Synthesis of novel 4‐(1‐(2‐cyclopropylphenyl)‐2‐(4‐substituted‐1H‐1,2,3‐triazol‐1‐yl)ethyl)morpholine analogues were demonstrated by conventional synthetic procedures. The structure of all the newly synthesized compounds were determined by 1H‐NMR, 13C‐NMR, HRMS and CHN analysis. Cytotoxicity of all synthesized compounds were tested against MCF‐7 Cell lines in different concentrations. The IC50 value of compounds was calculated using graph Pad Prism Version5.1. 4‐chloro substituted analogue exhibited superior result than the standard reference Doxorubicin drug. Compounds which are containing 3‐methoxy, 2‐methoxy and 4‐methoxy substituents showed a moderate effect, and 2‐chloro, 3‐triflouromethyl and 2‐methyl substituted analogues showed lower results. Molecular docking studies performed on the crystal structure of human estrogen receptor alpha ligand‐binding domain with all molecules and are well in agreement with cell line studies. The predicted pharmacokinetics support that these compounds have more drug‐likeness properties.

A novel series of thiazole-triazole-piperazine multi hybrids was designed for antimicrobial activity and the synthetic method for this series has been developed by copper catalyzed 1,3-dipolar cycloaddition of thiazole-based azide with Boc-piperidine based alkyne in the presence of CuSO4 and sodium ascorbate. Boc deprotection followed by alkylation of piperidine moiety in hybrid derivatives was also carried out. All the target compounds were confirmed using FTIR, 1H NMR, 13C NMR and LC-MS spectral techniques. These compounds were screened for the antimicrobial activity against bacteria and fungi. The antimicrobial activities are also comparable to standard drugs ampicillin and clotrimazole. All the molecules showed good to moderate activity and supported by molecular docking studies and ADME prediction.

Novel series of fused heterocycles in which amino triazole fused to biphenyl thiazole were synthesized in a multistep reaction starting from 2-aminothiazole. The amino compound with ethoxy carbonyl isothiocyanate afforded the ethyl carbamate thiomide derivative of thiazole, which further underwent intramolecular cyclization with hydroxyl amine hydrochloride in presence of DIPEA to furnish the fused thiazolotriazole amine. Haloaryl group in the fused heterocycle under Suzuki coupling condition afforded biphenyl derivatives of fused thiazolotriazole amines. All the synthesized compounds were confirmed based on their spectral data.

In this study, we report the synthesis of a library of new 4-(3-nitro-2H-chromen-2-yl)-1,3-diphenyl-1H-pyrazol e analogues. Condensation of pyrazole carbaldehyde precursor with nitromethane yielded (E)-4-(2-nitrovinyl)-1,3-diphenyl-1H-pyrazole intermediate. This intermediate upon intermolecular cyclization with substituted salicylaldehydes individually, produced 4-(3-nitro-2H-chromen-2-yl)-1,3-diphenyl-1H-pyrazole analogues. The structures of compounds were confirmed by the interpretation of 1H-NMR, 13C-NMR and Mass spectral analysis.