Exploration of anti-inflammatory activity of pyrazolo[3,4-d]pyrimidine/1,2,4-oxadiazole hybrids as COX-2, 5-LOX and NO release inhibitors: Design, synthesis, in silico and in vivo studies.

New pyrazolo[3,4-d]pyrimidine derivatives 7a-h and 8a-h were synthesized and evaluated for their in vitro inhibitory potential against COX-1, COX-2, 5-LOX along with the NO release inhibitory activity to assess their anti-inflammatory potential. Most compounds confered inhibitory activity at a micromolar level and exhibited prominent selectivity towards COX-2 especially in the 8a-h series. The most useful compound 8e as a COX-2/5-LOX dual inhibitor, exhibited IC results of; 1.

In Vitro Antimycobacterial Activity and Physicochemical Characterization of Diaryl Ether Triclosan Analogues as Potential InhA Reductase Inhibitors.

Two sets of diphenyl ether derivatives incorporating five-membered 1,3,4-oxadiazoles, and their open-chain aryl hydrazone analogs were synthesized in good yields. Most of the synthesized compounds showed promising in vitro antimycobacterial activity against H37Rv. Three diphenyl ether derivatives, namely hydrazide , oxadiazole and naphthylarylidene exhibited pronounced activity with minimum inhibitory concentrations (MICs) of 0.

Design, synthesis and anticancer activity of novel valproic acid conjugates with improved histone deacetylase (HDAC) inhibitory activity.

Twenty-five valproic acid conjugates have been designed and synthesized. All target compounds were explored for their in vitro anti-proliferative activities using the MTT-based assay against four human cancer cell lines includingliver (HePG2), colon (HCT116), breast (MCF7) and cervical (HeLa) carcinoma cell lines. Out of six valproic acid-amino acid conjugates 2a-f.

Design, synthesis and biological evaluation of novel 5-((substituted quinolin-3-yl/1-naphthyl) methylene)-3-substituted imidazolidin-2,4-dione as HIV-1 fusion inhibitors.

A series of novel 5-(substituted quinolin-3-yl or 1-naphthyl)methylene)-3-substituted imidazolidin-2,4-dione 9-26 was designed and synthesized. The prepared compounds were identified using H NMR, C NMR as well as elemental analyses. The inhibitory activity of 9-26 on HIV-1 replication in MT-2 cells was evaluated.