Anti-HIV Activity of New Substituted 1,3,4-Oxadiazole Derivatives and their Acyclic Nucleoside Analogues

Abstract

A number of new 5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazole derivatives, 2 -5 and 8 -11, were synthesized. The 2-{5-[(naphthalen-5-yloxy)methyl]-1,3,4-oxadiazol-2-ylthio}acetohydrazones 6a and 6b were synthesized by the reaction of the hydrazide 4 with the corresponding monosaccharides. Cyclization of the sugar hydrazones 6a and 6b with acetic anhydride afforded the substituted oxadiazoline derivatives 7a and 7b. The synthesized compounds were evaluated for their antiviral activity against, the human immunodefi ciency virus (HIV-1) and some of these compounds showed moderate to high antiviral activity.

Synthesis andin VitroAntimicrobial Activity Screening of New 3‐Acetyl‐2,5‐disubstituted‐1,3,4‐oxadiazoline Derivatives

“…In this research, we synthesized thirteen new 1,3,4oxadiazoline derivatives (14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26) and evaluated them for their in vitro antimicrobial activity. New 1,3,4-oxadiazoline derivatives were obtained in the reaction of corresponding hydrazide-hydrazones of isonicotinic acid with acetic anhydride.…”

“…[8] They may also function as modulating molecular properties by positioning substituents in the periphery of the molecule. [9] Unique antibacterial, [10][11][12][13] antifungal, [11][12][13] antitubercular, [14] antiviral, [15] analgesic, [16] anti-inflammatory, [16,17] anticancer, [18,19] anticonvulsant, [20,21] antioxidant [22] and antidiabetic properties [23] provide a range of possibilities of potential applications of oxadiazole-based derivatives in the field of medical chemistry.…”

Design, synthesis, antimicrobial evaluation, and molecular docking studies of novel symmetrical 2,5‐difunctionalized 1,3,4‐oxadiazoles

“…1,3,4‐Oxadiazoles are valuable five‐membered aromatic heterocycles that possess a wide range of biological properties, including antibacterial, antifungal, antiviral, anti‐inflammatory, antiparasitic, and anti‐HIV activities. Some examples of drugs used in clinical medicine, containing the 1,3,4‐oxadiazole unit, are furamizole, which is an antibiotic drug, and raltegravir, an antiretroviral medication used to treat HIV infection (Figure ).…”

Synthesis and Antimicrobial Activity of Novel Heterocycles Containing Thiazolidinone and 1,3,4-Oxadiazole Moieties

“…The derivatives of 1,3,4-oxadiazoles have been used as pharmacophores due to their favorable metabolic profile and ability to engage in hydrogen bonding [7]. The diverse pharmacological activities of both these moieties are widely exploited [8][9][10][11][12][13][14][15][16][17][18][19][20] as they are not only synthetically important but also possess a wide range of promising pharmacological activities. Keeping this in view, the authors have outlined simple and maneuverable synthetic methodologies for drugs containing 4-thiazolidinone and 1,3,4-oxadiazole scaffolds and evaluated for their antimicrobial activitiy.…”