Pub Date : 2024-01-29DOI: 10.3897/pharmacia.71.e111984
Zahra Jawd Mohammed Ali Al-Musawi, Atheer M. R. Al-juhaishi
This study aimed to assess the role of D2 receptor A-241G (rs1799978) genetic polymorphism and olanzapine response and safety in Iraqi schizophrenic patients. The case-control study composed of 100 schizophrenic patients consisting of both genders were recruited from the Psychiatry Outpatient Department and 50 apparently healthy volunteers, served as a control group. Patient response to olanzapine was evaluated with the aiding of the PANSS and genotyping of D2 receptor A-241G (rs1799978) polymorphisms was detected using the nested PCR method. The heterozygous (AG) and mutant (GG) alleles of D2 receptor A-241G (rs1799978) were significantly predominated in schizophrenic patients and absent in healthy volunteers. Schizophrenic patients with the G allele of D2 receptor A-241G (rs1799978) and who were administered olanzapine exhibited a notable resistance to olanzapine. In conclusion, the genetic polymorphism of D2 receptor A-241G (rs1799978) was significantly associated with resistance to olanzapine in Iraqi schizophrenic patients.
{"title":"Association study between D2 receptor A-241G, rs1799978 genetic variation and olanzapine efficacy in Iraqi schizophrenic patients","authors":"Zahra Jawd Mohammed Ali Al-Musawi, Atheer M. R. Al-juhaishi","doi":"10.3897/pharmacia.71.e111984","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e111984","url":null,"abstract":"This study aimed to assess the role of D2 receptor A-241G (rs1799978) genetic polymorphism and olanzapine response and safety in Iraqi schizophrenic patients. The case-control study composed of 100 schizophrenic patients consisting of both genders were recruited from the Psychiatry Outpatient Department and 50 apparently healthy volunteers, served as a control group. Patient response to olanzapine was evaluated with the aiding of the PANSS and genotyping of D2 receptor A-241G (rs1799978) polymorphisms was detected using the nested PCR method. The heterozygous (AG) and mutant (GG) alleles of D2 receptor A-241G (rs1799978) were significantly predominated in schizophrenic patients and absent in healthy volunteers. Schizophrenic patients with the G allele of D2 receptor A-241G (rs1799978) and who were administered olanzapine exhibited a notable resistance to olanzapine. In conclusion, the genetic polymorphism of D2 receptor A-241G (rs1799978) was significantly associated with resistance to olanzapine in Iraqi schizophrenic patients.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140490144","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2024-01-29DOI: 10.3897/pharmacia.71.e110013
S. Vlasov, O. Borysov, H. Severina, V. Vlasov, Amjad Ibrahim M. Abu Sharkh, V. Georgiyants
According to the recent studies bezylcarboxamide fragment attached to the thiophene ring of thieno[2,3-d]pyrimidine is beneficial for antimicrobial activity of the compounds. Therefore we focused our efforts on constructing of the simple molecules such as N-(benzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamides to get deeper insight into their antimicrobial activity. As the optimal procedure for preparation of target compounds we choose 1,1’-carbonyldiimidazole promoted interaction of 5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid with the series of substituted benzyl amines. The obtained amides showed good activity against the strains of S. aureus and B. subtilis, which was higher for the derivative without substituents in benzene ring or the compounds with small substituents like methyl or methoxyl groups in the para-position of the benzene ring. Docking studies showed that despite the good values of the scoring functions, the conformational analysis of the ligands’ poses in the active site revealed their ability for only partial inhibition of TrmD of P. aeruginosa.
{"title":"Synthesis, in silico and in vitro antimicrobial activity of N-(benzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamides","authors":"S. Vlasov, O. Borysov, H. Severina, V. Vlasov, Amjad Ibrahim M. Abu Sharkh, V. Georgiyants","doi":"10.3897/pharmacia.71.e110013","DOIUrl":"https://doi.org/10.3897/pharmacia.71.e110013","url":null,"abstract":"According to the recent studies bezylcarboxamide fragment attached to the thiophene ring of thieno[2,3-d]pyrimidine is beneficial for antimicrobial activity of the compounds. Therefore we focused our efforts on constructing of the simple molecules such as N-(benzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamides to get deeper insight into their antimicrobial activity. As the optimal procedure for preparation of target compounds we choose 1,1’-carbonyldiimidazole promoted interaction of 5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid with the series of substituted benzyl amines. The obtained amides showed good activity against the strains of S. aureus and B. subtilis, which was higher for the derivative without substituents in benzene ring or the compounds with small substituents like methyl or methoxyl groups in the para-position of the benzene ring. Docking studies showed that despite the good values of the scoring functions, the conformational analysis of the ligands’ poses in the active site revealed their ability for only partial inhibition of TrmD of P. aeruginosa.","PeriodicalId":508564,"journal":{"name":"Pharmacia","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140490083","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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