Prajwal L. Lobo

Synthesis and biological evaluation of some 1,3,4-oxadiazole derivatives.

The acid hydrazides (2) derived from ibuprofen and 4-methylthiophenyl acetic acids have been subjected to cyclization with carbon disulphide under basic conditions to yield 1,3,4-oxadiazol-2-thiones (3) which on aminomethylation with formaldehyde and secondary amines afforded a series of Mannich bases (4 and 5). Purity of the compounds has been confirmed by TLC. Structures of these compounds were established on the basis of elemental analyses and spectral studies. The newly synthesized compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic and antimicrobial activities.

Synthesis, antimicrobial and antioxidant activities of 2-[1-{3,5-diaryl-4,5-dihydro-1H-pyrazolenyl}]-4-(4-nitrophenyl)-[1,3]-thiazoles

In this study, various substituted chalcones, prepared by condensing substituted acetophenones with substituted aldehydes/arylfurfurals, were treated with thiosemicarbazide in basic media to produce 1-thiocarbonyl-3,5-disubstituted pyrazolines which on further reaction with substituted phenacyl bromides afforded the title compounds in good yield. Structures of the newly synthesized compounds were assigned on the basis of elemental analyses, IR, 1H NMR, and mass spectral studies. The newly synthesized compounds were tested for their in vitro antibacterial and antifungal activities against a variety of microorganisms and antioxidant activities by diphenylpicrylhydrazyl radical scavenging assay. Among the derivatives, compounds 3b, 3e, 6a, and 6h were identified as potent antioxidants. Compounds 3d, 3e, and 6a–f have emerged as the most promising antimicrobial agents displaying the maximum activity against all the tested microorganisms.

Three-Component Reaction: Synthesis, Characterization, and Biological Study of Some Fused Bridgehead Nitrogen Heterocyclic Systems Containing 4-Methylthiophenyl Moiety

Abstract Several substituted thiazolo-[3,2-b]-1,2,4-triazole derivatives 4 were synthesized by a one-pot, three-component reaction of 3-(4-methylthiobenzyl)-1,2,4-triazole-5-thiol 3, substituted 5-aryl-furan-2-carboxaldehydes/substituted aromatic aldehydes, and monochloroacetic acid in acetic acid using acetic anhydride and anhydrous sodium acetate. Compound 3 was obtained from 4-methylthiophenyl acetic acid by esterification followed by hydrazinolysis. All structures of the newly synthesized compounds were elucidated by elemental analysis and spectral data. The newly synthesized compounds were also screened for their antimicrobial and anti-inflammatory activities. Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. GRAPHICAL ABSTRACT

Synthesis of Some Fused Triazole Derivatives Containing 4-Isobutylphenylethyl and 4-Methylthiophenyl Moieties

A series of substituted [1,3]thiazolo[3,2-b][1,2,4]triazole derivatives 4 were synthesized in good yield by condensing 2-substituted-1,2,4-triazole-5-thiols 3 with various N-aryl-maleimides in acetic acid media. All structures of the newly synthesized compounds were elucidated by elemental analyses and spectral data. Graphical Abstract Synthesis of Some Fused Triazole Derivatives Containing 4-Isobutylphenylethyl and 4-Methylthiophenyl Moieties

Synthesis and antimicrobial evaluation of some new 2-(6-oxo-5,6-dihydro[1,3]thiazolo[3,2-b]-2-aryloxymethyl-1,2,4-triazol-5-yl)-N-arylacetamides.

A series of 2-(6-oxo-5,6-dihydro[1,3]thiazolo[3,2-b]-2-aryloxymethyl-1,2,4-triazol-5-yl)-Narylacetamides 6 were synthesized in good yield by condensing 5-aryloxymethyl-4H-1,2,4-triazole- 3-thiol 5 with various substituted N-phenyl-maleimides in acetic acid media. The newly synthesized compounds were characterized by spectral data and tested for their in vitro antibacterial and antifungal activity against a variety of microorganisms. Graphical Abstract Synthesis and Antimicrobial Evaluation of Some New 2-(6-Oxo-5,6- dihydro[1,3]thiazolo[3,2-b]-2-aryloxymethyl-1,2,4-triazol-5-yl)-Narylacetamides

Synthesis, Characterization and Biological Studies of Some Bioactive Thiazolotriazole Derivatives

The key precursor rac-2-(4-isobutylphenyl)ethyl-1,2,4-triazole-5-thione (3) was synthesized in good yield from Ibuprofen (1). One-pot three-component reactions of 3 with 5-aryl-furan-2-carboxaldehydes/ substituted aromatic aldehydes and monochloroacetic acid in acetic acid in the presence of acetic anhydride and anhydrous sodium acetate afforded substituted thiazolo[3,2-b][1,2,4]triazole derivatives 4 and 5. The structures of the newly synthesized compounds were elucidated by elemental analyses and spectral data. The compounds were tested for their in-vitro antimicrobial activities. Graphical Abstract Synthesis, Characterization and Biological Studies of Some Bioactive Thiazolotriazole Derivatives