Design and development of electronic jacquard for Korai mat weaving loom

A low-cost computerised mat weaving handloom has beendeveloped. After successful field trials at the client locations,300% increase in productivity is observed. Now any weaver canweave mat of any design within 2 days instead of 6-8 days,increasing their earning per mat. Easy to use pedallingmechanism, electronic jacquard and the software tool aredeveloped. This innovation facilitates electronic design storage,eliminates recurring cost on punched cards and the weaverdependence on designers while weaving marriage mats. The welldesigned pedalling and jacquard lifting mechanism results inbetter ergonomics. The system is designed to operate with powerof just 75 watt, so that it can be driven by solar power

Synthesis and SAR studies of potent H+/K+-ATPase inhibitors of quinazolinone-Schiff’s base analogues

A series of quinazolinone derived Schiff base derivatives 7–36 were synthesized and characterized by analytical and spectroscopic techniques. The synthesized analogues were screened for their in vitro H+/K+-ATPase inhibition. Most of the compounds showed excellent activity, compared to that of omeprazole, a reference drug. In particular, hydroxy and methoxy derivatives 13–24 were the most active compounds possessing a significant increase for different substituents on the benzene ring thus, contributing positively to gastric H+/K+-ATPase inhibition. Preliminary structure-activity relationship revealed that the compounds 13–24 with electron donating moiety (OH, OCH3) were found to be excellent activity and compounds 9–12 and 25–36 with electron withdrawing moiety (Cl, F, NO2 and Br) were found to be least antiulcer agents

Synthesis and SAR studies of urea and thiourea derivatives of Gly/Pro conjugated to piperazine analogue as potential AGE inhibitors

Synthesis of a series of urea and thiourea derivatives of glycine and proline conjugated to 2,3-dichlorophenyl piperazine has been reported. The structures were confirmed by physical and spectroscopical measurements followed by characterization of antiglycation activity. All synthesized compounds were able to inhibit protein glycation, particularly halogen containing derivatives without preference of oxygen or sulphur at the urea function. The best analogues are nearly 20 fold (\textless 5 μM) more potent than the reference standard, rutin (41.9 μM)

Design and synthesis of amino acids-conjugated heterocycle derived ureas/thioureas as potent inhibitors of protein glycation

Protein glycation is believed to play an important role in the development of long-term disorders associated with diabetic complications. In view of the wide occurrence of advanced glycation end products (AGE's) and the oxidative stress derived from them in a variety of diabetic complications, it would be of great interest to identify and develop AGE inhibitors. In this study, synthesis and in vitro antiglycation activity of a small library of forty urea/thiourea derivatives of Phe/Tyr/Glu/Lys-benzisoxazole hybrids are reported. Structures of the compounds were confirmed by IR, NMR, mass spectrometry, and elemental analysis. Most of the title compounds exhibited promising activity. Best antiglycation activity was found for Tyr analogue with methoxy group as a substituent particularly at the para position with IC50 value of 1.9 μM against the positive control, Rutin, with IC50 = 41.9 μM. Thus, the title compounds represent novel class of potent antiglycating agents

Design and development of electronic jacquard for Korai mat weaving loom

360-364A low-cost computerised mat weaving handloom has been developed. After successful field trials at the client locations, 300% increase in productivity is observed. Now any weaver can weave mat of any design within 2 days instead of 6-8 days, increasing their earning per mat. Easy to use pedalling mechanism, electronic jacquard and the software tool are developed. This innovation facilitates electronic design storage, eliminates recurring cost on punched cards and the weaver dependence on designers while weaving marriage mats. The well designed pedalling and jacquard lifting mechanism results in better ergonomics. The system is designed to operate with power of just 75 watt, so that it can be driven by solar power

Synthesis and evaluation of novel ureido/thioureido derivatives of amino acid conjugated 2,3-dichlorophenyl piperazine as highly potent antiglycating agents

We report the synthesis and in vitro antiglycation activity of more than 80 amino acid–heterocycle conjugate derived ureas and thioureas. They were characterized by physical and spectroscopical methods. Many of the analogues synthesized showed activity at the sub-micro molar level. Introduction of different amino acids as linker and systematic variation of the substituents on the aromatic ring revealed promising leads. In particular, compounds containing Glu and Tyr as the linkers exhibited high antiglycating potency with IC50 1–4μM as against the reference, rutin with IC50 41.9μM. Conclusions Compounds bearing halogen atoms emerged as the most active analogues and serve as lead for future studies

An unexpected reaction to methodology: An unprecedented approach to transamidation

This report describes an unprecedented protocol for the synthesis of N,N′-substituted ureas using a cross-coupling method. Mono substituted ureas were modified by an economically viable and simple method using commercially available isocyanates and sodium hydride as the reagents. In addition, the method involves no expensive metal complexes or catalysts and all reactions are carried out at room temperature. Furthermore, both symmetrical and asymmetrical ureas were successfully obtained in single step reactions with reasonable yields

Benzisoxazole: a privileged scaffold for medicinal chemistry

The benzisoxazole analogs represent one of the privileged structures in medicinal chemistry and there has been an increasing number of studies on benzisoxazole-containing compounds. The unique benzisoxazole scaffold also exhibits an impressive potential as antimicrobial, anticancer, anti-inflammatory, anti-glycation agents and so on. This review examines the state of the art in medicinal chemistry as it relates to the comprehensive and general summary of the different benzisoxazole analogs, their use as starting building blocks of multifarious architectures on scales sufficient to drive human drug trials. The number of reports describing benzisoxazole-containing highly active compounds leads to the expectation that this scaffold will further emerge as a potential candidate in the field of drug discovery

Inhibition of protein glycation by urea and thiourea derivatives of glycine/proline conjugated benzisoxazole analogue-Synthesis and structure-activity studies

Synthesis of a new series of urea/thiourea derivatives of Gly/Pro conjugated benzisoxazole has been reported. Structure of the compounds was characterized by physical and spectroscopical data and has been screened for their in vitro antiglycation activity. Several compounds showed promising activity with IC50 < 5 μM compared to standard rutin (IC 50 = 41.9 μM). Further, it was found that compounds containing methoxy and bromine substituents have exerted highly potent activity. Thus, the title compounds represent novel class of potent antiglycating agents