{"title":"新型取代二硝基吩噻嗪衍生物的合成及其抗组胺作用","authors":"D. Bisht, Anita Singh, Ashok Sharma, V. Parcha","doi":"10.4103/jrptps.JRPTPS_72_21","DOIUrl":null,"url":null,"abstract":"Background: Phenothiazine consists of a three-ring structure compound in which two benzene rings are connected with nitrogen and sulfur atoms at nonadjacent sides. Phenothiazine and its substituted derivatives are abundantly able to produce a variety of important pharmacological and valuable therapeutic effects, and till now, these are under profound investigational processes. Objective: To synthesize and evaluate the antihistaminic potential of some newly synthesized dinitrophenothiazine derivatives. Materials and Methods: Different derivatives have been synthesized by the appropriate chemical scheme using dinitrophenothiazine as a basic nucleus. The completion of the chemical reactions has been monitored by thin-layer chromatography. The chemical structures of the newly synthesized products (P1–P25) were affirmed by elemental analysis and by spectral (infra-red, 1H nuclear magnetic resonance, and mass spectroscopy) findings and further examined for antihistaminic potential in guinea pigs. The synthesized products were also evaluated for their acute toxicity study and were found nontoxic. Results: The majority of the synthesized products of the dinitrophenothiazine series, namely, P07, P11, P12, P13, P15, P16, P17, P18, P19, and P20, have shown antihistaminic activity and compared with mepyramine (standard drug) at 0.8 µg/mL. Among the synthesized products, P18 was found to exhibit maximum antihistaminic activity. However, all the synthesized compounds were found to elicit a significant antihistaminic effect when compared with the standard drug. Conclusion: Therefore, dinitrophenothiazine compounds could be a good starting point to develop efficacious and potent analogues, as an antihistaminic agent in the treatment of allergic disorders.","PeriodicalId":16966,"journal":{"name":"Journal of Reports in Pharmaceutical Sciences","volume":"11 1","pages":"132 - 140"},"PeriodicalIF":0.7000,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Synthesis and antihistaminic potential of some novel substituted dinitrophenothiazine derivatives\",\"authors\":\"D. Bisht, Anita Singh, Ashok Sharma, V. Parcha\",\"doi\":\"10.4103/jrptps.JRPTPS_72_21\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Background: Phenothiazine consists of a three-ring structure compound in which two benzene rings are connected with nitrogen and sulfur atoms at nonadjacent sides. Phenothiazine and its substituted derivatives are abundantly able to produce a variety of important pharmacological and valuable therapeutic effects, and till now, these are under profound investigational processes. Objective: To synthesize and evaluate the antihistaminic potential of some newly synthesized dinitrophenothiazine derivatives. Materials and Methods: Different derivatives have been synthesized by the appropriate chemical scheme using dinitrophenothiazine as a basic nucleus. The completion of the chemical reactions has been monitored by thin-layer chromatography. The chemical structures of the newly synthesized products (P1–P25) were affirmed by elemental analysis and by spectral (infra-red, 1H nuclear magnetic resonance, and mass spectroscopy) findings and further examined for antihistaminic potential in guinea pigs. The synthesized products were also evaluated for their acute toxicity study and were found nontoxic. Results: The majority of the synthesized products of the dinitrophenothiazine series, namely, P07, P11, P12, P13, P15, P16, P17, P18, P19, and P20, have shown antihistaminic activity and compared with mepyramine (standard drug) at 0.8 µg/mL. Among the synthesized products, P18 was found to exhibit maximum antihistaminic activity. However, all the synthesized compounds were found to elicit a significant antihistaminic effect when compared with the standard drug. Conclusion: Therefore, dinitrophenothiazine compounds could be a good starting point to develop efficacious and potent analogues, as an antihistaminic agent in the treatment of allergic disorders.\",\"PeriodicalId\":16966,\"journal\":{\"name\":\"Journal of Reports in Pharmaceutical Sciences\",\"volume\":\"11 1\",\"pages\":\"132 - 140\"},\"PeriodicalIF\":0.7000,\"publicationDate\":\"2022-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Reports in Pharmaceutical Sciences\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.4103/jrptps.JRPTPS_72_21\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Reports in Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4103/jrptps.JRPTPS_72_21","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Synthesis and antihistaminic potential of some novel substituted dinitrophenothiazine derivatives
Background: Phenothiazine consists of a three-ring structure compound in which two benzene rings are connected with nitrogen and sulfur atoms at nonadjacent sides. Phenothiazine and its substituted derivatives are abundantly able to produce a variety of important pharmacological and valuable therapeutic effects, and till now, these are under profound investigational processes. Objective: To synthesize and evaluate the antihistaminic potential of some newly synthesized dinitrophenothiazine derivatives. Materials and Methods: Different derivatives have been synthesized by the appropriate chemical scheme using dinitrophenothiazine as a basic nucleus. The completion of the chemical reactions has been monitored by thin-layer chromatography. The chemical structures of the newly synthesized products (P1–P25) were affirmed by elemental analysis and by spectral (infra-red, 1H nuclear magnetic resonance, and mass spectroscopy) findings and further examined for antihistaminic potential in guinea pigs. The synthesized products were also evaluated for their acute toxicity study and were found nontoxic. Results: The majority of the synthesized products of the dinitrophenothiazine series, namely, P07, P11, P12, P13, P15, P16, P17, P18, P19, and P20, have shown antihistaminic activity and compared with mepyramine (standard drug) at 0.8 µg/mL. Among the synthesized products, P18 was found to exhibit maximum antihistaminic activity. However, all the synthesized compounds were found to elicit a significant antihistaminic effect when compared with the standard drug. Conclusion: Therefore, dinitrophenothiazine compounds could be a good starting point to develop efficacious and potent analogues, as an antihistaminic agent in the treatment of allergic disorders.
期刊介绍:
The Journal of Reports in Pharmaceutical Sciences(JRPS) is a biannually peer-reviewed multi-disciplinary pharmaceutical publication to serve as a means for scientific information exchange in the international pharmaceutical forum. It accepts novel findings that contribute to advancement of scientific knowledge in pharmaceutical fields that not published or under consideration for publication anywhere else for publication in JRPS as original research article. all aspects of pharmaceutical sciences consist of medicinal chemistry, molecular modeling, drug design, pharmaceutics, biopharmacy, pharmaceutical nanotechnology, pharmacognosy, natural products, pharmaceutical biotechnology, pharmacology, toxicology and clinical pharmacy.