Mallikarjun B. Kalashetti

Synthesis, hypoglycemic and hypolipidemic activities of novel thiazolidinedione derivatives containing thiazole/triazole/oxadiazole ring.

Novel thiazolidinedione derivatives were synthesized by incorporating pharmacologically significant heterocycles viz, substituted thiazole, triazole, and oxadiazole moieties linked to the central phenyl ring via heteroatomlinkage with one/two carbon spacer as the structural analogs of Pioglitazone by employing multistep synthetic protocols. Structures of all the newly synthesized intermediates and target molecules were established by analytical and spectral data. These newly synthesized compounds were screened for their invivo hypoglycemic and hypolipidemic activities in male wistar rats. Some of the synthesized compounds demonstrated good activity.

Benzothieno[3,2-e][1,2,4]triazolo[4,3-c]pyrimidines: Synthesis, Characterization, Antimicrobial Activity, and Incorporation into Solid Lipid Nanoparticles

Fused triazolothienopyrimidines were prepared from the corresponding 2‐amino‐4,5,6,7‐tetrahydrobenzo[b]thiophene‐3‐carbonitrile. These precursors were intern prepared by employing the Gewalds reaction. All the newly synthesized compounds were characterized by spectral and analytical data. Title compounds displayed promising antibacterial and antifungal activities. Compound 3h which exhibited good antimicrobial activity was incorporated into SLN and characterized for particle size, entrapment efficiency (EE%), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and in‐vitro release studies. It showed narrow particle size distribution with high entrapment efficiency. In‐vitro release study of compound loaded SLNs in phosphate buffer of pH 7.4, exhibited a biphasic pattern with an initial burst and prolonged release over 24 h.

Synthesis and local anaesthetic activities of 2-aminothiazole/thiadiazole analogues of lidocaine

Various 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.Graphical AbstractVarious 2-aminothiazole and 2-aminothiadiazole derivatives viz N-[4-(2-Chloro-4-fluoro-phenyl)-thiazol-2-yl]-2-substituted acetamides (3a, 4a, 5a) and N-[5-(4-substituted aryl)-[1,3,4]thiadiazol-2-yl]-2-acetamides (3b, 3c, 4b, 4c, 5b, 5c) were synthesized from their corresponding properly substituted 2-aminothiazoles and 2-aminothiadiazoles. Structures of all the newly synthesized compounds were established by analytical and spectral data. Synthesized compounds were screened for their local anaesthetic activity using the rat sciatic nerve model.

Synthesis, characterization, antibacterial and antifungal activity of thienopyrimidines and triazolothienopyrimidines

Aseries of novel triazole fused tetracyclic thienopyrimidines (III – X) were synthesized from the corresponding precursor 5-amino-4-cyano-3-methylthiophene-2-carboxylic acid ethyl ester I. The precursor were in turn prepared via the Gewald reaction. Structures of all the newly synthesized compounds were characterized by spectral and analytical data. All the tested compounds displayed promising antibacterial and antifungal activities.

6-Chloro-3-[(di­methyl­amino)­methyl­idene]thio­chroman-4-one

The asymmetric unit of the title compound, C12H12ClNOS, contains three independent molecules, with the thiochroman ring adopting a sofa conformation in each one. The crystal structure features C—H⋯O interactions; one of the O atoms accepts three such bonds. Together, the hydrogen bonds give rise to a molecular tape propagating in [010].

Declination in the fertility of lands due to the flood in Bagalkot district

Soil plays a very vital role as it produces food for human beings and animals. The organic matter in soil as decomposed by a host of micro organism. Due to human activities, soil is the receptor of many pollutants including pesticides, fertilizers, etc., Hence, soil is an important component of environmental chemical cycle.

4-Imino-2,7-dimethyl-5,6,7,8-tetra­hydro-4H-1-benzothieno[2,3-d]pyrimidin-3-amine

In the title compound, C12H16N4S, the fused benzothiophene and the pyrimidine rings are coplanar [dihedral angle = 1.61 (6)°]. Three C atoms of the cyclohexene ring (at positions 3, 6 and 7) are disordered over two sites with an occupancy ratio of 0.702 (8):0.298 (8). The cyclohexene ring in both the major and minor components adopts a half-chair conformation. The crystal structure is stabilized by N—H⋯N and C—H⋯N interactions, resulting in the formation of inversion dimers with R 2 2(10) and R 2 2(12) graph-set motifs.

2-Amino-4-methyl-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile

In the title compound, C10H12N2S, the thiophene ring is essentially planar (r.m.s. deviation = 0.0290 Å). The two C atoms of the cyclohexene ring (at positions 6 and 7) are disordered over two sets of sites in a 0.810 (5):0.190 (5) ratio. The cyclohexene rings in both the major and minor occupancy conformers adopt a half-chair conformation. In the crystal, there are two types of N—H⋯N interaction. One of these results in centrosymmetric head-to-head dimers corresponding to an R 2 2(12) graph-set motif and the other forms a 20-membered macrocyclic ring involving six molecules.