Synthesis of New Potential Chemotherapeutic Agents Incorporating Naproxen Sub-Structure

A Series Of Potential Biologically Active Compounds Have Been Synthesized Through The Derivatization of Carboxyl Group In Naproxen Core Structure Involving The Conversion The Naproxen To Its Methyl Ester Then To TheAcid Hydrazide. The Acid Hydrazide Of Naproxen Was Incorporated With Hydrazones, Diamide Linkage, Oxadiazole, Pyrazolone, Triazole, Quinazoline And Indole Containing Motifs. The Targeted Compounds Have Been Achieved In A Very Good Yield Under Conventional Heat And Irradiation Conditions. All Compounds Have Been Characterized By Ir, 1h-Nmr, 13c-Nmr And Mass Spectra.Keywords: Naproxen; Anti-Inflammatory; Nsaid's

3-(1-Adamant­yl)-4-amino-1-(2-benzoyl-1-phenyl­eth­yl)-1H-1,2,4-triazol-5(4H)-thione

In the title compound, C27H30N4OS, the 3-(adamantan-1-yl)-4-amino-1H-1,2,4-triazole-5(4H)-thione unit and the O atom are each disordered over two sets of sites with refined site-occupancies of 0.7630 (13) and 0.2370 (13). The 1,2,4-triazole ring of the major component forms dihedral angles of 62.61 (17) and 61.93 (16)° with the benzene rings, while that of the minor component makes corresponding angles of 86.3 (4) and 79.1 (4)°. The dihedral angle between the benzene rings is 39.21 (16)°. The mol­ecular structure is stabilized by an intra­molecular C—H⋯N hydrogen bond, which generates an S(6) ring motif. In the crystal, mol­ecules are linked into inversion dimers by pairs of N—H⋯S hydrogen bonds

N′-[(1E)-(4-Fluoro­phen­yl)methyl­idene]thio­phene-2-carbohydrazide

In the title compound, C12H9FN2OS, the thienyl ring is disordered over two positions, with the S atom of the major component [occupancy = 87.08 (16)°] oriented towards the ortho-H atom of the benzene ring. The mol­ecule is nearly planar, the dihedral angle between the thio­phene and benzene rings being 13.0 (2)° in the major component. The azomethine C=N double bond in the mol­ecule is of an E configuration. In the crystal, mol­ecules are linked by pairs of N—H⋯O hydrogen bonds, forming inversion dimers

Synthesis of New Potential Chemotherapeutic Agents Incorporating Naproxen Sub-Structure

A Series of Potential Biologically Active Compounds Have Been Synthesized Through the Derivatization of Carboxyl Group in Naproxen Core Structure Involving the Conversion the Naproxen to its Methyl Ester then to the Acid Hydrazide. The Acid Hydrazide of Naproxen was incorporated with Hydrazones, Diamide Linkage, Oxadiazole, Pyrazolone, Triazole, Quinazoline and Indole Containing Motifs. The Targeted Compounds have been achieved in a very good yield under Conventional Heat and Irradiation Conditions. All Compounds have been characterized by Ir, 1h-Nmr, 13c-Nmr and Mass Spectra

2-{[5-(Adamantan-1-yl)-4-methyl-4H-1,2,4-triazol-3-yl]sulfan­yl}-N,N-dimethyl­ethanamine

In the title compound, C17H28N4S, the 1,2,4-triazole ring is nearly planar [maximum deviation = 0.005 (2) Å]. There are no significant hydrogen bonds observed in the crystal structure. The crystal studied was a non-merohedral twin, the refined ratio of twin components being 0.281 (3):0.719 (3)

Impact of Geometric Parameters, Charge, and Lipophilicity on Bioactivity of Armed Quinoxaline, Benzothiaole, and Benzothiazine: Pom Analyses of Antibacterial and Antifungal Activity

<div><p></p><p>A series of four different armed heterocyclic candidates; 1-(2-methyl-2,3-dihydro-1,3-benzothiazol-2-yl)acetone (<b>2</b>), 1-(3-methyl-4H-1,4-benzothiazin-2-yl)ethanone (<b>3</b>), 2-[(2-aminophenyl)dithio]aniline (<b>4</b>), and 3-hydroxy-3-methyl-4-(3-methyl-2-quinoxalinyl)-2-butanone (<b>5</b>) have been prepared and their microbial activities were evaluated. A correlation of the structure and activities relationships of these compounds with respect to molecular modeling, Lipinski Rule of Five, drug likeness, toxicity profiles, and other physico-chemical properties of drugs are described and verified experimentally.</p></div