This thesis divided into four chapters and each chapter includes its own number of derivatives and references. Due to great biological significance of heterocyclic compounds, here in this dissertation we have described synthesis and bioactivities of benzothiazole, thiadiazole and isatin analogs in search of important therapeutic agents. Variety of benzothiazole, thiadiazole and isatin analogs were synthesized, characterized by 1HNMR, 13CNMR and HR-EIMS and screened for enzyme inhibition studies (α-glucosidase, α-amylase and thymidine phosphorylase activities). The results are separately discussed in the forthcoming chapter 1, 2 and 3. In first chapter, Benzothiazole based oxadiazole derivatives (122-144) have been synthesized and evaluated for α-glucosidase inhibition. All analogs exhibited a varying degree of α-glucosidase inhibitory potential with IC50 values ranging in between 0.5 ± 0.01 - 30.90 ± 0.70 μM when compared with the standard acarbose (IC50 = 866.30 ± 3.20 μM). In second chapter, two series of thiadiazole are described. In first series, thiadiazole quinoline analogs (180-209) were synthesized and screened for α-amylase inhibitory potential. Thirteen analogs 180, 181, 182, 183, 184, 185, 201, 202, 204, 205, 206, 207 and 209 showed outstanding α-amylase activity with IC50 values ranges between (0.002 ± 0.60 to 42.31 ± 0.17 μM) which is many folds better than standard acarbose having IC50 value 53.02 ± 0.12 μM. Eleven analogs 190, 192, 193, 194, 195, 197, 198, 200, 201, 202 and xxx 207 showed good to moderate inhibitory potential while seven analogs 187, 192, 195, 199, 200 and 208 were found inactive. In second series, 2-amino-thiadiazole based Schiff bases (211–219) were synthesized and screened for α-glucosidase inhibitory activity. All compounds showed outstanding α-glucosidase inhibition ranging between 2.30 ± 0.1μM to 25.30 ± 0.5μM when compared with the standard inhibitor acarbose having IC50 value 39.60 ± 0.70μM. Among the series, analogs 211, 214, 216 and 217 showed potent α-glucosidase activity which was more active than standard acarbose. The remaining analogs also showed excellent α-glucosidase inhibition. In third chapter, a new class of exceptionally potent isatin based oxadiazole (88-117) has been synthesized and evaluated for thymidine phosphorylase inhibitory potential. All analogs showed potent thymidine phosphorylase inhibition when compared with standard 7-Deazaxanthine, 7DX (IC50 = 38.68 ± 1.12 μM). In chapter four, procedures for different biological assay are described.
روگ ہجر دا دل نوں لا سٹیا سانوں عشق نے مار مکا سٹیا نہ خواباں تک اِنہاں سفنیاں نیں یوسف وچ کھوہ دے پا سٹیا ہوئے عشق دے وچ فقیر راجے جامہ حلیہ سب بدلا سٹیا سائنس نہیں کوئی عشق دا حل کر دی سائنس داناں مغز کھپا سٹیا جدوں عشق زلیخا دے کھچ کیتی یوسف مصر دے وچ لیا سٹیا مہینوال تجارتاں چھڈ بیٹھے پاسہ عشق نے سب پرتا سٹیا
On the one hand Islam espouses the notion of free trade, and on the other hand it frowns on state interference in trade. Developed and developing countries make head way freely in a free trading culture. This state of affairs buoys up the spirits of traders and inspires them to invest freely and lead to an economic upturn. Thus society flourishes. Foreign direct investment flows in a country from free trade. The scientificand technical expertise of industrialized countries is transferred to low income countries. Not only high quality products are available in abundance in the open market but also the moderation of prices is automatically established by the competition of business people. In this way, the free trading culture functions as a filtering device in the free market and, without any artificial or external interference, discharges all the tasks efficiently from its own internal logic. Critics of free trade, on the other hand, demur the system fills the coffers of multinational corporations but suppresses the rights of workers, locals and small industrialists. The real purpose of this system is to establish Western powers’ control over global resources. Taking advantage of the flexibility of the free trading culture, traders artificially raise prices through monopoly and hoarding.
Path planning and trajectory generation for nonholonomic mobile robot in dynamic environment is a difficult problem. It has to consider the nonholonomic constraints of robot as well as the detection and avoidance of the possible collision with dynamic obstacles. In this research an adaptive path planning technique has been proposed for mobile robot motion in an environment with dynamic obstacles. A trajectory is formulated between the starting and target positions for the three wheeled mobile robot. For this purpose kinematics and dynamic models of the mobile robot have been used. Inverse kinematics model has been developed by the wheel space technique for calculating the required wheels displacements to reach the target location. A collision-free motion of robot between its starting and goal positions is required to be executed therefore, a safe global path which is a sequence of control points is planned, incorporating the prior knowledge of environment. Artificial potential function has been implemented for calculating intermediate target positions between the initial and final position of mobile robot, to avoid obstacles in its path. A feasible global path is calculated for vthe known environment and a time based trajectory is generated. This global path is set as a reference path for the wheeled mobile robot. When dynamic obstacles moving with certain velocity come in the path of mobile robot, it has to modify the path to avoid possible collision. An algorithm is proposed in this dissertation which efficiently detects and avoids the possible collision with dynamic obstacles. This novel algorithm detects possible collision with dynamic obstacle even if its velocity is not uniform. Expected collision of obstacle coming in the path of mobile robot is detected by measuring the relative velocity of obstacle and mobile robot at each time step. The reactive scheme of algorithm is activated for changing the velocity of mobile robot to avoid the expected possible collision and the local path planner plans a modified path to be executed by the mobile robot.