (R, R1 = H), I (R = H, R1 = 2-Cl), I(R = H, R1 = 4-Me), and I (R = 4-Cl, R1 = 4-OCH3) showed good activity against A. niger with MIC 31.25 μg/mL, which are comparable to standard drug ravuconazole having MIC 31.5 μg/mL. Compounds I (R = 4-Cl, R1 = 2-Cl) and I (R = 4-Cl, R1 = 4-CH3) showed activity against A. niger with MIC 7.81 μg/mL which is comparable to standard drug Fluconazole having MIC 7.81 μg/mL and fourfold more activity with respect to drug Ravuconazole. The antibacterial activity of compounds I led to the conclusion that these scaffolds could aid in the creation of lead drugs to treat microbial infection. This study involved multiple reactions and reactants, such as Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate (cas: 17355-75-8Safety of Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate).
Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate (cas: 17355-75-8) belongs to pyrazole derivatives. Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. Pyrazole rings have been used as core components of several leading non-steroidal anti-inflammatory drugs (NSAIDs) and antihypertensive drugs. It has also been found to be useful as a bifunctional ligand for metal catalysis.Safety of Ethyl 1,5-diphenyl-1H-pyrazole-3-carboxylate
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics