Review: 37 refs.

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Review: 19 refs.

Objective:The present work deals with the designing, scoring, synthesis and, characterization of 1-(4-(2-(4-Substitutedphenylamino)-2oxoethyl)phenylsulfonyl)-3-(4-substitutedbenzoyl)urea (5A-5B),1-(4-(2-(4-substitutedphenylamino)-2-oxoethyl)phenylsulfonyl)-3-(4-substitutedbenzoyl)guanidine(5C-5E) and, 1-(4-Substitutedbenzoyl)-3-(4-(2-oxo-2-(piperazin-1-yl)ethyl)phenylsulfonyl)urea (5F-5H) based derivatives as hypoglycemic agents.Methods: Docking calculations were performed to predict the binding affinity between the AKR1C1 complexes and sulphonylureas compounds using the Glide docking program. Docking studies on LigPrep treated ligands were carried out to predict the binding pocket of protein 4YVP using the docking program. The QikProp program was used to predict the ADME/T properties of the analogues. All these newly synthesized compounds were screened for their in vivo hypoglycemic activity by most relevant animal models like alloxan-induced diabetic rats by measuring blood plasma concentration compared with reference drug glibenclamide.Results: Novel compounds 1were synthesised and characterized using spectral and analytical data. The results of molecular docking and in vivo hypoglycemic activity, all compounds have shown considerable activity with respect to glibenclimide, but compounds 5D (52.49±7.73) and 5E(48.18±4.22)are equipotent with respect to activity as compared to standard glibenclamide(55.97±3.19). Conclusion:Compounds 5D and 5E have exhibited good hypoglycemic activity,hence both the derivatives will consider as a lead molecule and further some modification in their structures to get a more potent anti-diabetic agent.Group I: Normal-Normal controlled rats fed with 0.5 ml of normal saline.Group II: Diabetic control (DC) rats; fed with 0.5 ml of normal saline.Group III: Diabetic rats treated with standard drug Glibenclamide 5 mg/kg body wt. Group IV: Diabetic rats; treated with synthesized drug No 5A in 1% CMC 50 mg/kg of body weight. Group V: Diabetic rats; treated with synthesized drug No 5B in 1% CMC 50 mg/kg of body weight Group VI: Diabetic rats; treated with synthesized drug No 5C in 1% CMC 50 mg/kg of body weight Group VII: Diabetic rats; treated with synthesized drug No 5D in 1% CMC 50 mg/kg of body weight Group VIII: Diabetic rats; treated with synthesized drug No 5E in 1% CMC 50 mg/kg of body weight Group IX: Diabetic rats; treated with synthesized drug No 5F in 1% CMC 50 mg/kg of body weight Group X: Diabetic rats; treated with synthesized drug No 5G in 1% CMC 50 mg/kg of body weight Group XI: Diabetic rats; treated with synthesized drug No 5H in 1% CMC 50 mg/kg of bodyThe dose for the newly synthesized compounds was decided on the basis of literature survey. [29] Glibenclamide was taken as the standard. The blood glucose level was determined at 0 and 3 h after administration of test compound using glucometer (Johnson and Johnson Pvt. Ltd.) % reduction in plasma glucose level was calculated for each animal. Statistical analysisPanchal et al. Pharm Sci, Vol 9, Issue 12, 226-232 Int J Pharm

The objective of the present review is to evaluate the therapeutic potential of phytochemicals against arthritis, which is asymptomatic disorder of chronic joint inflammation followed by swelling and pain. Here, we discussed about the anti-arthritic activity of many phytomolecules such as Norisoboldine, Berberine, Triptolide, Hesperidin Hesperidin, Madecassocide, Hydroxy napthoquinone, Ginsenoside, Cryptotanshinone, Kirenol, Thymoquinone, Chlorogenic acid, Curcumin, Bromelain, Andrographolide and Allicin. These compounds are able to control inflammatory responses, proinflammatory cytokines, osteoclast differentiation and to prevent bone erosion in the joints. In this article, we reviewed anti-arthritic activities of phytichemicals from 2011-2019, using various scientific websites like PubMed, Google Scholar, Science Direct etc. Till date clinical trials conducted with anti-arthritic phytomolecules are very less. Hence, more clinical trials are needed to bring plant molecules as safe and effective anti-arthritic drugs in the market, either alone or in combination with other anti-arthritic agents.