Isolation, Structural Elucidation, and Biological Activity of the Chemical Constituents of the Plants belonging to Family Betulaceae and Apiaceae. 

Isolation, structure elucidation and biological activities of extracts obtained from medicinal plants of family Lamiaceae and Compositae were done to check their therapeutic efficacy. Results obtained were submitted and added valuable information to literature.

<p> Isolation, structure elucidation of the compounds from medicinally important plants belonging to genera Symplococus and Ricinus is in progress. As extracts are reported to have good biological activity like antioxidant, antimicrobial activity etc, the biological activities of the isolated compounds will be done to check therapeutic importance of the selected plants.&nbsp;</p>

Isolation of compounds from extracts of Nepeta suaris were done and data obtained after structure elucidation and biological activities was reported to contribute new information to literature.

Isolation and structure elucidation  as well as Biological activities of Stachys parviflora are in progress. 

1.   Abstract

Biologically active 2-Arylbenzothiazoles derivatives has drawn interest towards synthesis of their new derivatives. Thiazole and its derivatives exist in a variety of natural products and a number of biologically active compounds.

2.   Literature Review and  Description

It is class of potent and selective antitumor agents which exhibit nanomolar inhibitory activity against a range of cancer cell lines i.e. human breast, colon and renal cell lines. Substituted thiazoles are an important class of biologically active compounds and are known to show a range of pharmacological activities like anti-tubercular, anti-parasitic, antimicrobial, anticancer etc. In addition, they possess significant utility as imaging agents for β-amyloid, chemiluminescent agents, calcium channel antagonists and photosensitizers.

Recently, benzothiazoles derivatives have been reported to show a competitive antifungal activity against Botrytis cinera as compared to commercially available fungicide Triadimefon; these compounds even has the potential to replace commercially available aryl-2-mercaptobenzothiazoles in agrochemicals.

Cyclooxygenase (COX) enzymes are involved in the production of prostaglandins which are subsequently involved in the cause of inflammation. There are two types of COX enzymes i.e. COX-1 and COX-2; whereas, COX-2 is selectively involved in causing inflammation. Currently, available marketed drugs NSAID’s are not selective inhibitors and inhibition of COX-1 cause ulceration; therefore, new selective inhibitors for COX-2 are required for more efficient treatment. Benzothiazole derivatives has been stated as active agents against COX-2 inhibition.

It is evident from the literature that this scaffold is biologically significant and synthesis of new derivatives can lead to potential molecules to show various biological activities.

3.   Scientific Objectives

Following are the main objectives of the project

1-Synthesis of new 2-arylbenzothiazoles derivatives.

2-Characterization of synthesized compounds using modern spectroscopic techniques.

3-Scientific publications (s) in the impact factor journals.

Drug development has been a principal driving force in the rapid maturation in the field of medicinal chemistry during the past several decades. Conjugated heterocyclic compounds possess extended π-systems have received substantial attention due to their synthetic and effective biological significances. Heterocycles bearing 1,3,4-oxadiazoles are reported to demonstrate a broad spectrum of pharmacological properties such as anti-depressant, antimicrobial, anticancer, anti-inflammatory, anticonvulsant, analgesic, antitubercular and anti-HIV activities

Based on these facts, designing of new chemical entities with potential biological effects require simulation of a suitable bioactive pharmacophore. The pharmacophore should not only require potency but must also be safer. In this perspective, the aim of current project is the synthesis of Oxadiazoles based Mannich Bases in order to explore the bioactivity profile as anti-depressant agent which may open up new opportunities for further investigations in one of the most vibrant and promising areas of research.

One-pot Access to Novel Thiazole Schiff Base Derivatives and Their Assessment as Potential Candidates for Diabetes Mellitus Inhibition

Natural products are fecund source of medicine since antiquity. Nature has selected plants as catalytic tool for healing. They stay vital to modern life as antibiotics, anti-cancer drugs, cardiac drugs, antifungal etc. The major achievements in the field of natural-products research of the past decades had clearly demonstrated that natural products represent an unparalleled and unquestionable source of molecular diversity for drug discovery and development, especially when many plant species are diminishing. Natural product holds firm position in medicinal industry so recent focus of pharmaceutical industry is to develop medicine based on isolation from plants. Pakistan is bestowed upon with wide variety of medicinal plants having enormous therapeutic activity. The research aim is to focus on plants that were used as folk medicines whose many varieties   are still untouched and unswayed. In the future, the synergy of natural-products research and biotechnology will drive new plant-drug development. The genus Polygonum & Fragaria are selected for the phyto-chemical investigation due to their immense therapeutic activity. The selected species for the investigation are Polygonum barbatum & Fragaria nubicola, Fragaria vesca. However the work may be extended to other plants. Plants will be collected and extracted, these extracts after concentration (on rotavap) will be subjected to chromatographic techniques. The isolated compounds will be identifying through different spectroscopic techniques (UV, IR, Mass, NMR). After that these pure compounds will be studied for biological assay. Natural products will be derivatized to see the effects of structural variations on the biological activities.

In silico Identification and In vitro evaluation of prospective inhibitors of alpha glucosidase

Dual Inhibition of a-Amylase and a-Glucosidase and their Mechanism of Action by Chemical Based Assay and Computational Studies

Effects of rigidity and flexibility on overall stability of proteins in extremophiles

Phytochemical investigation of the plants belonging to the genera Convolvulus and Stellaria is carried out for new compounds.