Medicinal Chemistry

Thiadiazole compounds have versatile activities such as anti-microbial, anti-inflammatory, anticancer, etc. Present study involves design of thiadiazole compounds as antidiabetic agent using docking studies. The designed molecules were synthesized and subjected to antidiabetic activity by in vitro and in vivo method. Compound TD7 was found to show potent antidiabetic activity in alloxan induced diabetes rat model. Molecular docking revealed that synthesized derivatives and target proteins were actively involved in binding and had significant correlation with biological activity.

A facile, convenient and high yielding synthesis of novel Acrylohydrazide thioglycosides via one-pot reaction of the potassium thiolate salts of aglycon part - prepared from readily available starting materials - with 2,3,4,6-tetra-O-acetyl- α-D-gluco- and galactopyranosyl bromides . Pharmacological evaluation of compounds 8j, 8b, 8h, 8k, 8f and 5b in vitro against (MCF-7) cell line (Breast carcinoma cell line) showing high- moderate anti-tumor activities with IC50 values ranging from 3.69-14.93 (μM), moreover molecular modeling of these compounds revealed that they have high binding affinity through hydrophobic-hydrophobic interaction and moderate selectivity through the hydrogen bond interaction with the atypical nucleotide binding pocket in the amino terminus of Hsp90.

Nanotechnology is the manipulation of material on an atomic and molecular scale; by changing its physical, chemical and biological properties to produce novel materials, devices, and systems. Nanomaterials exhibit remarkable characteristics such as high surface to volume ratio, catalytic activity, and biocompatibility which make them suitable for various biomedical applications. Nanotechnology have prospective to improve the whole healthcare process for patient; starts from diagnosis to treatment and follow-up monitoring. Medical diagnosis based on nanotechnology provides two major advantages: rapid testing and early diagnosis. The potential contributions of c in the medical diagnosis are extremely broad and improve traditional diagnostic tools and methods in the field of clinical diagnosis, imaging and electro- diagnosis. Emerging modalities such as biochip, microarray, nanobarcode, micro-electromechanical systems, lab on chip and nanobiosensor have revolutionized the field of medical diagnosis. Nanoscale materials and nano-enabled techniques are used for diagnosis of various diseases such as cardiovascular diseases, cancer, diabetes, infectious disease, musculoskeletal and neurodegenerative disease etc. Among all medical applications of nanotechnology, nanobiosensor especially enzyme nanobiosensor are sensitive, reliable, robust, reproducible and cost effective diagnostic tool to meet the requirements of healthcare.

Isatin (1H-indole-2,3-dione) and its analog, are versatile substrates which acts as a precursor for large number of pharmacologically active compounds, thus having a significant importance in the synthesis of different heterocyclic compound.Isatin shows varity of biological activities such as antimicrobial, anticancer, antiviral, anticonvulsant, antiinflammatory and analgesic.This review focused on isatin synthetic methods and its biological activity as anticonvulsant. An Isatin derivative shows potent anticonvulsant activity at low concentration among all the derivatives, Schiff bases are found to be most potent anticonvulsant agent.

A series of Isoninicotinic acid hydrazide (INH) incorporated derivatives of thiazolidin-4-one (2a-h, 3a-h), azetidin-2- one (4a-h) and 1,3,4-oxadiazole (5a-h) were synthesized in satisfactory yield and pharmacologically evaluated for their in vitro antifungal activity. All the synthesized compounds were in good agreement with elemental and spectral data. A majority of the tested compounds showed good to moderate antifungal activity against all tested pathogenic fungal strains. To evaluate the toxicity of the compounds on liver, estimation of enzymes was also carried out.

Emerging epidemiological evidence suggests that T2DM may be associated with an increased risk of certain cancers. However, the underlying molecular mechanism linked these two diseases remains largely unknown. SHP2, a non-receptor protein tyrosine phosphatase encoded by pro-oncogene PTPN11, has been reported involved in insulin resistance through PI3K/Akt/mOTR signaling and has also been considered to play a vital role in carcinogenesis via Ras/Erk pathways. Based on our previous studies, we hypothesize that SHP2 may present a key molecule linked both T2DM and cancers through both Ras/Erk and PI3K/AKT/mTOR signaling pathways. We believe that the comprehensive and detailed investigation of SHP2 may provide a new insight into the underlying molecular mechanism linked both T2DM and cancers, thereby facilitating the process to discover novel therapeutic targets to prevent and treat cancers.